ES2350748T3 - PREPARED UNDERSTANDING HYPERMARKED POLYMERS. - Google Patents

Abstract

Prepared in the form of particles comprising at least one substance of low molecular weight with a molecular weight in the range of 15 g / mol to 1000 g / mol and at least one hyperbranched polymer, characterized in that the particles have a size comprised in the range of 1 μm to 1000 μm, the low molecular weight substance is included in a sheath, which contains hyperbranched polymer, and the hyperbranched polymer contains a hydrophilic core with polyester units and hydrophobic end groups, where the hyperbranched polymer has a higher molecular weight or equal to 6000 g / mol and a hydroxyl number in the range of 0 to 200 mg KOH / g, the degree of branching being in the range of 20 to 70% and the hyperbranched polymer has a melting temperature of at least 30 ° C

Description

Preparations comprising polymers hyperbranched

The present invention relates to preparations comprising at least one substance of low molecular weight and at less a hyperbranched polymer.

Hyperbranched polymer preparations as well as low molecular weight substances they know themselves. By general rule preparations of this type are used in order to achieve a delayed action of the low molecular weight substance. Additionally, preparations of this type exhibit numerous positive properties

Hyperbranched polymers are described in many places. For example, polymers of this type are exposed in EP-A 0 630 389. This document contains particularly describe hyperbranched polyesters, which can used in acrylic resins, saturated polyester resins and unsaturated polyester resins, epoxy resins, phenolic resins, polyurethane resins or dental materials. A use of these polymers as carrier material, in order to release so delayed low molecular weight substances, not described in this document.

Additionally, polymers are exposed hyperbranched in WO 97/06825. Hyperbranched polymers described in this document are in many cases polyamides, which They can be used in a multitude of applications. In this case it is essential that the initiating molecule be an aromatic compound, which can be transformed into a simple process step into a polymer hyperbranched The hyperbranched polymers thus obtained can  be used in a multiplicity of applications. They belong to them particularly plastic building materials, fibers, sheets, plastic materials for the production of bottles, vehicles for medications, as well as membranes and supports for catalysts

The production of hyperbranched polymers is further described in J. Chem. Soc. Perkin Trans. 1992 (pages 2459-2469), where the hyperbranched polymer is Produces in a multi-step process.

In Macromolecules 1993, 26, pages 4617-4623 the production of a polyester is exposed hyperbranched aromatic with terminal groups phenol and acetate. The synthesis is based on a melting condensation of monomers A 2 B, for example chloride 3,5 (bistrimethylsiloxy) benzoyl and acid 3,5-diacetoxybenzoic.

US 5041516 publishes a multi-step process for the production of polyesters from aliphatic monomers and aromatic

Additionally, the production of polyesters from aromatic and aliphatic monomers in US 5,136,014. In addition, patent specification US 5,183,862 describes the production of hyperbranched polyesters from aliphatic and aromatic monomers.

Additionally, US 5,196,502 discloses the production of aromatic hyperbranched polyesters with use of diacetoxybenzoic acids and acids monoacetoxidibenzoic.

US 5,225,522 publishes polyesters multi-branched with aliphatic and aromatic groups as well as processes for its production.

Additionally, publication US 5,227,462 describes hyperbranched polyesters, which may contain groups both aliphatic and aromatic.

Compositions for the production of inks that contain hyperbranched polymers are published in the US 5,266,106.

The production of polymer particles surface functionalized, described in US 5,306,561.

US 5,362,843 publishes a process for the production of hyperbranched macromolecules.

US 5,418,301 publishes a process for the production of dendritic macromolecules.

Additionally, WO 98/30604 describes compositions that may comprise polymers hyperbranched as well as metal compounds. In this case it particularly expose polyamidoamines and polyesters.

Additionally, in WO 2004/072153 the use of hyperbranched polymers as a vehicle for medicines, where it is said that the vehicle molecule facilitates a delayed release as well as a transport of medications to the cells. In this regard modified dendrimers are exposed particularly, which exhibit nitrogen groups.

Additionally, publication WO 00/065024 describes polymers with cells for encapsulation of molecules hydrophobic In this case a multiplicity of remains are combined hydrophobic with a polyol core, then transformed the polymer obtained by polyalkylene oxides, in order to obtain a water soluble polymer.

Additionally, publication WO 2005/034909 describes compositions comprising a hyperbranched polymer, which is coupled to a biologically active moiety.

In addition, publication WO 03/037383 describes preparations comprising hyperbranched polymers. As polymers hyperbranched polyamidoamines are particularly exposed or polypropylene amines

Additionally polymers are described hyperbranched in WO 00/06267, exposing as hyperbranched polymers particularly polyetherimides.

Additionally prepared, which they comprise dendritic polymers and pharmaceutical active ingredients, in WO 03/033027, where the dendrimer comprises groups cationic

a) Additionally, the use of hyperbranched polymers for the selective release of active ingredients has been described by Zou et al . Macromol Biosci 5 (2005) 662-668. In this case, hyperbranched polymers are provided with ionic groups. The molecular weight of the hyperbranched polymers used is approx. 5500 g / mol, without indicating any melting temperature of the hyperbranched polymer.

b) Additionally, they are described in the Publications US 6,379,683 or EP 1,034,839 B1 nanocapsules, which They contain hyperbranched polymers. Hyperbranched polymers exhibit a molecular weight of approx. 4800 g / mol.

Additionally, they are described in WO 97/14404 Compositions comprising dendrimers. However, these dendrimers do not serve for encapsulation of substances. In WO 97/14404 are not described prepared within the meaning of this invention.

Compositions containing polyesters Dendritic are described in US 6,284,233. However, polyesters Dendritic does not work for the encapsulation of substances. In U.S 6,284,233 are not described as prepared herein. invention.

The use of dendritic polymers with hydroxyl functionality in cosmetic compositions is described in WO 01/17485. However, these compositions do not contain prepared any in the sense of the present invention.

The dissertation of S. Suttiruengwong "Silica Aerogels and Hyperbranched Polymers as Drug Delivery Systems ", Erlangern 2005, describes encapsulated systems that may contain hyperbranched polymers. However, the polymers described have a molecular weight of 4600 g / mol at most, without specify any data about the melting temperature of the hyperbranched polymer

Publication DE 10 2004 026 904 describes hyperbranched polyesters, which are particularly suitable As an ingredient in printing inks. However, these hyperbranched polyesters do not serve to encapsulate substances In DE 10 2004 026 904 no preparations are described in the sense of the present invention.

Publication US 6,525,170 also describes hyperbranched polyesters. However, the polyesters of Examples contain a hydrophobic core. Additionally, the polymers have a molecular weight of approx. 1400 g / mol before the various transformations, without being explicitly described the properties of the polymers obtained after the modification. Additionally, there is a lack of data regarding glass transition temperatures or melting points of the polymers obtained.

Additionally, document US 2002/0002242 publishes hyperbranched polymers, which are used for modification of surface properties. In this case the core of these polymers can be hydrophobic, exhibiting the polymers globally amphiphilic properties. These polymers do not work for encapsulation of low molecular weight substances. I dont know describe preparations within the meaning of the present invention.

Publication US 2003/0114553 describes dental compositions, which may contain star polymers. However, no hyperbranched polymer is exposed with a hydrophilic core and hydrophobic end groups. Are not described neither prepared for the delayed release of compounds of low molecular weight

In addition, US 2004/016394 describes cosmetic compositions, which may contain polymers hyperbranched However, the properties of these polymers hyperbranched, particularly molecular weight, the degree of branching, hydroxyl number or melting point is not They mention explicitly.

Additionally polymers are exposed hyperbranched in WO 93/17060. However, these polymers do not describe in relation to the controlled release of compounds of low molecular weight They are not exposed prepared in the sense of present invention

Publication WO 2006/031388 publishes polymers dendritic, which can be used particularly in applications orthopedic However, many different polymers are exposed, without any of the explicitly exposed polymers exhibiting the all of the properties of hyperbranched polymers to Use in this case. Thus, data is particularly lacking as far as to the melting point of the polymers. Additionally, it is not described any hyperbranched polymer with a hydrophilic core and groups hydrophobic terminals, exhibiting a molecular weight of at least 6000 g / mol

WO 2006/031358 publishes polymers dendritic, which can be used particularly in applications ophthalmic However, a large number of polymers are exposed. different, without any of the exposed polymers explicitly display all the properties of polymers hyperbranched to use in this case. Thus they are particularly lacking data regarding the melting point of the polymers. further no hyperbranched polymer with a core is described hydrophilic and hydrophobic end groups, having a weight molecular of at least 6000 g / mol.

Therefore, it should be noted that a multitude of preparations have been described, comprising polymers hyperbranched as well as low molecular weight compounds. Without However, the long-standing commitment to provide preparedness remains most advantageous possible.

Given the state of the art indicated and set forth herein, was within the scope of the present invention provide preparations that exhibit a property profile excellent.

In particular, the corresponding preparations to the invention they should release the low molecular weight substance in a medium selected to the greatest extent possible along a prolonged period of time, the release should be the most constant possible.

According to an additional aspect, the release of low molecular weight substances should be able to control as much Simple and reliably possible.

Subsequently, it was the objective of the present invention provide preparations that have a content particularly high of the low molecular weight substance.

Additionally, the preparation should exhibit a particularly high stability, so that the substances of particularly sensitive low molecular weight can be stored for a particularly long period of time, without the properties of the low molecular weight substance are altered essentially. In this context, the preparations should exhibit a particularly high shear stability, so that it is possible a transformation of the preparations simple and without problems.

These purposes and others, which have not been explicitly mentioned, but that can be deduced as obvious from the ideas presented here, or that are inferred logically of these, are resolved by the preparations described in the claim 1. Suitable modifications of these preparations are put under protection in the referred secondary claims to claim 1.

So, thanks to a hyperbranched polymer that it comprises a hydrophilic core with polyester units as well as groups hydrophobic terminals,

where the hyperbranched polymer has a weight molecular greater than or equal to 6,000 g / mol and a hydroxyl number in the range of 0 to 200 mg KOH / g, whose degree of branching is in the range of 20 to 70% and the hyperbranched polymer has a melting temperature of at least 30 ° C, it is possible to provide, in an unpredictable way, preparations comprising at least one molecular weight substance low and at least one hyperbranched polymer, which exhibit a profile of properties improved.

Thanks to the measures corresponding to the One or more of the following advantages can be obtained:

According to a particular aspect, the preparations corresponding to the invention release the weight substance low molecular rate in a multiplicity of media along a particularly long period of time.

According to another embodiment of the present invention, the release of the low molecular weight substance can take place after a period of storage Long in a short period.

In both embodiments, the release it can be controlled by external parameters, for example temperature, pH, radiation frequency and class of the medium that circle the preparation.

Additionally, the preparation exposed in the this case makes a particularly stable conservation possible of sensitive substances of low molecular weight. Therefore, substances can be stored safely and easily, being able to reduce in many cases a risk of fire and / or explosion.

In addition, substances can be preserved chemically active, particularly oxidizing, without these substances are active in the environment.

In addition, the preparations corresponding to the invention are surprisingly stable, so these can keep for a prolonged period of time, without having degradation place. Otherwise, preparations can transform, due to its high shear stability, easily and favorably in costs.

Additionally, the corresponding preparations to the invention, depending on the low molecular weight substance, They are harmless from a health point of view.

On the other hand, the corresponding preparations to the invention may contain a particularly high proportion of the low molecular weight substance.

Due to the highly branched structure of the polymer and the ability to adjust solubility properties of the polymer by the number of hydrophobic groups, can in as opposed to the state of the art, get a better control over the amount of low molecular weight substance that is free per unit of time.

Load concentration in the preparation corresponding to the invention of the molecular weight substance low per g of vehicle polymer may, due to the structure hyperbranched polymer and the possibility of adjusting polymer solubility properties by the number of groups hydrophobic, fit specifically for application. In this context can even be reached load concentrations that are clearly higher than the load concentrations of the technique above (more than 20% by weight of low molecular weight substance referred to the binary system consisting of polymer and substance of low molecular weight).

Unexpectedly, it has been found that in case of hyperbranched vehicle polymers the processes of encapsulation can work with clearly reduced quantities of solvents or compressed gases. Hyperbranched polymer can behave both by itself and solvent / dispersant The solvent / gas concentrations reduced in this way lead compared to the technique previous to safer processes, given that polymers hyperbranched cannot form explosive vapors of any kind as other solvents of the prior art.

The preparations corresponding to the invention they comprise a hyperbranched polymer with a hydrophilic core. Hydrophilic means that the nucleus is able to absorb an amount high water According to a preferred aspect of the present invention, the hydrophilic core is soluble in water. Preferably, Water solubility at 90 ° C is at least 10% by weight, so particularly preferred at least 20% by weight. This magnitude is measured based on the hyperbranched polymer before the hydrophobicization, that is to say on the hydrophilic core as such. The measurement can be performed according to the method called the flask, in the which measures the water solubility of the pure substance.

In this method, the substance (the materials solids have to be sprayed) dissolves in water at a temperature that is slightly higher than the temperature of the proof. When saturation is reached, the solution is cooled and keeps at the temperature of the test. The solution is stirred until That balance is reached. In an alternative, the measure can be performed directly at the test temperature, when by respective sampling makes sure that the saturation balance. In such case, the concentration of the test substance in the aqueous solution, which must not contain any particle of undissolved substance, is determined with a appropriate analysis method.

The hydrophilic core preferably exhibits a hydroxyl number measured before hydrophobicization included in the range of 400 to 600 mg KOH / g, particularly preferred in the range of 450 to 550 mg KOH / g. This property is measured according to ASTM E222. In this case, the polymer is reacted with a defined amount of acetic anhydride. Anhydride Unprocessed acetic acid is hydrolyzed with water. Then you Titrate the mixture with NaOH. The hydroxyl number is obtained at from the difference between a comparison sample and the value measured for the polymer. In this case, the number of acidic groups of the polymer.

The hyperbranched polymer corresponding to the The invention exhibits a core comprising polyester units. Hyperbranched polymers with polyester units are described particularly in EP 0 630 389. As a rule, in most of cases the hydrophilic core is a central unit that is derived of an initiator molecule with at least 2, preferably at least 3 hydroxy groups, and the repeating units are derived from monomers containing at least one carbonyl group and at least two groups hydroxy

Highly branched globular polymers, they are also designated in the technical literature as "polymers dendritic ". These dendritic polymers synthesized from of multifunctional monomers can be classified into two categories different, the "dendrimers" and the "polymers hyperbranched ". Dendrimers have a structure of very regular generation, with radial symmetry. They supply mono-dispersed globular polymers, since, - in comparison with hyperbranched polymers - are produced in multi-stage synthesis with a high synthesis expense. In this case The structure is characterized by three different areas: - the core polyfunctional, which constitutes the center of symmetry, - different well defined layers with radial symmetry of a repetitive unit (generation) and - the terminal groups. Polymers Hyperbranched are, as opposed to dendrimers, polydisperses and, in regards to its branching and structure irregular. In addition to dendritic and linear units, there are also - as opposed to dendrimers - in polymers hyperbranched linear units.

Regarding the various possibilities for the synthesis of dendrimers and hyperbranched polymers, it refer to

a) Fréchet J.M.J., Tomalia D.A., Dendrimers and Other Dendritic Polymers, John Wiley & Sons, Ltd., West Sussex, UK 2001 as well as

b) Jikei M., Kakimoto M., Hyperbranched polymers: a promising new class of materials, Prog. Polym. Sci., 26 (2001) 1233-1285 and / or

c) Gao C., Yan D., Hyperbranched Polymers: from synthesis to applications, Prog. Polym. Sci., 29 (2004) 183-275

which are hereby incorporated as references and are applicable as part of the publication of the present invention

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Hyperbranched and highly polymers Branches described in these publications are also polymers Preferred vehicle within the meaning of the present invention. In in relation to this it is preferred that hyperbranched polymers possess at least 3 repetitive units per molecule, preferably at least 10 repetitive units per molecule, and so additionally preferred at least 100 repetitive units per molecule, additionally preferably at least 200 units repetitively and additionally preferably at least 400 repetitive units, which exhibit in each case at least three, preferably at least four linking possibilities, where at minus three of these repetitive units, particularly preferred at least 10 and additionally preferred at least 20 in each case at least three, preferably at least four linking possibilities are linked with at least three, preferably at least four repetitive units additional.

In many cases, hyperbranched polymers display at most 10,000, preferably at most 5000 and of particularly preferred mode at most 2500 units repetitive

In a preferred embodiment, the highly branched polymer exhibits at least three units repetitive, which respectively exhibit at least 3 possibilities of possible union, where at least three of these repetitive units They exhibit at least two possible link possibilities.

In this case, under the concept "unity repetitive "is preferably understood as a structure that Repeat in all cases within the hyperbranched molecule. Under the concept "link possibility" is understood preferably that functional structure within a unit repetitive with which a union to another unit is possible repetitive Referring to the examples presented above of a dendrimer or a hyperbranched polymer, the unit repetitive is a structure that contains in each case three joining possibilities (X, Y, Z):

one

The combination units link individual to each other can take place by polymerization of condensation, by radical polymerization, by polymerization anionic, by cationic polymerization, by polymerization with group transfer, by coordinative polymerization or by polymerization with ring opening.

The initiator molecule concepts, as well as Repetitive unit are universally known to experts. Thus, hyperbranched polymers to be used according to the invention can be obtained by polycondensation, where from an alcohol polyvalent acid groups are first transformed carboxylic of the monomers. In this case ester groups are formed. Since the monomers contain at least two hydroxy groups, the macromolecule exhibits after each transformation more groups hydroxyl than before transformation.

Preferably, the initiator molecule is a aliphatic polyol, preferably containing 3, 4, 5, 6, 7 or 8, of particularly preferably 3, 4 or 5 hydroxy groups.

Particularly preferred, the molecule Initiator is selected from ditrimethylolpropane, ditrimethylolethane, dipentaerythrite, pentaerythrite, alkoxylated pentaerythrite, trimethylolethane, trimethylolpropane, alkoxylated trimethylolpropane, glycerin, neopentyl alcohol, dimethylolpropane and / or 1,3-dioxane-5,5-dimetanol.

According to a particular aspect of the present invention, the repetitive units are derived from monomers with a carboxyl group and at least two hydroxy groups. To these monomers Preferred belong particularly dimethylpropionic acid, acid α, α-bis (hydroxymethyl) butyric acid, acid α, α, α-tris (hydroxymethyl) acetic acid,  acid α, α-bis (hydroxymethyl) valeric, acid α, α-bis (hydroxy) propionic and / or 3,5-dihydroxybenzoic acid.

Very particularly preferably, the core hydrophilic is obtained by acid polymerization dimethylolpropionic, being used as a starting molecule so particularly preferred dithrimethylolpropane, trimethylolpropane, ethoxylated pentaerythrite, pentaerythrite or glycerin.

According to a preferred embodiment, the hydrophilic core preferably has a molecular weight of at least 1500 g / mol, preferably at least 2500 g / mol. This magnitude refers to the weighted average molecular weight value (Mw), which can be measured by gel permeation chromatography, the measurement being carried out in DMF and using polyethylene glycols as a reference (see among others Burgath et al . In Macromol. Chem. Phys., 201 (2000) 782-791). In this case, a calibration curve is used, which has been obtained using standards of polystyrene as a standard. This magnitude therefore represents an apparent measurement value.

Preferably, the hydrophilic core may exhibit a glass transition temperature that is comprised in the range of -40 to 60 ° C, particularly preferably 0 to 50 ° C and very particularly preferably 10 to 40 ° C. The glass transition temperature can be determined by the DSC procedure, a heating rate of 3 ° C / min (peak of tan DNA δ; Netzsch DMA 242, flexion of 3 points, 1 Hz, 3 ° C / min).

The surface hydrophobicization is obtained as a rule as the last reaction step by transformation of at least a part of the free hydroxyl groups, preferably with a long chain carboxylic acid.

Preferably, the degree of functionalization of the hyperbranched core molecule with terminal groups hydrophobic, preferably with fundamental units containing fatty acids, is at least 30%, particularly preferably at least 40% According to a further aspect of the present invention, the degree of functionalization of the core molecule hyperbranched with hydrophobic end groups, preferably with fundamental units that contain fatty acids, is in the range of 30 to 100%, preferably in the range of 35 to 95%, particularly preferably in the range of 40 to 90% and very particularly preferred in the 45 to 85% range.

The degree of functionalization refers to the proportion of hydroxyl groups that are transformed by the hydrophobicization Therefore, the degree of functionalization or The degree of esterification with fatty acids can be determined by the measure of the hydroxyl number for the core molecule hyperbranched before the hydrophobicization reaction, and then of the hydrophobicization reaction.

In addition to the hydrophilic core, the polymer Hyperbranched exhibits hydrophobic end groups. In this context, the concept hydrophobic end groups means that at minus a part of the ends of the polymer chain Hyperbranched exhibits hydrophobic groups. In this context you can assume that because of this you get a surface at least partially hydrophobicized

The hydrophobic concept is known in itself by experts, where groups that are at least in one portion of the ends of the hyperbranched polymers, considered in themselves, they exhibit a solubility in water reduced

According to a particular aspect, the surface is hydrophobicized by groups that are derived from carboxylic acids that they contain at least 6, preferably at least 12 carbon atoms. The carboxylic acids preferably exhibit a maximum of 40, preferably at most 32 carbon atoms, so particularly preferably at most 20 carbon atoms and of very particularly preferably at most 18 atoms of carbon. In this context, the groups can be derived from acids saturated and / or unsaturated fatty. Preferably, the proportion of carboxylic acids with 12 to 18 carbon atoms is at least 30% by weight, particularly preferably at least 50% in weight and very particularly preferably at least 60% by weight, referred to the weight of carboxylic acids used for hydrophobicization

To them belong particularly acids fatty, which are contained in flax seed, soy and / or the taloil. Particularly suitable are fatty acids that contain a small proportion of double bonds, for example acid hexadecenoic acid, particularly palmitoleic acid, and acid octadecenoic acid, particularly oleic acid.

Preferred carboxylic acids have in this context a melting point of at least 35 ° C, preferably at least 40 ° C and particularly preferably at least 60 ° C. Therefore, carboxylic acids are preferably used linear saturated. They belong particularly acidic octanoic acid, decanoic acid, dodecanoic acid, acid tetradecanoic acid, hexadecanoic acid, heptadecanoic acid, acid octadecanoic acid, eicosanoic acid, docosanoic acid and acid tetracosanoic Saturated fatty acids are particularly preferred  with 16 to 22 carbon atoms, particularly preferably 16 at 18 carbon atoms.

The hyperbranched carrier polymer (after hydrophobicization) exhibits a molecular weight of at least 6000 g / mol, particularly preferably at least 7500 g / mol. Preferably, the molecular weight is at most 30,000 g / mol, particularly preferably at most 25,000 g / mol. This magnitude refers to the weight average molecular weight (Mw) value, which can be determined by gel permeation chromatography, the measurement being made in DMF and using polyethylene glycols as a reference (see among others Burgath et al . In Macromol. Chem. Phys. , 201 (2000) 782-791). In this case a calibration curve is used, which has been obtained by using polystyrene standards. This magnitude therefore represents an apparent measurement value.

The polydispersity Mw / Mn of polymers preferred hyperbranched is preferably comprised in the range from 1.01 to 6.0, particularly preferably in the range from 1.10 to 5.0 and very particularly preferred in the range of 1.2 to 3.0, the average value can also be obtained Numerical molecular weight (Mn) per GPC.

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The hydrophilic core weight ratio to hydrophobic end groups may preferably be comprised in the range of 10: 1 to 1:10, particularly preferably 1: 1 to 1: 2.5. This relationship is obtained from the average value weighted hydrophilic core and the weighted average value of the hyperbranched polymer

The viscosity of the hyperbranched polymer is preferably in the range of 50 mPas to 5.00 Pas, particularly preferably in the range of 70 mPas to 3.00 Pas, this magnitude can be determined by viscosimetry rotary at 110 ° C and 30 s -1 between two 20 mm plates.

The acid number of the hyperbranched polymer it is preferably in the range of 0 to 20 mg KOH / g, particularly preferably in the range of 1 to 15 mg KOH / g and very particularly preferably in the range 6 to 10 mg KOH / g. This property can be measured by titration with NaOH (see DIN 53402).

Additionally, the hyperbranched polymer exhibits after hydrophobicization a hydroxyl number in the range of 0 to 200 mg KOH / g, preferably in the range of 1 to 150 mg KOH / g and very particularly preferred in the range of 10 to 140 mg KOH / g. This property is measured according to ASTM E222. In this context, the polymer is made react with a defined amount of acetic anhydride. He Unprocessed acetic anhydride is hydrolyzed with water. TO The mixture is then titrated with NaOH. The hydroxyl number is obtained from the difference between a comparison sample and the value found for the polymer.

In this case it should be taken into account that the number of acidic groups of the polymer. This can be obtained by acid number, which can be determined by the process described previously.

c) The degree of branching of the hyperbranched polymer is in the range of 20 to 70%, preferably 25 to 60%. The degree of branching depends on the components used for the production of the polymer, particularly the hydrophilic core, as well as the reaction conditions. The degree of branching can be determined according to Frey et al ., This process being described in D. Hölter, A. Burgath, H. Frey, Acta Polymer, 1997, 48, 30 und H. Magnusson, E. Malmström, A. Hult, M Joansson, Polymer 2002, 43, 301.

The hyperbranched polymer exhibits a melting temperature of at least 30 ° C, particularly preferably at least 35 ° C and very particularly preferably at least 40 ° C. According to a particular aspect of the present invention, the melting point of the hyperbranched polymer can be preferably at most 65 ° C, particularly preferably at most 60 ° C, especially preferably as maximum 57 ° C and very especially preferably at most 55 ° C. The melting temperature can be determined by calorimetry Differential Scan (DSC), p. ex. with the Mettler DSC 27 HP and with a heating rate of 10ºC / min.

The water solubility of the polymer hyperbranched after hydrophobicization is preferably at most 10% by weight, particularly preferably as maximum 7% by weight and very particularly preferably as maximum 5% by weight, measured according to the flask method indicated previously at 40 ° C.

Additionally, hyperbranched polymers particularly preferred exhibit in the case of mixing with water at a temperature of 60 ° C or lower, preferably 50 ° C or lower and particularly preferably approx. 48ºC exclusively liquid-liquid equilibria, but not in no case exhibit solid-liquid equilibria or solid-liquid-liquid equilibria, where a mixture is used to determine this property 50% by weight of water and 50% by weight of the hyperbranched polymer. The measurement can be performed by filtration experiments, the mixture is filtered through a pore size filter appropriate, which is preferably 20 µm or less. In presence of solid-liquid equilibria or equilibria solid-liquid-liquid, remain the solid components of the balances lagged in the filter, while in the case of balances liquid-liquid no residue is observed. This property can be controlled among other things by the degree of functionalization and by the carboxylic acids used for the hydrophobicization In case the hyperbranched polymers have a small degree of functionalization and / or carboxylic acids Short chain, these polymers present in the conditions employees indicated above as a general rule exclusively liquid-liquid equilibrium, but do not present solid-liquid equilibrium

Preferably, the hyperbranched polymer It consists essentially of hydrogen, oxygen and carbon. He concept essentially means that others are contained elements up to 10% by weight maximum, particularly preferably a maximum of 5% by weight in the polymer hyperbranched

According to a particular aspect of the present invention, the hyperbranched polymer can be degraded enzymatically This can be achieved for example in such a way that the hydrophilic core and / or hydrophobic envelope comprise ester groups enzymatically degradable organic.

Hyperbranched polymers or preparations Preferred according to the present invention exhibit degradation enzymatic after 3 days or less, preferably two days or so less and particularly preferably a day or less. In In this context, the preparations are degraded with an appropriate enzyme, particularly a lipase, for example Lipomod 34P (Biocatalyst Lmt., United Kingdom), measuring the time until it has been released 50% by weight of the active substance. For example, they can be studied prepared with a load grade of 10 to 20% by weight, where preferably 0.22 g can be suspended with particles of polymer loaded with the active substance in 15 ml of buffer phosphate (pH 5.01) or in 15 ml of Lipomod 34P enzyme solution (Biocatalyst Lmt., United Kingdom) in the same buffer (the concentration of Lipomod 34P was 0.5 mg / ml). The samples may be contained in a 37 ° C water bath without mixing. In intervals of regular time, for example 5 hours, samples can be taken of approx. 2 ml, the concentration of the principle can be analyzed active with appropriate processes, for example HPLC (Chromatography High Pressure Liquid). In this context, the release of a comparison sample, which does not contain enzyme some, in order to exclude stability problems at storage under the chosen measurement conditions, thereby obtains the value indicated above by the difference between the Sample measure and comparison sample.

The production of these polymers Hyperbranched is particularly exposed in EP 630 389. As a rule In general, an initiating molecule can be reacted with at at least one compound containing at least two hydroxyl groups and at less a carboxylic acid group. With this you get a core hydrophilic, which can be reacted with at least one compound hydrophobic, for example a long chain carboxylic acid.

Usually the reaction is performed at a temperature in the range of 0 ° C to 300 ° C, preferably 100 ° C to 250 ° C, the reaction can be accelerated by known esterification catalysts. To these catalysts they belong for example Lewis and Brönstedt acids, particularly p-toluenesulfonic acid, acid methanesulfonic acid, trifluoroacetic acid, BF 3, AlCl 3 and SnCl 4; titanium compounds, particularly titanate of tetrabutyl; zinc powder and / or tin powder.

Preferably, the water released during the esterification is separated from the reaction mixture.

In addition to a hyperbranched polymer, the preparations corresponding to the invention contain at least one low molecular weight substance. In this case, the weight substance low molecular is preferably not combined covalent with the hyperbranched polymer. This can be done by example by ionic or polar interactions or by forces of Van-der-Waals.

Due to polymer interaction hyperbranched and low molecular weight substance can differentiate the preparation of the present invention from a mixture Conventional of these components.

This interaction can be determined in a way known. Depending on the low molecular weight substance, they are Many spectroscopic methods are appropriate for this. For example partial changes in the infrared spectrum can be observed.

Additionally, the corresponding preparations to the invention they can display against a conventional mixture a delayed release of the low molecular weight substance in a medium, which is different from the low molecular weight substance of the prepared. Delayed release can be measured according to the process described by Smirnova, I .; Suttiruengwong, S .; Arlt, W. "Feasibility study of hydrophilic and hydrophobic silica aerogels as drug delivery systems "; Journal of Non-Crystalline Solids (2004) 54-60.

As a rule the time difference for obtain an identical concentration of the molecular weight substance low in the medium in which the molecular weight substance is released low, it is at least 1 minute, preferably at least 5 minutes. In this context, said time difference refers to the measure of a preparation of the present invention and the measurement of a mixture conventional of these components under identical conditions of a delayed release Delayed Release means that conditions are not selected in such a way that the preparation releases the low molecular weight substance as quickly as possible. These conditions are familiar to experts by knowledge of this request. The values of the conventional mixture can also determined by separate addition of the components.

According to a particular embodiment, the prepared is encapsulated, being known by experts the concept "encapsulation". In the prepared encapsulated, the low molecular weight substance may be included for example in a sheath comprising the polymer hyperbranched This can be done for example by a matrix encapsulation and / or encapsulation core-sheath.

According to a particular aspect of the present invention, the preparation of the present invention may be present in the form of particles. In this context, these particles preferably exhibit a size in the range of 1 at 1000 µm, particularly preferably 10 to 500 \ mum.

The shape of the particles is not critical in itself. same, however, the particles may preferably have a spherical shape

The spherical concept means in the context of the present invention that the particles preferably have a appearance in the form of small balls, it being evident to experts that, Due to the production methods, they may also be contained particles with another shape, or that the shape of the particles can deviate from the ideal ball shape.

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Therefore, the spherical concept means that the ratio of the maximum dimension of the particles to the minimum dimension is a maximum of 4, preferably a maximum of 2, measuring these dimensions in all cases through the center of particle gravity. Preferably, at least 70%, of particularly preferably at least 90%, based on the number of particles are spherical.

The particle size can be determined by generally known methods. In this case they can be used by example microscopic images, which can be evaluated visually and / or With the help of computers.

Additionally, preferred microparticles exhibit a particle size distribution particularly narrow. Thus, preferably at least 80% by weight of the particles fall within a range of sizes of 200 µm maximum, preferably 100 µm maximum, and of particularly preferred mode 50 µm maximum.

According to a particular aspect of the present invention, preferably 90% of the particles have a size  in the range of 1 to 1000 µm, so particularly preferred 3 to 800 µm, especially preferably 7 to 700 µm and very especially preferably 10 to 500 µm.

The preparations of the present invention can present extraordinary shear stability, which in Many cases can be influenced by the choice of polymer hyperbranched and process conditions during production of the preparations. Preferably, the preparations exhibit a shear stability of 1 minute or more, preferably 5 minutes or more, determining this stability by a load that corresponds to a 15,000 ULTRA-TURRAX agitator revolutions per minute, preferably 20,000 revolutions per minute. In general, a dispersion occurs in this case, for example in a Pharmaöl (Paraffin Oil WINOG 100 Pharma from Univar GmbH), where the dispersion may contain, for example, 10% by weight of the preparation The particles are tested before and after stability measure, which can be investigated for example with a ULTRA-TURRAX stirrer at 15,000 revolutions per minute, preferably 20,000 revolutions per minute, microscopically, evaluating the shape, size and distribution of the particles. Shear stability is assigned in the conditions mentioned above in case they cannot essentially alterations of any kind are observed.

The storage stability of preparations corresponding to the invention is in many cases also surprisingly high, depending on the class and composition of the medium, in case the preparations are stored in the form of dispersions or emulsions, and / or the temperatures of storage. Under the preferred storage conditions, Preferred preparations may be stored for a period of long time, for example 10 days or more, preferably 30 days or more and particularly preferably 90 days or more. This magnitude can be measured by the release of the active substance in a medium or degradation of the low molecular weight substance. In In this context, these data refer to the period of time up to that a maximum of 10% of the weight substance has been released low molecular in a medium, in which prepared can be stored the preparation, or the time until it has degraded as maximum 10% of the low molecular weight substance, for example by oxidation.

Low molecular weight substance exhibits preferably a molecular weight in the range of 15 g / mol to 1000 g / mol, particularly preferably 30 g / mol to 800 g / mol, and very particularly preferably 60 g / mol at 500 g / mol

The low molecular weight substance can be selected within a wide range. They belong to it particularly compounds containing a peroxide group, amino acids, catalysts, dyes and / or pigments, vitamins, monomers, flavorings and / or flavorings, components biologically active, particularly a medication, initiators, persulfates, silicones, surfactants, silicas, silanes, enzymes and coenzymes, solvents, fillers, crosslinkers reagents, detergents, hair dyes, additives for concrete or plant extracts.

Surprisingly, the preparations of the present invention make it possible for chemical compounds particularly labile, for example initiators and / or persulfates can be stored and be transported in safe conditions, being the conditions of storage and transport essentially less demanding than those of solutions or powders of these substances. This way you can significantly reduce the risk of explosions or inflammation.

To biologically active components particularly preferred peptides, vitamins and precursors of vitamins, fats and fatty acids, amino acids and amino acid precursors, for example creatine, sugars and derivatives of sugars, nucleotides, nucleic acids as well as precursors and derivatives thereof, for example DNA oligomers and RNA.

To vitamins belong particularly Vitamin A, B vitamins, for example vitamin B1, vitamin B2, vitamin B3 (folic acid) and vitamin B12, vitamin C (ascorbic acid), complex D vitamins, particularly 7-dehydrocholesterol, lumisterol, calciferol, ergocalciferol, cholecalciferol, 22,23-dihydroergocalciferol and sitocalciferol, vitamin E (tocopherol) and vitamin K (phylloquinone, menaquinone).

To the preferred amino acids belong particularly DL-methionine, L-lysine, L-threonine, L-tryptophan and L-leucine.

Additionally, the corresponding preparations to the invention may contain as a molecular weight substance under particularly flavoring agents, flavoring agents, natural extracts, flavor enhancing compounds, identical to natural flavorings, as well as additives food modified with enzymes.

Perfumes belong in particular ketones, aldehydes, sulfur-containing compounds, esters of carboxylic acids, alcohols and / or natural extracts.

To ketones to be used preferably belong, for example, acetone, acetophenone, 2,6-dimethyl-4-heptanone,  3-decen-2-one, methyl ethyl ketone, methyl ethyl ketone, methyl heptyl ketone, methylnonyl ketone, 4-methyl-2-pentanone,  methylpropyl ketone, 1-methyl-4-isopropenyl-6-cyclohexen-2-one (D, L-carvone) and / or propiophenone.

To the aldehydes to be used preferably Particularly acetaldehyde, butyraldehyde, aldehyde belong cinnamic, decanal, dodecanal, heptanal, hexanal, isobutyraldehyde, E-2-Decennial, E-2-dodecanal, E-2-hexanal, E-2-nonenal, E-2-octenal, 2,4-decadienal, 2,4-dodecadienal, 2,4-heptadienal, 2,4-nonadienal and / or 2,4-octadienal.

To sulfur-containing compounds to be used preferably they belong among other sulfides, such as dimethyl disulfide, dimethyl trisulfide, disulfide diphenyl, dipropyl disulfide, dipropyl trisulfide, sulfide of ethylmethyl, isopropyl disulfide, methylpropyl disulfide, methylpropyl trisulfide, methyl 2-thiophuroate, 4-methylthio-2-butanone, 3-methylthio-1-hexyl acetate, Y 4- (methylthio) 4-methyl-2-pentanone;

thiocarboxylic acids and acid derivatives thiocarboxylic, particularly thioesters, such as 3- (methylthio) ethyl butyrate, ethyl thioacetate, 3- (methylthio) methyl propionate, methyl thiobenzoate, methyl thiobutyrate, methyl thiohexanoate, methyl thio-isovalerate, and thioacetate n-propyl;

mercaptans, particularly hexylmercaptan, isoamilmercaptan, isobutylmercaptan and / or

thioketones, for example thiomentone.

To the esters of carboxylic acids to be used preferably belong among others amyl acetate, acetate isoamyl, ethyl acetate, ethyl p-anisate, ethyl formate, ethyl hexanoate, ethyl octanoate, esters of butyric acid, n-hexyl acetate, crotonate of n-hexyl, hexyl isovalerate, butyrate isoamyl, isoamyl hexanoate, isobutyl butyrate, propionate of isobutyl, methyl benzoate, acetate 2-methylbutyl, methyl cinnamate, decanoate methyl, methyl isovalerate, methyl octanoate, propionate methyl, neryl acetate, neryl isobutyrate, acetate n-octyl, phenethyl acetate, isobutyrate phenethyl, phenethyl isovalerate, phenethyl propionate, acetate phenylpropyl, phenylpropyl hexanoate, acetate n-propyl, n-propyl formate, and / or n-propyl isobutyrate.

To the alcohols to be used preferably they belong in particular anisic alcohol, benzyl alcohol, 1-butanol, 1-hexanol, alcohol isoamyl, isobutyl alcohol, nerol, ethanol, phenethyl alcohol, Propanol, 2-heptanol, 2-octanol, 3-octanol, 2-nonanol and / or 3-hexanol

To natural extracts belong particularly banana extracts, strawberry extracts, extracts of cocoa, vanilla extracts, coffee extracts, extracts of tea, nut extracts, rum extracts, fruit extracts Citrus, almond extracts, apple extracts and extracts of spices These extracts can be obtained in many cases commercially They belong particularly Cocoa Absolute 14620, Cocoa LC 10167, Cocoa P 11197, Cocoa U88; all of which They can be obtained from Degussa AG. Natural extracts are in this context extracts that can be obtained from natural sources or that exhibit properties that are analogous to these extracts.

According to an additional aspect of the present invention, natural extracts can be used as the substance of low molecular weight Natural extracts are extracts that are They get from natural materials. To the extracts preferred natural belong compositions that are obtained by extraction of pineapple, apple, banana, beer, pear, strawberry, fruits citrus, raspberry, currant, coffee, coffee essence, cherry, mango,  orange essence, passion fruit, rum, cherry, endrin, and / or pure whiskey malt

In addition, the preparations corresponding to the invention may contain natural and synthetic additives, such as food additives, particularly 2-acetyl-3,5 (6) -dimethyl-pyrazine, 2-acetyl-pyrazine, 2-acetyl-thiazole, 2,3-diethyl-5-methyl-pyrazine, 2,3-diethyl-pyrazine, 2,3-dimethyl-pyrazine, 2,5-dimethyl-pyrazine, 2,6-dimethyl-pyrazine, 2-ethyl-3,5-dimethyl-pyrazine, 2-ethylfuran, 2-ethyl-3-methyl-pyrazine, 2-ethyl-5 (6) -methyl-pyrazine, 3-ethylpyridine, 2-methoxy-3-isobutyl-pyrazine, 2-methoxy-3 (5), (6) -methyl-pyrazine, 2-methoxy-pyrazine, 2-methyl-pyrazine, 2-pentilfuran, 2,3,5-trimethyl-pyrazine and / or the Compound 1036 (a known cognac essence substitute usually).

Additionally, the corresponding preparations to the invention may contain dietary additives modified with enzymes (Enzyme Modified Diary Ingredients; EMDI). These additives can be obtained for a multiplicity of foods, for example as cheese flavorings under the trade designation CPF® Cheese Paste Flavors, NCF® Powder Cheese Flavors, BCF® Liquid Blue Cheese Flavors, FDF® Liquid. Cheese Flavors Additionally they are EMDI available as butter flavored materials, for example LBO® Butterfat / Cremepaste Flavors; NBF® Powdered Butterfat Flavors; FDF® / DMF® Liquid Butter Flavors. To the compounds preferred with a peroxide group belong particularly H 2 O 2, persulfates and / or organic peroxides.

To monomers belong particularly olefins, for example 1-butene, 1-hexene, norbornene;

vinyl halides, such as chloride vinyl, vinyl fluoride, vinylidene chloride and fluoride vinylidene;

vinyl esters, such as vinyl acetate;

styrene, styrenes substituted with a alkyl substituent on the side chain, such as p. ex. α-methylstyrene and ? -ethylstyrene, styrenes substituted with a alkyl substituent on the ring, such as vinyltoluene and p-methylstyrene, halogenated styrenes, as per example monochlorostyrenes, dichlorostyrenes, tribromo styrenes and tetrabromo styrenes;

heterocyclic vinyl compounds, such as 2-vinylpyridine, 3-vinylpyridine, 2-methyl-5-vinylpyridine, 3-ethyl-4-vinylpyridine, 2,3-dimethyl-5-vinylpyridine, vinylpyrimidine, vinylpiperidine, 9-vinylcarbazole, 3-vinylcarbazole, 4-vinylcarbazole, 1-vinylimidazole, 2-methyl-1-vinylimidazole, N-vinyl pyrrolidone, 2-vinyl pyrrolidone, N-vinyl pyrrolidine, 3-vinyl pyrrolidine, N-vinylcaprolactam, N-vinylbutyrolactam, vinyl oxolane, vinyl furan, Vinylthiophene, Vinylthiolane, Vinylthiazole and Hydrogenated Vinylthiazole, Vinylxazole and Hydrogenated Vinylxazole; vinyl- and isoprenyl ethers; maleic acid and maleic acid derivatives, such as mono- and diesters of maleic acid, maleic anhydride, anhydride methylmaleic, maleimide, methylmaleimide; fumaric acid and derivatives of fumaric acid, such as mono- and diesters of acid fumaric;

dienes, such as divinylbenzene;

as well as acrylates and methacrylates, which hereinafter referred to as (meth) acrylates.

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These include for example

(met) acrylates, which are derived from saturated alcohols, such as methyl (meth) acrylate, (meth) ethyl acrylate, (meth) acrylate n-propyl, (meth) isopropyl acrylate, (meth) n-butyl acrylate, (meth) tert-butyl acrylate, (meth) pentyl acrylate, (meth) hexyl acrylate, 2-ethylhexyl (meth) acrylate, (meth) heptyl acrylate, (meth) acrylate 2-tert-butylethyl, (meth) octyl acrylate, (meth) acrylate 3-iso-propylheptyl, (meth) nonyl acrylate, (meth) decyl acrylate, (meth) undecyl acrylate, (meth) acrylate 5-methylundecyl, (meth) dodecyl acrylate, 2-methyldodecyl (meth) acrylate, (meth) tridecyl acrylate, (meth) acrylate 5-methyltridecyl, (meth) acrylate tetradecyl, (meth) pentadecyl acrylate, (meth) hexadecyl acrylate, (meth) acrylate 2-methylhexadecyl, (meth) acrylate heptadecyl, (meth) acrylate 5-iso-propylheptadecyl, (met) acrylate of 4-tert-butyloctadecyl, (meth) 5-ethyl octadecyl acrylate, (met) acrylate of 3-iso-propyloctadecyl, (meth) octadecyl acrylate, (meth) acrylate nonadecyl, (meth) eicosyl acrylate, (meth) acrylate of cetileicosyl, (meth) stearylenyl acrylate, (meth) docosyl acrylate and / or (meth) acrylate eicosiltetratriacontil;

(meth) cycloalkyl acrylates, such as (meth) cyclopentyl acrylate, (meth) acrylate 3-vinylcyclohexyl, (meth) acrylate cyclohexyl, (meth) bornyl acrylate;

(met) acrylates that are derived from unsaturated alcohols, such as (meth) acrylate 2-propynyl, (meth) allyl acrylate, (meth) vinyl acrylate and / or (meth) acrylate oil

(meth) aryl acrylates, such as methacrylate of benzyl or phenyl methacrylate, where aryl moieties can be in each case unsubstituted or contain up to 4 substituents;

methacrylates of halogenated alcohols, such as 2,3-dibromopropyl methacrylate,

methacrylate 4-bromophenyl,

(met) acrylate of 1,3-dichloro-2-propyl,

2-bromoethyl methacrylate,

2-iodoethyl methacrylate,

chloromethyl methacrylate.

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Additionally, preferred low molecular weight substances in the range of detergents and additives can be used, which are used in agents for washing hair and hair dyes, for example acetaminophen, acetylated lanolin alcohol, Achillea Millefolium, Aesculus Hippocastanum, Agave Rigida, Aloe Barbadensis , alumina, aluminum hydrochloride, aluminum formate, aluminum hydroxide, magnesium hydroxide, stearates, particularly aluminum stearate and magnesium stearate, aluminum silicate, aluminum triestearate, aminomethylpropanol, ammonia, ammonium bicarbonate, ammonium sulfate , ammonium thioglycolate, ammonium thiolactate, amodimethicone, Anthemis nobilis and Arachis hypogaea .

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To the preferred catalysts belong particularly catalysts containing metals that are used in hydrogenation or hydrogenation (sic), for example for hardening of fatty acids, hydrogenation of nitriles and polyols, hydrogenation of resins, aromatic compounds and oils whites; selective hydrogenation of acetylenes and dienes, as well as selective hydrogenation of AMS to cumene.

Additionally, catalysts belong to them which are used for oxidation, for example for oxidation selective in order to produce ethylene oxide and acetate monomers vinyl purification of waste gases from processes, by example for the elimination of CO and VOCs; gas purification residuals containing halogenated hydrocarbons; as well as the catalysts for the purification of industrial gases.

These catalysts generally contain metals, for example nickel, cobalt, copper, molybdenum, chromium, iron, as well as platinum group metals, for example rhodium, palladium and platinum Catalysts of this type are known per se. themselves and can be obtained commercially in many cases. To them particularly belong products under the commercial designation catASium® as well as cataXium®, from Degussa.

Examples of these catalysts are among others

(-) - 2,3-bis [(2R, 5R) -2,5-dimethylphospholanyl] maleic anhydride- (1,5-cyclooctadien) rhodium (I) -tetrafluoroborate
(catASium® M (R) Rh);

(-) - 2,3-bis [(2R, 5% (sic)) - 2,5-dimethylphospholanyl] acid maleic-N-methylimide- (1,5-cyclooctadien-rhodium (I) -tetrafluoroborate (catASium® MN (R) Rh);

(+) - 2,3-bis [(2S, 5S) -2,5-dimethylphospholanyl] maleic anhydride- (1,5-cyclooctadien) rhodium (I) -tetra-fluoroborate
(catASium® M (S) Rh);

(+) - 2,3-bis [(2S, 5S) -2,5-dimethylphospholanyl] maleic acid-N-methylimide- (1,5-cyclooctadien-rhodium- (I) -tetrafluoro-
borate (catASium® MN (S) Rh);

(+) - (3R, 4R) -bis (diphenylphosphino) -1-benzylpyrrolidin- (catASium® D (R));

(+) - (3R, 4R) -bis (diphenylphosphino) -1-benzylpyrrolidin- (1,5-cyclooctadien) -rodium (I) tetrafluoroborate (catASium® D (R) Rh);

butildi-1-adamantylphosphine (cataCXium® A);

bencildi-1-adamantylphosphine (cataCXium® ABn);

trans-di (mu-acetate) bis [o- (di-o-tolylphosphino) benzyl] dipaladium (II) (cataCXium® C);

N-phenyl-2- (dicyclohexylphosphino) pyrrole (cataCXium® PCy);

N-phenyl-2- (di-t-butylphosphino) pyrrole (cataCXium® PtB);

1- (methoxyphenyl) - (dicyclohexylphosphino) pyrrole (cataCXium® POMeCy);

1- (2,4,6-trimethylphenyl) -2- (dicyclohexylphosphino) imidazole (cataCXium® PICy).

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In relation to the catalysts, the preparations corresponding to the invention make possible a long and stable inalterability of these, as well as manipulation particularly simple Additionally, catalysts can be released over a period of time particularly prolonged in the reaction mixture.

The low molecular weight substances described previously they can be used individually or as a mixture of Two, three or more. In this context, mixtures may contain low molecular weight substances of the same class or classes different. Thus, for example, a combination may comprise as molecular weight substance under a mixture containing a Vitamin and a flavoring agent.

For the production of preparations corresponding to the invention, the Low molecular weight compounds and hyperbranched polymers. Various methods are appropriate for this, particularly coacervation, RESS, GAS and / or PGSS processes, as well as processes that use coaxial nozzles, spray drying, coating in fluidized bed and microencapsulation.

According to preferred processes, a compressed gas is used or at least two liquid phases are formed, both phases containing the low molecular weight substance, and at least one liquid phase containing a hyper-polymer.
Measured

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In the case of the RESS (Rapid Expansion of Supercritical Solution) process, a mixture comprising a supercritical fluid and a substance dissolved therein is suddenly expanded. A more detailed account of this process with additional documentation is presented in Gamse et al ., Chemie Ingenieur Technik 77 (2005), No. 6, pages 669 to 679.

In the case of the GAS process, a gaseous or supercritical precipitation agent is added to a diluted solution of a low molecular weight substance in the presence of hyperbranched polymers. Preferably, this process can also be conducted continuously. These processes have been particularly exposed by Gamse et al ., Chemie Ingenieur Technik 77 (2005), No. 6, pages 669-679 and Tom, JW; Lim, GB; Debendetti, PG; Prod'homme, RK Supercritical Fluid Engineering Science, Washington DC 1993: Brennecke, JF; Kiran, E .; American Chemical Society: 1993.

In the case of the PGSS process, a compressed gas is added to a solution or a melt. The saturated gas mixture is then expanded with a nozzle, forming solid particles. PGSS processes have been described among others by Gamse et al ., Chemie Ingenieur Technik 77 (2005), No. 6, pages 669 to 679; Pérez de Diego, Y. Production of Controlled Drug Delivery Microparticles using Supercritical CO2, 004 ; and Shariati, A .; Peters, CJ Recent developments in particle design using supercritical fluids. Current Opinion in Solid State & Materials Science 2003 , 7 (4-5), 371-383.

Additionally, the preparation corresponding to the invention can preferably be obtained by the PCA (Precipitation with Compressed Fluid Antisolvent) process, in which a solvent / solid solution is sprayed in a high pressure chamber, and the contact between the phases takes place in the Spray chamber between fine droplets and supercritical fluid, thereby forming fine particles (eg Gamse et al ., Chemie Ingenieur Technik 77 (2005), No. 6, pages 669 to 679).

In addition, the preparations according to the present invention can preferably be produced by the SEDS (Solution Enhanced Dispersion by Supercritical Fluids) process. In the SEDS process, a liquid stream is also obtained, which contains the low molecular weight substance and the hyperbranched polymer. This liquid stream is already placed in the nozzle in contact with the supercritical fluid. By this variant of the process, particularly small particles can be obtained (eg Gamse et al ., Chemie Ingenieur Technik 77 (2005), No. 6, pages 669 to 679).

Additionally, the preparations corresponding to the invention can be obtained or transformed by the CPF process. In the CPF (Concentrated Powder Form) process there is no alteration of the particle size. The objective of this process is to achieve a high concentration of a liquid in a solid. The liquids in this case can be contacted with an appropriate gas, for example CO2 in a static mixer before spraying, or dissolved in very viscous substances, whereby a drastic reduction in viscosity can be achieved. The very fine droplets of liquid produced by means of a nozzle collide with the solid dosed in parallel and adhere to it, whereby agglomerates can be formed, which contain high proportions of liquid. Additionally, the solid may be thoroughly impregnated with this liquid (eg Gamse et al ., Chemie Ingenieur Technik 77 (2005), No. 6, pages 669 to 679).

In the processes described above, which operate with high pressure, particularly the RESS, GAS and / or processes PGSS, the encapsulation can be advantageously performed at temperatures in a range of -20ºC to 250ºC, preferably 0 ° C to 180 ° C and particularly preferably 10 ° C at 150 ° C. The pressure in these processes may vary within a wide range, these high pressure processes can be performed  preferably in a range of 0.5 bar to 400 bar, so particularly preferred 1 bar to 200 bars and very 1 bar to 100 bars particularly preferred.

In the case of high pressure processes, the concentration of the low molecular weight component in the polymer hyperbranched is preferably in the range of 0.5% by weight to 95% by weight, particularly preferably 1% by weight at 80% by weight and very particularly preferably 5% in Weight at 50% by weight.

In the case of coacervation, the particles are formed by precipitation from a polymer solution hyperbranched and low molecular weight substance.

It is generally distinguished between coacervation simple and complex, as well as between aqueous phase separation and organic (R. Arshady, "Microspheres and microcapsules - A survey of manufacturing techniques, Part III: Coacervation ", Polymer Engineering and Science 30 (1990) 905 et seq.). In coacervation A simple colloidal component is used, e.g. jelly, using in complex coacervation two colloidal components loaded with opposite load, e.g. jelly and gum arabic. The principle of Coacervation is based on the fact that p. ex. an aqueous solution of gelatin is transformed by adding ethanol in a biphasic system, which is composed of a phase rich in gelatin (coacervate) and a phase poor in jelly. This is very analogous to a fractionation of polymer, but in this case they are formed, with incorporation of forces shear, microparticles with an average size of 2-5000 micrometers

The production of microcapsules by coacervation It can often be subdivided into three steps: (1) obtaining (from three) non-miscible phases, (2) separation of the colloid as a sheath from the capsule and (3) solidification of the capsule sheath.

The three immiscible phases comprise a medium external, a core material and a sheath material of the capsule. The pod material of the capsule is dissolved in the external medium and the core material is dispersed therein. By incorporation of an external stimulus (temperature, pH, electrolytes) the capsule sheath material becomes insoluble in the external environment and is deposited on the boundary surface to give a dispersed core material. After filtration, the pod of the capsule is finally hardened by heat input, crosslinking or solvent removal, or dried by spray or lyophilization.

Preferably, the coacervation is performed at temperatures in the range of -20 ° C to 150 ° C, so particularly preferably 0 ° C to 100 ° C and very particularly preferably 10 ° C to 90 ° C.

The pressure during which the Coacervation is not subject to any particular limitations. In In many cases, coacervation can be performed at a pressure in the range of 10 mbar to 10 bar, preferably 200 mbar to 5 bar and particularly preferably 500 mbar to 3 bars.

Preferably, the concentration of the component Low molecular weight in the hyperbranched carrier polymer can be in the range of 0.5% by weight to 95% by weight, of particularly preferably 1% by weight to 80% by weight and so very particularly preferred 5% by weight to 50% by weight, without this It should be considered in this case as a limitation.

This process has been described among others by

R. Arshady, "Microspheres and microcapsules - A survey of manufacturing techniques, Part III: Coacervation ", Polymer Engineering and Science 30 (1990) 905 et seq .;

Jain, RA The manufacturing techniques of various drug loaded biodegradable poly (lactide-co-glycolide) (PLGA) devices. Biomaterials 2000 , 21 (23), 2475-2490;

Jung, J .; Perrut, M. Particle design using supercritical fluids: Literature and patent survey. Journal of Supercritical Fluids 2001 , 20 (3), 179-219; Y

Subramaniam, B .; Rajewski, RA; Snavely, K. Pharmaceutical processing with supercritical carbon dioxide. Journal of Pharmaceutical Sciences 1997 , 86 (8), 885-890.

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Spray drying is a process. susceptible of continuous realization for drying of solutions, suspensions or pasty compositions. This process is very known, being able to commercially acquire plants for the completion of the process As a general rule, the material to be dried is incorporates by means of a nozzle (that works by liquid pressure or compressed air or inert gas) or rotary spray discs (4000-50,000 rpm) in a stream of hot air (depending on the temperatures of the device, up to 220º), which dries the same in fractions of 1 second to give a fine powder. The air hot can pass in the same direction of the current of spray or counterclockwise (parallel or countercurrent process), depending on the type of construction or purpose of use. The device of spray is located on top of a tower of spraying, and the dry material that descends separates into its mostly by a cyclone separator of the air stream and You can leave now.

Under microencapsulation the inclusion is understood of at least one substance (active substance) with the help of at least a second (sheath material). In many cases, the first one does not It can be used directly for different reasons (solubility, reactivity, stability, etc.), or actions must be taken determined by microencapsulation (eg release curves for controlled release, protection features individual, etc.).

In practice there are a number of approaches for microencapsulation, which essentially end in two methods, namely, matrix encapsulation and encapsulation core-sheath.

For both methods solutions can be obtained commercial. For this, formulations and processes individually adapted to the active ingredients. A Commercial supplier of these solutions is BRACE GmbH, Alzenau

According to a preferred aspect of the present invention, the preparations corresponding to the invention can Obtained through a process that includes the following steps:

preparation of a polymer melt that comprises at least one hyperbranched polymer and at least one low molecular weight substance,

introduction of polymer melt in a second liquid phase, in which the hyperbranched polymer is hardly soluble, the second liquid phase having a solidification temperature that is lower than the temperature of solidification of the hyperbranched polymer,

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dispersion of the polymer melt in the second liquid phase at a temperature that is greater than or equal to the solidification temperature of the hyperbranched polymer, and

solidification of polymer melt dispersed in the second liquid phase.

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According to the preferred process, a polymer melt is produced. The term "polymer melt" designates a state capable of flowing from a composition, comprising at least one hyperbranched polymer and at least one substance of low molecular weight. Preferably, the viscosity of the polymer melt is in the range of 50 mPa * s to 5000 Pa * s, particularly preferably in the range of 100 mPa * s to 1000 Pa * s, this magnitude can be determined by rotational viscosimetry. The state susceptible to flow depends in this case, among other things, on the temperature. Preferably, the above-mentioned polymer melt viscosity ranges are measured at a temperature in the range of 10 to 200 ° C, particularly preferably in the range of 50 to 150 ° C. According to a particular aspect of the present invention, the melt viscosity of the polymer can be in the range of 100 mPa * s to 1000 Pa * s, this magnitude can be measured by rotational viscosimetry at 110 ° C and 30 s -1 between two plates
20 mm

The low molecular weight substance is preferably distributed finely in the polymer melt.  Known devices can be used for this purpose, as per example stirring devices, comprising a boiler of agitation with propeller stirrers, discs, toothed discs, anchor, spiral, vane, blade, vane oblique, cross vane, screw, MIG, INTERMIG, ULTRA-TURRAX, worm, belt, finger, basket, impeller, as well as dispersers and homogenizers, that can work among other things with ultrasound. The devices can generally display at least one axis, in which can be mounted in turn preferably 1 to 5 stirring elements.

In this way, for example, a solution, a suspension or a dispersion, being able to reach as maximum particle size of the dispersed phase present preferably 5,000 µm, particularly preferably maximum 1000 µm, in case the weight substance Low molecular is in the form of particles.

The parameters necessary for this depend on the devices described above. Preferably, the stirring speed may be in the range of 10 at 25,000 revolutions per minute, particularly preferable in the range of 20 to 10,000 revolutions per minute.

The temperature at which the mass is produced polymer melt, it can also be comprised within a wide interval, this one depending among other things on the solidification temperature of the hyperbranched polymer. Preferably, the temperature is in the range of -20 ° C to 250 ° C, particularly preferably in the range from 0 ° C to 200 ° C. According to a particular aspect of the present invention, the temperature during the production of the melt polymer is selected from 10 ° C to 200 ° C, so particularly preferred in the range of 15 ° C to 150 ° C by above polymer solidification temperature hyperbranched The pressure used during the production of the Polymer melt is not critical either, depending on this in said cases of the low molecular weight substance class and of the solidification temperature of the hyperbranched polymer. By For example, the pressure can be selected within the range of 0.1 mbars to 200 bar, preferably in the range of 10 mbars to 100 bars

According to a particular aspect of the present invention, preferably not added to the polymer melt  any solvent, particularly no organic solvent, does not particularly preferably containing the melts of any solvent polymer. As organic solvent is understood in this context a substance, in which the polymer is soluble hyperbranched, and that has to be separated during the process of production, since this compound should not be contained in prepared In this context, it should be understood that many of the low molecular weight substances discussed above may have solvent properties. However, these substances are a desired component of the preparations, so that these compounds do not represent any solvent within the framework of the present invention. Therefore, the use of solvents is not necessary for the realization of the process. On the other hand, some substances low molecular weight are supplied in dissolved form, not being critics in general the solvents used in this case for the use of the low molecular weight substance, so that these they are for example harmless from a health point of view, in if the low molecular weight substance is biologically active Adjuvants of this type do not have to be separated necessarily before the melt production of polymer. In many cases these adjuvant substances can incorporated into the polymer melt.

The polymer melt described previously, according to the invention, a second phase is conducted liquid, in which the hyperbranched polymer is hardly soluble and having a solidification temperature lower than the solidification temperature of the hyperbranched polymer.

The "hardly soluble" concept means that the solubility of the hyperbranched polymer in the Second liquid phase should be as small as possible. The Solubility is in many cases temperature dependent. By consequently, the dispersion conditions can be selected in many cases in such a way that a proportion as small as possible of the hyperbranched polymer dissolves in the second liquid phase. Preferably, the hyperbranched polymer has a solubility. at the dispersion temperature according to the 20% flask method in maximum weight, preferably 10% maximum weight in the Second liquid phase

The second liquid phase has a temperature of solidification below the solidification temperature of the hyperbranched polymer As a rule, this temperature is deduces from the melting temperature or the temperature of glass transition of the main constituent of the second phase liquid, with decreases in the point of solidification by means of adjuvants or additives, or by use of mixtures of materials. This magnitude can be obtained from DSC measures, mentioning the melting points or points of solidification of the main usual constituents of the Second liquid phase in consultation works.

Preferably, the second liquid phase It comprises harmless substances from the sanitary point of view, which particularly display an approval according to the Community Food Additives Registry according to the Regulation (EC) No. 1831/2003, Rev. 4 Status: published on 29 May 2006 (FDA).

In the case of the use of polymers hydrophobic hyperbranched, is used in the second liquid phase preferably at least one hydrophilic substance as constituent principal. To hydrophilic substances, which may be contained as the main constituent in the second liquid phase, they belong particularly water and alcohols with 1 to 7, preferably 1 to 4 carbon atoms, particularly methanol, ethanol, propanol and / or butanol

The second liquid phase may also contain of the main constituent additional adjuvants, particularly dispersants and stabilizers. These adjuvants are known for the experts, counteracting the dispersants an aggregation of the particles. To them belong particularly emulsifiers, protective colloids and surfactants, which can be used in each case depending on the hyperbranched polymers employees, the low molecular weight substance and the constituent main of the second liquid phase. To the surfactants particularly preferred surfactants belong anionics, such as lauryl ether sulfate, cationic surfactants and non-ionic surfactants, such as polyvinyl alcohols and ethoxylated fatty alcohols. Stabilizers can be used for a multiplicity of applications, obtaining or stabilizing these adjuvants get An unstable desired state. They belong in particular sedimentation impediment agents, such as pectins and / or carrageenan

Preferably, the second liquid phase comprises 60 to 100% by weight of the main constituent, for example  the hydrophilic substances discussed above, such as water or alcohols with up to 4 carbon atoms. Additionally, the second Liquid phase may contain 0 to 40% by weight of substances adjuvants, particularly 0 to 20% by weight of emulsifiers and 0 to 20% stabilizers.

The polymer melt incorporated in the second liquid phase disperses at a temperature that is higher or same as polymer solidification temperature hyperbranched

The polymer solidification temperature Hyperbranched designates within the framework of the present invention the temperature at which the hyperbranched polymer solidifies, of such that polymer particles no longer agglomerate to this temperature without external influences to form agglomerates more thick. Depending on the constitution and properties of crystallization, solidification temperature may be given for example by the glass transition temperature or the temperature of fusion of the hyperbranched polymer, which can be determined by example by the DSC process (Differential Scanning Calorimetry; Dynamic Differential Calorimetry).

In this case, it should be taken into account that partially crystalline polymers can exhibit not only a glass transition temperature but also a temperature of fusion, in this case the temperature at which the particles do not exhibit any agglomeration. In case the surface is essentially crystalline, then it is decisive in In many cases the melting point of these constituents.

In this context, dispersion means that the polymer melt comprising at least one substance of Low molecular weight is finely distributed in the second phase liquid continues. The dispersion can be carried out in this case with known devices and devices, such as devices stirring, comprising a stirring boiler with stirrers of propeller, of discs, of toothed discs, of anchor, of spiral, of blades, blades, oblique blades, cross-blades, screw, MIG, INTERMIG, ULTRA-TURRAX, screw endless, tape, finger, basket, impeller, as well as dispersers and homogenizers, which can operate among other things With ultrasound The devices may contain as a rule at least one axis, on which they can be mounted in turn preferably 1 to 5 stirring elements.

The duration and energy contribution of the dispersant depend in this context on particle size and the distribution of desired particle sizes. Therefore, the duration of the dispersant can be selected within a wide range Preferably, the dispersion is carried out during a period of time in the range of 1 second to 5 hours, particularly preferably in the range of 10 seconds to 2 hours

According to an additional aspect, the melt of polymer may preferably comprise 10 to 99.99% by weight, of particularly preferred mode 50 to 99.00% by weight and very particularly preferred 70 to 90% by weight polymer hyperbranched Additionally, the polymer melt can preferably comprise 0.01% by weight to 90% by weight, preferably 1% by weight to 50% by weight and very particularly preferred 10% by weight to 30% by weight of substance of low molecular weight

According to a particular aspect of the present invention, the Newton Number may be comprised during the dispersion preferably in the range of 0.1 to 1000, so particularly preferred in the range of 0.4 to 800.

Depending on an embodiment Particular of the process corresponding to the invention, the Number of Reynolds during dispersion is preferably comprised in the range of 1 to 10 7, particularly preferably in the range of 10 to 10 6.

The parameters necessary for this depend on the devices described above. Preferably, the stirring speed may be in the range of 10 at 25,000 revolutions per minute, particularly preferably in the range of 20 to 10,000 revolutions per minute.

In this context the Newton Number used or the stirring speed depends on the particle size and the distribution of desired particle sizes. The more energy is contribute and the dispersion time is longer, they can Obtain both smaller particle sizes. A distribution narrow particle sizes can also be obtained by a High dispersion energy and prolonged dispersion time. Moreover, prolonged dispersion times and energies high dispersion are in many cases linked to cuts additional.

The temperature at which the polymer melt is dispersed in the second liquid phase can also be within a wide range, this being dependent among other things on the solidification temperature of the pre-branched polymer. Preferably, the temperature is in the range of -20 ° C to 250 ° C, particularly preferably in the range of 0 to 200 ° C. The pressure employed in the dispersion of the polymer melt is not critical either, this in many cases depending on the type of the low molecular weight substance and the solidification temperature of the hyperbranched polymer. For example, the pressure can be selected in the range of 10 mbar to 200 bar, preferably in the range of 100 mbar to
100 bars

The temperature during dispersion is higher or same as polymer solidification temperature hyperbranched Preferably, the dispersion temperature is between 1 ° C and 200 ° C, particularly preferably 5 ° C to 150 ° C and very particularly preferably 10 to 50 ° C per above polymer solidification temperature hyperbranched

The weight ratio of polymer melt at the second liquid phase it can be comprised within a wide range Preferably, this relationship is comprised in the range from 1: 1 to 1: 1000, particularly preferably 1: 1.5 to 1: 500.

During dispersion, the composition may contain for example 50 to 99% by weight, preferably 70 to 98% in weight of second liquid phase and 1 to 50% by weight, preferably 2 to 30% by weight polymer melt.

Once the polymer melt is dispersed in the second liquid phase, the polymer melt dispersed solidifies. Solidification can take place by known methods, for example by adding salts to a temperature slightly higher than solidification temperature or by cooling. Preferably, the solidification of the dough Polymer melt is produced by cooling the second phase liquid at a temperature below the temperature of solidification of the hyperbranched polymer.

The type of cooling depends among others things of particle size and size distribution of desired particle. Fast cooling can lead between other things to a particle size distribution particularly uniform and small particles, since it can avoid an aggregation. In this case the formation of aggregates is smaller for a large cooling volume.

Additionally, the size distribution of particle and particle size can be influenced by adjuvants, such as dispersants and emulsifiers. These additives can be added for example in the second phase, being able to perform an additivation of the surface of the particles formed. This additivation can also reduce an aggregation of the microparticles during drying or during storage.

Depending on the application, the composition thus obtained can be further transformed immediately, without purification, concentration or separation. According to a particular embodiment, the present process may comprise the step of separating the microparticles formed in the second phase
liquid

The separation can be done by processes known, particularly by filtration, centrifugation, sedimentation, magnetic separation, flotation, sieving or decantation, being able to use the processes individually or in combination. In this case, the compounds of the second liquid phase they can be separated essentially completely, so that get dry microparticles or the particles can concentrate, in which case relatively large quantities are still contained Large compounds of the second liquid phase of the product final. Preferably, the final product may contain at least 80% by weight of microparticles, particularly preferably at minus 95% by weight of microparticles.

The devices that can be used for separation or concentration of the microparticles, denominated in hereinafter also separators, are generally known. So can be used, among others, centrifuges, decanters, centrifugal force separators, filters, for example filters gravity, suction filters (vacuum filters), filters pressure, suction-pressure filters, press filters, filters drum-vacuum, tape filters, disk filters, flat filters, chamber press filters, frame press filters, cartridge filters, leaf filters, membrane filter plates and / or tape presses sieve

The temperature during separation or concentration can also be comprised within a wide interval, depending on this among other things of the solidification temperature of the hyperbranched polymer. Finally to avoid aggregation of the particles, the temperature selected should be below the temperature of solidification of the hyperbranched polymer. Preferably, the temperature is in the range of -20 ° C to 250 ° C, from particularly preferably in the range of -10 ° C to 100 ° C. The pressure used during separation or concentration is not criticism either, depending in many cases on the type of substance of low molecular weight and temperature of solidification of the hyperbranched polymer. For example, the pressure can be selected within the range of 10 mbar to 200 bars, preferably within the range of 100 mbar to 100 pubs.

After separation, the particles obtained can be washed. To this end, the particles can be treated  with a washing liquid, in order to separate from the particles the remains of additives and / or the low molecular weight substance which are found on the surface of the particles. By consequently, the particles, particularly the polymers Hyperbranched should not be soluble in the washing liquid. On the other hand, the substance to be separated, for example the substance of Low molecular weight, should exhibit the greatest solubility possible. Among the preferred hydrophilic washing liquids are particularly find water and / or alcohols with 1 to 7, preferably 1 to 4 carbon atoms, particularly methanol, ethanol, propanol and / or butanol. These liquids can be used also in the form of mixtures of two, three or more liquids.

The temperature during washing can be also within a wide range, depending on this among other things of the polymer solidification temperature hyperbranched In order to avoid aggregation of the particles, the selected temperature should be lower than the temperature of solidification of the hyperbranched polymer. Preferably, the temperature is within the range of -20 ° C to 250 ° C, particularly preferably in the range of -10 ° C to 100 ° C. The pressure used during washing is not critical either, being it is dependent in many cases on the class of the weight substance  Low molecular and polymer solidification temperature hyperbranched For example, the pressure during washing can be selected within the range of 10 mbar to 200 bar, preferably in the range of 100 mbar to 100 bar.

The devices that can be used for Particle washing are known as a rule. So, devices comprising a reservoir can be used for example mixer and a separator. Mixing tanks comprise preferably the apparatus and devices described above for dispersion Additionally, mixing tanks They can be provided with thermoregulation. Therefore, these Mixing tanks may include heating elements or chillers

In a further step, the microparticles obtained can be dried. The devices that can be used For drying the microparticles are generally known. Thus, they can be used among other drum dryers, dryers oscillators, plate dryers, screw dryers, paddle dryers, cylinder dryers, dryers rollers, freeze dryers, fluidized bed dryers, dryers spray, suspension dryers, drying mills, grid dryers, tunnel dryers, vacuum dryers and / or vacuum-contact dryers.

The temperature during drying can be also covered within a wide range, depending this among other things of the solidification temperature of hyperbranched polymer In order to avoid an aggregation of particles, the selected temperature should be lower than solidification temperature of the hyperbranched polymer. Preferably, the temperature during drying is comprised in the range of -20 ° C to 150 ° C, particularly preferable in the range of -10 ° C to 100 ° C. The pressure used during drying it is not critical either, depending on this in many cases of the low molecular weight substance class and the solidification temperature of the hyperbranched polymer. By For example, the pressure can be in the range of 0.1 mbar at 10 bar, preferably in the range of 0.2 mbar to 2 pubs.

The process described above can be done with simple installations, which may be constituted by components known in themselves. Installations appropriate preferably comprise at least two deposits mixers and a separator, where the mixing tanks are linked together by at least one conduction and the second deposit Mixer is attached to the separator. The second phase withdrawn in the separator can be returned again by a recycle line to a mixing tank

According to a preferred embodiment, in the pipe between the first mixing tank, in which polymer melt is produced and the second deposit mixer, in which the polymer melt is dispersed in the second liquid phase, a pump may be provided, which is Suitable for very viscous liquids. Among the preferred pumps are particularly find screw pumps, for example pumps screw with 1, 2 or 3 screws, screw compressors, pumps of vanes, rotating piston pumps, rotary pumps, pumps piston, rotary piston pumps and / or pumps peristaltic

According to a particular aspect of the present invention, the installation preferably contains at least three mixing tanks, where at least two mixing tanks They are connected by pipes with at least one mixing tank. In this case at least one mixing tank is used for production. of the polymer melt, at least one mixing tank for the production of the second liquid phase and at least one deposit mixer for dispersion of the polymer melt in the Second liquid phase The polymer melt and the second phase Liquid can be produced in separate mixing tanks additional charges or continuously, in order to guarantee a continuous production of microparticles.

Preferably, the installation may contain at least one dryer, which is attached to the separator. Additionally, the installation may preferably comprise a device for particle washing.

Solidification of polymer melt in the dispersion it can be realized in the installation by means of various measures For example, it can cool in the tank mixer, in which the dispersion has been prepared. This can be carried out for example by external cooling or by adding liquids that preferably have the same composition or a composition analogous to that of the second liquid phase. Preferably  a heat carrier or heat exchanger, a mixing valve or a mixing tank additional.

The installation may include pumps, which they can serve for example for the transport of liquids or for the obtaining overpressure pressure or subatmospheric pressure. The bombs appropriate depend on the respective purpose. To the bombs Preferred belong for example impending pumps, as per example water lifts, screw conveyors, bellows pumps, piston pumps, rotary piston pumps, gear pumps with external / internal gears, pumps membrane, rotary distributor pumps, centrifugal pumps, peristaltic pumps, timing belt pumps, spindle pumps Eccentric helical, screw pumps and screw compressors, and / or hydraulic ram;

hydraulic pumps, such as pumps centrifuges, axial pumps, diagonal pumps and / or pumps radials;

bubble pumps, water jet pumps, steam jet pumps, shock siphons (hydraulic ram), easel pumps (sounding pumps);

vacuum pumps, such as pumps impellers, pumps with entrainment fluid, molecular pumps, turbomolecular pumps, cryogenic pumps, sorption pumps, and oil diffusion pumps.

Installations of this type are illustrated by way of example in subsequent figures described with greater detail.

Figure 1 describes a first form of realization of an installation for the execution of the process of the present invention

In Figure 1, a first form of realization of an installation for the execution of the process of the present invention This installation can display for example one, two or more 1 or 2 feeds, for example pipes or screws endless feeding, through which the one is fed or more hyperbranched polymers and / or one or more substances of weight low molecular to a first mixing tank 3. In the tank mixer 3, the fed substances can be transformed into a polymer melt, comprising at least one polymer hyperbranched and at least one substance of low molecular weight. In the mixing tank 3 can be finely distributed components in each other. This way it can be produced by example a solution, a dispersion or a suspension. In many cases the hyperbranched polymer forms the matrix phase, in which The low molecular weight substance is distributed. For it the devices described above can be used.

The polymer melt obtained in the mixer tank 3 can be transported for example with a pump 4 going through conduit 5, for example a pipe, to the tank mixer 6.

The mixing tank 6 may have one, two, three, four or more additional pipes 7, 8, 9, 10, for example pipes or feeding conveyor organs, such as screws or pumps, through which they can be added by example stabilizers, emulsifiers, hot water and / or cold water. In the description of the present figure, an example is used Water as the second liquid phase. However, it is evident to the expert that any other compound can also be used described above as the main constituent of the second liquid phase instead of or together with water. Water serves therefore exclusively as an example for the compounds described previously, which can be conveniently replaced by the other substances

Feed pipes 7, 8, 9, 10 all of them can flow into the mixing tank 6. Additionally, these feed lines can meet also before entering the mixing tank 6.

Before feeding the melt of polymer in the mixing tank 6, can be produced for example in pipes 7, 8, and 9 a solution comprising as main constituent for example water or ethanol as well as adjuvants, for example stabilizers and emulsifiers. This solution can be heated to a temperature higher than solidification temperature of the hyperbranched polymer. Additionally, the fed components may already have a convenient temperature.

After the production of a solution corresponding in the mixing tank 6, the melt of polymer produced in mixer tank 3 can be fed to the mixing tank 6. In mixing tank 6, the melt of polymer is dispersed in the solution described above. For the mixer tank 6 has devices for known dispersion. For this, the devices can be used described above.

After they have been obtained by dispersion the size and size distribution of the desired droplets, the polymer melt present dispersed in the second phase liquid, for example water, can solidify. For this you can cold water is introduced, for example, in the mixing tank 6 by a line 10. Additionally, the mixing tank 6 can cooled by means of a cooling fluid, which is passed through middle of a heat conveyor or double wrap.

The particles thus obtained can be separated from The second liquid phase. For this, the composition obtained in the mixer tank 6, which contains the microparticles solidified, it can be conducted for example with a pump 11 a through the pipe 12 to the separator 13. The separator 13 serves to the subsequent separation or concentration of the microparticles contained in the second liquid phase, being able to be used for it any of the devices indicated above. In this case the microparticles of the second are separated in the separator liquid phase, and in many cases a further concentration The second separate liquid phase, which can contain for example water, emulsifiers and stabilizers, can impersonate a recycle line 14, for example a pipe, to the mixing tank 6.

Separated microparticles can be sent to dryer 17 for example with a pump 15 through the concentration of feed 16, for example, a pipe. In dryer 17 the remains of the second liquid phase can be removed, for example Water. Dry microparticles can be removed from the dryer by pipe 18.

Temperatures during charging may be within a wide range. Preferably, the charging is carried out at a temperature in the range of -10º to 150ºC, particularly preferably 0 ° C to 80 ° C.

The preparations corresponding to the invention they may contain a surprisingly high proportion of the low molecular weight substance. According to a particular aspect of the present invention, the weight ratio of hyperbranched polymer The low molecular weight substance may be comprised in the range of 40: 1 to 0.5: 1, particularly preferably in the 20: 1 to 2: 1 range. The degree of load can preferably be in a range of 1% to 99%, so particularly preferred 5% to 90% and very particularly 10 to 30%, given the degree of load by the weight ratio of the substance of low molecular weight to the total weight of the preparation.

Low molecular weight substances can free from the combination corresponding to the invention or the preparation corresponding to the invention in any way desired. For example, an enzymatic degradation can be used to release the substance of low molecular weight. In this way, the release time can be controlled by the rate of degradation.

Additionally, the release can be controlled by a change in the value of pH, temperature, pH, frequency of radiation and type of medium.

The type of medium can be modified for example by the addition of solvents.

As solvents for medium variation can be used among other water, alcohols such as ethanol or isopropanol, compressed CO2, compressed propane, tetrahydrofuran, toluene, acetone, benzoyl peroxide, solutions  aqueous HCl, hexane, acetic acid, ethanediol, dichloromethane, dichloroethane or ionic liquids.

Depending on the degree of functionalization of the hyperbranched polymer and the medium in which the low molecular weight substance, therefore the most diverse solvents, in order to obtain the most release delayed as possible or as quickly as possible. If the release of low molecular weight substances encapsulated in polar means, the release is much slower the more groups OH of the hyperbranched core polyester be esterified / functionalized with fatty acids. This effect can favor by adding suitable solvents.

Additionally, the release of the principle active can be controlled by the thickness of the polymer sheath of support, which surrounds the low molecular weight substance or the active principle, and / or by the degree of functionalization / degree of hydrophobicization or the hydroxyl number of the polymer hyperbranched

The release time is much longer thicker is the support polymer sheath. The thickness of the support polymer sheath can be increased particularly by increase in polymer concentration in the starting mixture (consisting of at least one hyperbranched polymer and a low molecular weight substance). In this context you can have influence the type of encapsulation process on this magnitude, being able to select the expert by simple routine tests the most appropriate process for the desired purpose among the mentioned above.

Surprisingly, it has been found that in the case of hyperbranched support polymers the concentration in the starting mixture (consisting of solvent + polymer of support + low molecular weight substance) can be raised by above the usual concentrations in the prior art of 10% by weight to a polymer concentration of 70% by weight. The Finally desired polymer concentration is decisive, along with temperature control or modification of the pH value or the dissolving power of the solvent in terms of sheath thickness of polymer and therefore as to the time of release.

In addition to the thickness of the polymer sheath of support, degree of functionalization or hydroxyl number They decide as to the time of release. In case the release of the encapsulated low molecular weight substance is perform in polar media, the release is much slower as more OH groups of hyperbranched core polyester are esterified / functionalized with fatty acids.

The preparations of the present invention can Used in numerous applications. For example, the preparations they can be used as hardeners, as crosslinking agents, as catalysts, as defoamers, as dispersants, as additives with antimicrobial or antifungal action, such as additives for increased scratch resistance of surfaces, such as additives in coatings or adhesives, such as fluidity enhancers and / or As s for concrete. Additionally, the preparations can be used in cosmetics, in medicines, in deodorants, in nutrient agents, in feeds, in beverages, in coatings of walls or floors, in joint materials, in gaskets and / or in varnish systems.

According to a particular aspect of the present invention, the preparation preferably comprises only small amounts of creatine, folic acid or tocopherol, if use these materials exclusively as a weight substance low molecular Particularly preferably, the amount of Keratin, folic acid or tocopherol is limited to 10% by weight, of particularly preferably 5% by weight, based on the weight of the prepared, in case the preparation does not contain any substance additional low molecular weight. However, they are preferred preparations containing combinations of creatine, folic acid and / or tocopherol with each other or with low molecular weight substances additional, these preparations may contain more than 10% by weight of creatine, folic acid or tocopherol.

The following illustrates in greater detail the present invention by way of examples, without it Be considered as a limitation.

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Examples Example 1

With use of the installation represented in Figure 1 a preparation corresponding to the invention, comprising DL-methionine and a hyperbranched polyester

The hyperbranched polyester used was obtained by hydrophobicization of a hydrophilic hyperbranched polyester, which it had a weight average molecular weight Mw value of 3500 g / mol, a glass temperature of approximately 35 ° C and a number of hydroxy of about 490 mg KOH / g (commercially available Perstorp® under the designation Boltorn H30®). The Hydrophobicization was performed by esterification of the hydrophilic polymer  with a mixture of eicosanoic acid and behenic acid (ratio expressed by weight of eicosanoic acid to behenic acid = 2 to 3), where 90% of the hydroxyl groups of the hydrophilic polymer had reacted The molecular weight Mw was 10,500 g / mol. Other particularities for the production of the hydrophilic polymer as well as for the esterification can be extracted from the documents EP-B1-0630389 or WO 93/01760.

For the preparation of the preparation they dispersed 20% by weight of the amino acid DL-methionine (CAS: 59-51-8; available commercially from Degussa® AG; ground particle size d90 in the range of 1 µm to 100 µm) in the polymer melted at a temperature of about 95 ° C with a stirrer spiral at 200 revolutions per minute in a first tank mixer for 5 minutes.

In an additional mixing tank was charged initially a mixture of surfactants consisting of 1% by weight of polyvinyl alcohol (M = 6000 g / mol, Polisciences®, Warrington, USA) and 0.1% by weight of an alcohol ethoxylated fat (Tego® Alkanol L4 from Degussa® AG) in water a 70 ° C with stirring.

Then the polymer melt produced in the first mixing tank, which also included polymer the low molecular weight substance was transferred from the first mixing tank under continuous agitation with a stirrer ULTRA-TURRAX at 2000 revolutions per minute at second mixing tank at 70 ° C.

After a residence time of 0.5 to 10 minutes and a cooling of the composition contained in the second mixing tank at a temperature, which was 15 ° C lower than the melting temperature of the polymer, particles formed. With a peristaltic pump the suspension was sent to a centrifuge, in the which particles of the active substance were separated at 25 ° C from the continuous phase Then the particles of the active substance dried in a vacuum dryer at 25 ° C and 10 mbar for 100 h.

These particles had a distribution of particle sizes of 200 \ mum <d_ {90, part \ text {í} cula} <300 µm. The particles were free of solvents undesirable and were made of hyperbranched polyester modified with fatty acids and approx. 12% by weight of DL-methionine, referred to the mass of the particle.

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Example 2

Example 1 was essentially repeated, using however a hyperbranched polyester, which had obtained by hydrophobicizing Boltorn H30® with an acid mixture stearic and palmitic acid (ratio expressed by weight of acid stearic to palmitic acid = 2 to 1), where 50% of the groups hydroxyl of the hydrophilic polymer had been transformed. The weight Molecular M w was 7500 g / mol.

The particles obtained had a 150 \ mum particle size distribution < d_ {90, part \ text {í} cula} <300 \ mum. The particles were exempt from undesirable solvents and were constituted by the Hyperbranched polyester modified with fatty acids and approx. 16% by weight of DL-methionine, referred to the mass of the particle.

Storage stability was tested, shear stability and enzymatic degradability of the microparticles obtained.

The determination of stability at storage was performed by microparticle storage dried in a glass bowl, storage is done at room temperature in an atmosphere that contained oxygen (air). After a storage period of 6 months, the methionine content determined chromatographically by HPLC was at least 98% of the initial value.

For the stability test at shear, there was a dispersion of the microparticles obtained in a Pharmaöl (WINOG 100 Pharma paraffin oil from Univar GmbH). For this the particles were transformed into a Standard Pharmaöl (Paraffin oil WINOG 100 Pharma from the firm Univar® GmbH) with an ULTRA-TURRAX stirrer, which spun for 1 minute at 20,000 rpm. A comparison of the microscopic image of the particles of the active substance before and after the transformation in the standard Pharmaöl indicated that no some alteration of the integrity of the particles was observed and that, therefore, the protective effect for the biologically active principle DL-methionine.

Enzymatic release of the active substance Microparticle content was performed with a lipase. For this was suspended 0.22 g of microparticles in 15 ml of solution of the enzyme Lipomod 34P (Biocatalyst Lmt., United Kingdom) in buffer phosphate (pH 5.01) (Lipomod 34P concentration was 0.5 mg / ml) The sample was stored in a 37 ° C water bath without mixing At regular intervals of time a sample of 2 ml The concentration of the active substance was analyzed chromatographically by HPLC. After 24 hours he had released approximately 70% of encapsulated methionine. For him On the contrary, the enzyme-free buffer solution had been released less than 20% of the encapsulated methionine after 24 hours.

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Example 3

Example 2 was essentially repeated, except that L-leucine was used (CAS: 61-90-5; commercially available from Degussa® AG; particle size d90 in the range of 1 µm to 10 µm) instead of DL-methionine. In In this case, the polymer melt was produced at a temperature of about 85 ° C. Additionally, the stirrer ULTRA-TURRAX was operated during the passage of the polymer melt to the second liquid phase at 3000 revolutions per minute.

The particles obtained had a 10 \ mum particle size distribution < d_ {90, part \ text {í} cula} <50 \ mum. The particles were exempt from undesirable solvents and were constituted by the Hyperbranched polyester modified with fatty acids and approx. 16% by weight of L-leucine, referred to the mass of the particles

In the study of stability at shear, these microparticles also had a high stability. A comparison of the microscopic image of the active substance particles before and after incorporation in the standard Pharmaöl indicated that no alteration could be seen some of the integrity of the particles and therefore, that the effect protector for the biologically active principle L-leucine could be maintained.

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Example 4

Example 2 was essentially repeated, except that L-lysine (CAS: 56-87-1; ground; 50% by weight; commercially available from Degussa® AG; size of particle d90 in the range of 1 µm to 10 µm) instead of DL-methionine In this case, the melt of Polymer was produced at a temperature of approximately 85 ° C.

The particles obtained exhibited a 150 \ mum particle size distribution < d_ {90, part \ text {í} cula} <300 \ mum. The particles were exempt from undesirable solvents and were constituted by the Hyperbranched polyester modified with fatty acids and approx. 8% by weight of L-lysine, referred to the mass of the particles

In the study of stability at shear, these microparticles also exhibited a high stability A comparison of the microscopic image of the active substance particles before and after incorporation in the standard Pharmaöl indicated that no alteration could be seen some of the integrity of the particles and therefore, that the effect protector for the biologically active principle L-lysine could be maintained.

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Example 5

Example 1 was essentially repeated, using however a hyperbranched polyester, which had obtained by hydrophobicizing Boltorn H30® with an acid mixture stearic and palmitic acid (ratio expressed by weight of acid stearic to palmitic acid = 2 to 1), where 95% of the groups Polymer hydroxyl had been transformed. Molecular weight M_ {w} was 10,000 g / mol. In addition, it was used L-tryptophan (CAS: 73-22-3; commercially available from Degussa® AG); particle size d90 in the interval 1 µm to 10 µm) instead of DL-methionine as a low molecular weight substance. In this case the melt Polymer was produced at a temperature of approximately 85 ° C. Additionally, the ULTRA-TURRAX agitator was made function during the passage of the polymer melt to the second liquid phase at 3000 revolutions per minute.

The particles obtained exhibited a 10 \ mum particle size distribution < d_ {90, part \ text {í} cula} <60 \ mum. The particles were free of undesirable solvents and made up of polyester hyperbranched modified with fatty acids and approx. 16% by weight of L-tryptophan, referred to the mass of particles

In the study of shear stability these microparticles also showed high stability. A comparison of the microscopic images of the particles of the active substance before and after incorporation in the Pharmaöl standard, showed that no alteration of the particle integrity and therefore that the effect protector for the biologically active principle L-tryptophan could be maintained.

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Example 6

Example 5 was essentially repeated, except that a solution of banana extract (20% by weight of banana extract in ethanol) instead of L-tryptophan. In this case, 20% was dissolved in volume of banana extract solution in the polymer molten.

The particles obtained had a distribution of particle sizes of 10 \ mum <d_ {90, part \ text {í} cula} <60 \ mum. The particles were free of solvents undesirable and were made of hyperbranched polyester modified with fatty acids and approx. 3% p of banana extract, referred to the mass of the particles.

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Example 7

Example 5 was essentially repeated, except that a combination of strawberry extract solution was used (20% by weight of strawberry extract in ethanol) and creatine (Creapure, CAS: 50-00-1, ground, available commercially from Degussa® AG; particle size d90 in the range of 0 µm to 10 µm) instead of L-tryptophan. In this case, 5% were dissolved in volume of strawberry extract solution and 20% by weight creatine in the molten polymer.

The particles obtained indicated a 10 \ mum particle size distribution < d_ {90, part \ text {í} cula} <60 \ mum. The particles were exempt from undesirable solvents and were constituted by the Hyperbranched polyester modified with fatty acids and approx. 0.8% by weight strawberry extract and 16% by weight creatine, referred to the mass of the particles.

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Example 8

Example 5 was essentially repeated, except that a combination of acid was used L (+) - ascorbic (vitamin C, CAS: 50-81-7), ground, available commercially from AcrosOrganics®, particle size d90 in the range of 0 µm to 10 µm and creatine (Creapure, CAS: 50-00-1, ground, available commercially from Degussa® AG; particle size d90 in the range of 0 µm to 10 µm) instead of L-tryptophan. In this case they dispersed 10% in weight of L (+) - ascorbic acid and 10% by weight of Creatine in molten polymer.

The particles obtained threw a 10 \ mum particle size distribution < d_ {90, part \ text {í} cula} <50 \ mum. The particles were exempt from undesirable solvents and were constituted by the Hyperbranched polyester modified with fatty acids and approx. 8% by weight of L (+) - ascorbic acid and 8% by weight of creatine, referred to the mass of the particles.

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Example 9

Example 5 was essentially repeated, except that a combination of lemon aroma solution (20% in weight of lemon aroma solution in ethanol) and percarbonate (sodium percarbonate for detergents, commercially available from AcrosOrganics®; particle size d90 in the interval from 1 µm to 10 µm), particle size d90 in the range from 0 µm to 10 µm) instead of L-tryptophan. In this case, 5% by volume of aroma solution of Lemon and 20% by weight sodium percarbonate in the polymer molten. Additionally, the ULTRA-TURRAX stirrer is operated during the passage of the polymer melt to the second liquid phase at 2000 revolutions per minute.

The particles obtained threw a 10 \ mum particle size distribution < d_ {90, part \ text {í} cula} <60 \ mum. The particles were exempt from undesirable solvents and were constituted by the Hyperbranched polyester modified with fatty acids and approx. 0.8% by weight of lemon aroma and 16% by weight of percarbonate of sodium, referred to the mass of the particles.

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Example 10

Example 2 was essentially repeated, except that ammonium persulfate (CAS: 7727-54-0; available commercially from Degussa® AG; particle size d90 in the range of 1 µm to 200 µm) instead of DL-methionine In this case, the melt of Polymer was produced at a temperature of approximately 70 ° C.

The particles obtained threw a 250 \ mum particle size distribution < d_ {90, part \ text {í} cula} <400 \ mum. The particles were exempt from undesirable solvents and were constituted by the Hyperbranched polyester modified with fatty acids and approx. 16% by weight of ammonium persulfate, based on the mass of the particles

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Example 11

Example 2 was essentially repeated, however, L-tryptophan (CAS: 73-22-3; commercially available from Degussa® AG; particle size d90 in the range of 1 µm to 10 µm) instead of DL-methionine. In In this case, the polymer melt was produced at a temperature of about 85 ° C. Additionally, the stirrer ULTRA-TURRAX remained in operation during the passage from the polymer melt to the second liquid phase at 1000 revolutions per minute.

The particles obtained accused a 300 \ mum particle size distribution < d_ {90, part \ text {í} cula} <500 \ mum. The particles were exempt from undesirable solvents and were constituted by the Hyperbranched polyester modified with fatty acids and approx. 16% by weight of L-tryptophan, referred to the mass of the particle. This example indicates that the particle size can easily adjust by the process corresponding to the invention at a desired value, without thick particles accusing formation Some fine dust.

Claims (34)

1. Particle preparation comprising at least one substance of low molecular weight with a molecular weight in the range of 15 g / mol to 1000 g / mol and at least one hyperbranched polymer, characterized in that the particles have a size comprised in the range of 1 µm to 1000 µm, the low molecular weight substance is included in a sheath, which contains hyperbranched polymer, and the hyperbranched polymer contains a hydrophilic core with polyester units and hydrophobic end groups, where the hyperbranched polymer has a molecular weight greater than or equal to 6000 g / mol and a hydroxyl number in the range of 0 to 200 mg KOH / g, the degree of branching being in the range of 20 to 70% and the hyperbranched polymer has a temperature of melting of at least 30 ° C. 2. Prepared according to claim 1, characterized in that the hyperbranched polymer has a degree of functionalization of at least 30%. 3. Prepared according to claim 1 or 2, characterized in that the hyperbranched polymer has a water solubility according to the 40 ° C flask method of 10% by weight maximum. 4. Prepared according to at least one of the preceding claims, characterized in that the hydrophilic core contains at least 90% by weight of repeating units, which are derived from polyester forming monomers. 5. Prepared according to at least one of the preceding claims, characterized in that the hydrophilic core has a central unit, which is derived from an initiator molecule with at least two hydroxy groups, and repetitive units, which are derived from monomers with at least one group. carboxyl and at least two hydroxy groups. 6. Prepared according to claim 5, characterized in that the initiating molecule is an aliphatic polyol. 7. Prepared according to claim 5 or 6, characterized in that the initiating molecule is selected from ditrimethylolpropane, ditrimethylolethane, dipentaerythritite, pentaerythritite, alkoxylated pentaerythritite, trimethylolethane, trimethylolpropane, alkoxylated trimethylolpropane, glycerol-dimethyl-oxy-dimethyl-ethane-1,3-dimethyl alcohol-diopene-1-dimethyl-ethane-1-dimethylpropyl-diopane-1-dimethyl ethane-1-dimethylolpropane 5,5-dimetanol. 8. Prepared according to at least one of claims 5 to 7, characterized in that the monomers are selected from the group consisting of dimethylpropionic acid, acid α, α-bis (hydroxymethyl) butyric acid, acid α, α, α-tris (hydroxymethyl) acetic acid, acid α, α-bis (hydroxymethyl) valeric, acid α, α-bis (hydroxy) propionic I 3,5-dihydroxybenzoic acid.

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9. Prepared according to at least one of the preceding claims, characterized in that the hydrophobic end groups are formed by groups derived from carboxylic acids with at least 10 carbon atoms. 10. Prepared according to claim 9, characterized in that the carboxylic acids have a melting point of at least 40 ° C. 11. Prepared according to claim 9 or 10, characterized in that at least a part of the carboxylic acids is selected from decanoic acid, dodecanoic acid, tetradecanoic acid, hexadecanoic acid, heptadecanoic acid, octadecanoic acid, eicosanoic acid, docosanoic acid and tetracosanoic acid. 12. Prepared according to at least one of the preceding claims 9 to 11, characterized in that at least a part of the hydrophobic end groups are formed by groups derived from carboxylic acids having a maximum of 18 carbon atoms. 13. Prepared according to at least one of the preceding claims 9 to 11, characterized in that the proportion of carboxylic acids with 12 to 18 carbon atoms is at least 30% by weight, based on the weight of the carboxylic acids used for hydrophobicization. 14. Prepared according to at least one of the preceding claims, characterized in that the hyperbranched polymer has an acid number in the range of 0 to 20 mg KOH / g. 15. Prepared according to at least one of the preceding claims, characterized in that the hyperbranched polymer has a melting temperature of a maximum of 57 ° C.

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16. Prepared according to at least one of the preceding claims, characterized in that the hydrophilic core has a hydroxyl number, measured before hydrophobicization, in the range of 400 to 600 mg KOH / g. 17. Prepared according to at least one of the preceding claims, characterized in that the low molecular weight substance is a compound with a peroxide group. 18. Prepared according to at least one of the preceding claims, characterized in that the low molecular weight substance is an amino acid. 19. Prepared according to at least one of the preceding claims, characterized in that the low molecular weight substance is a catalyst. 20. Prepared according to at least one of the preceding claims, characterized in that the low molecular weight substance is a dye and / or pigment. 21. Prepared according to at least one of the preceding claims, characterized in that the low molecular weight substance is a vitamin. 22. Prepared with at least one of the preceding claims, characterized in that the low molecular weight substance is a monomer. 23. Prepared according to at least one of the preceding claims, characterized in that the low molecular weight substance is a flavoring or flavoring agent. 24. Prepared according to at least one of the preceding claims, characterized in that the low molecular weight substance is a biologically active component, particularly a medicament, a vitamin, an enzyme, a coenzyme, and / or a plant extract. 25. Prepared according to at least one of the preceding claims, characterized in that the low molecular weight substance is an initiator, a silicone, a surfactant, a silica, a silane, a solvent, a filler, a reactive crosslinker, a detergent, a hair dye and / or a concrete additive. 26. Prepared according to at least one of the preceding claims, characterized in that the hyperbranched polymer is enzymatically degradable. 27. Prepared according to at least one of the preceding claims, characterized in that at least 80% by weight of the particles are within a size range of 100 µm or less. 28. Prepared according to at least one of the preceding claims, characterized in that the hyperbranched polymer exhibits at 48 ° C in a 50% / 50% mixture with exclusively liquid-liquid equilibrium water, but does not exhibit any solid-liquid or solid-liquid-liquid equilibrium . 29. Process for the production of preparations according to at least one of claims 1 to 28 by mixing a hyperbranched polymer and at least one weight substance low molecular 30. Use of a preparation according to at least one of claims 1 to 28, as a hardening agent, as crosslinking agent, as catalyst, as antifoam, as dispersant, as an additive with antimicrobial or antifungal action, as an additive to increase the scratch resistance of surfaces, as an additive in coatings or adhesives, such as fluidity improver and / or as an additive for concrete. 31. Use of a preparation according to at least one of claims 1 to 28 in cosmetics, in medicines, in deodorants, in food products, in feed, in drinks, in wall or floor coverings, in joint materials, in gaskets and / or in varnish systems. 32. Process for the release of low molecular weight substances from preparations according to at least one of claims 1 to 28, characterized in that the hyperbranched polymer degrades enzymatically. 33. Process for the production of preparations according to at least one of claims 1 to 28, characterized in that a compressed gas is used or at least two liquid phases are formed, both phases containing the low molecular weight substance and containing at least one liquid phase. a hyperbranched polymer. 34. Process for the production of preparations according to at least one of claims 1 to 28, comprising the production steps of a polymer melt comprising the less a hyperbranched polymer and at least one substance of weight low molecular, incorporation of the polymer melt into a second liquid phase, in which the hyperbranched polymer is hardly soluble and that has a solidification temperature lower than the polymer solidification temperature hyperbranched, dispersion of the polymer melt in the second liquid phase at a temperature that is greater than or equal to the solidification temperature of the hyperbranched polymer, and solidification of the polymer melt dispersed in the Second liquid phase