EP1178777A2 - Forme galenique pour administration dans des orifices corporels - Google Patents

Forme galenique pour administration dans des orifices corporels

Info

Publication number
EP1178777A2
EP1178777A2 EP00943585A EP00943585A EP1178777A2 EP 1178777 A2 EP1178777 A2 EP 1178777A2 EP 00943585 A EP00943585 A EP 00943585A EP 00943585 A EP00943585 A EP 00943585A EP 1178777 A2 EP1178777 A2 EP 1178777A2
Authority
EP
European Patent Office
Prior art keywords
capsule
capsule according
active ingredient
rapidly disintegrating
namely
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Withdrawn
Application number
EP00943585A
Other languages
German (de)
English (en)
Inventor
Roland Bodmeier
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Individual
Original Assignee
Individual
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Individual filed Critical Individual
Publication of EP1178777A2 publication Critical patent/EP1178777A2/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816—Wall or shell material
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056—Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4816—Wall or shell material
    • A61K9/4825—Proteins, e.g. gelatin

Definitions

  • the present invention relates to capsules for the application of active substances which rapidly enter body openings, e.g. disintegrate in the oral cavity or after rectal or vaginal application.
  • Solid dosage forms e.g. tablets or capsules
  • enter the stomach and release the drug which is then absorbed in the gastrointestinal tract or acts locally.
  • swallowing solid dosage forms is difficult and can lead to compliance problems (e.g. not taking or spitting out the dosage form). Swallowing solid dosage forms without liquid is difficult or impossible.
  • traveling taking solid dosage forms with water is often not recommended for hygienic reasons.
  • the application of solid single-body systems is also difficult in animals.
  • the rapidly disintegrating dosage forms described also have some disadvantages, such as lack of mechanical stability and high sensitivity to moisture.
  • the tablets produced by lyophilization are very fragile, for example they cannot be pressed out of a blister pack, but have to be removed. Also, the tablet-like dosage forms are usually made with very low hardness in order to accelerate their disintegration To enable increased porosity or to reduce the damage to coated active ingredient particles.
  • the object of this invention was therefore to develop a rapidly disintegrating dosage form which avoids many of the problems mentioned above.
  • a capsule for applying active substances comprising at least one macromolecule which is soluble and / or rapidly disintegrating in aqueous liquids, or a mixture of at least two of these substances, the capsule rapidly disintegrating into body openings after application .
  • the object is achieved according to the invention in that a capsule for oral administration of active ingredients is made available, the capsule rapidly disintegrating in the mouth or in the oral cavity.
  • the object is achieved in that a capsule for vaginal, rectal or nasal Application of active ingredients is provided, the capsule rapidly disintegrating after insertion into the body opening.
  • the object is achieved in that a capsule quickly disintegrates after being introduced into body openings which have arisen as a result of surgical interventions or injuries.
  • the macromolecule is selected from natural and / or synthetic polymers, such as proteins and peptides, for example gelatin, albumin, polysaccharides, for example agar-agar, alginates, carageen, chitosan, dextrin, dextran, pectin, starch and their derivatives, gums, cellulose derivatives , for example hydroxypropylmethyl cellulose, hydroxypropyl cellulose, methyl cellulose, carboxymethyl cellulose, polyacrylates, namely polyacrylic acid, polyacrylamide, polyethylene glycol, polyvinyl alcohol (also partially hydrolyzed), polyvinyl pyrrolidone, polyoxyethylene oxypropylene and
  • natural and / or synthetic polymers such as proteins and peptides, for example gelatin, albumin, polysaccharides, for example agar-agar, alginates, carageen, chitosan, dextrin, dextran, pectin, starch and their derivatives, gums,
  • a capsule is preferred according to the invention, one or more disintegrants, swelling agents (swelling agents) and / or solubilizers or mixtures thereof being contained as further auxiliaries.
  • the disintegration accelerator is selected from, for example, effervescent salts, sugar, sucrose, sorbitol, mannitol, sucrose. It is also preferred according to the invention that further auxiliaries, namely flavorings, sweeteners, colorants, preservatives, gelling agents, fillers, pigments, wetting agents (surfactants) and plasticizers are contained.
  • the capsule according to the invention is further characterized in that the capsule shell has micropores.
  • the capsule shell encloses cavities in the form of gas bubbles.
  • the capsule according to the invention itself comprises an active ingredient in the capsule shell.
  • the active substance-containing filling is solid, semi-solid or liquid.
  • the active substance is in retarded form.
  • the active ingredient is present in taste-masked form.
  • Another object of the present invention is a medicament comprising a capsule according to the invention and a pharmaceutical preparation contained therein, comprising at least one active pharmaceutical ingredient and, if appropriate, further pharmaceutically acceptable auxiliaries and additives.
  • the object of the invention was therefore achieved with a rapidly disintegrating capsule-like dosage form.
  • the active ingredient / excipient mixture is filled into a rapidly disintegrating capsule shell.
  • the capsule disintegrates quickly or quickly dissolves in the oral cavity, the solid or liquid contents are then swallowed.
  • Rapidly disintegrating is a broad term and means that the capsule shell quickly loses its shape after application in the oral cavity and can be swallowed quickly with the contents.
  • the disintegration can be positively influenced by moving the capsule (eg by moving the tongue).
  • the disintegration time is a few minutes, but preferably less than 30 seconds.
  • the capsule according to the invention has a number of advantages.
  • the coated active ingredient particles are e.g. not exposed to high pressures.
  • the capsule material used according to the invention can be any material which is soluble or disintegrating in aqueous liquids.
  • Macromolecules which dissolve or disintegrate rapidly in water are preferably used. These include both natural and synthetic polymers, such as proteins / peptides (e.g. gelatin, albumin), polysaccharides (e.g. agar-agar, alginates, carageen, chitosan, dextrin, dextran, pectin, starch and their derivatives, gums of natural origin) cellulose derivatives (e.g. hydroxypropylmethyl cellulose, hydroxypropyl cellulose, methyl cellulose, carboxymethyl cellulose), polyacrylates (e.g. polyacrylic acid, polyacrylamide), polyethylene glycol, polyvinyl alcohol (also partially hydrolyzed),
  • proteins / peptides e.g. gelatin, albumin
  • polysaccharides e.g. agar-agar, alginates, carageen, chi
  • Molecular weight plays an important role in the case of polymers; capsule materials with a low molecular weight disintegrate or usually dissolve more quickly. Higher concentration liquid systems can also be produced with the low molecular weight oligomers / polymers.
  • the molecular weight of the polymers can be determined, for example, by hydrolytic or enzymatic degradation can be reduced. In the case of some polymers (eg gelatin) the molecular weight can be reduced, for example, by heating (eg autoclaving).
  • the capsule materials can also be used in combination.
  • Rapidly disintegrating / rapidly dissolving auxiliaries e.g. disintegrants such as effervescent salt or sugar and sugar derivatives such as sorbitol, mannitol, mannitol, sorbitol, sucrose
  • disintegrants such as effervescent salt or sugar and sugar derivatives such as sorbitol, mannitol, mannitol, sorbitol, sucrose
  • Decay can also be affected by the porosity of the capsule shell.
  • Gas bubbles can be incorporated into the capsule shell to increase the porosity and thus to accelerate the disintegration during the capsule shell production (e.g. dispersion of gas in the liquid during the immersion process).
  • volatile components can be incorporated into the capsule shell during manufacture, which, when removed, result in a porous capsule shell.
  • auxiliary substances can also be incorporated into the capsule shell.
  • these include, for example, flavorings, sweeteners, colorants, preservatives, gelling agents (to support the formation of the capsule shell, for example during the immersion process), fillers, pigments, wetting agents (surfactants) and plasticizers.
  • the capsules can also be coated with a thin layer which, for example, reduces sensitivity to moisture or has a positive effect on the flow of saliva.
  • the active ingredient also in "treated form", for example micro / nanoparticles
  • the contents of the capsule contain the active ingredient and, if necessary, various auxiliary substances.
  • the contents can be solid, semi-solid or liquid.
  • the dosage forms according to the invention are normally used for active substances which are absorbed in the gastrointestinal tract or which act locally. However, absorption or local effects in the oral cavity is also possible.
  • the capsule can also be used in other body openings. This includes in particular the vaginal, rectal, nasal route of application and also body openings caused by surgical interventions or injuries.
  • the dosage forms according to the invention can be used for the administration of a large number of active substances or combinations of active substances. Possible drugs are listed in the textbook of pharmacology and toxicology "drug effects" by E. Mutschier,ticianliche Verlagsgesellschaftsch mbH.
  • the active ingredient may be in a delayed form.
  • the active ingredient can, for example, be incorporated into pellets (matrix or reservoir pellets), microparticles (eg microsphere or microcapsules) or colloidal particles (eg nanoparticles, liposomes).
  • Different retarding materials can be used, e.g. polymers with pH-dependent solubility (e.g. enteric polymers) or polymers insoluble in gastrointestinal juice (e.g. cellulose derivatives, acrylate derivatives, polyester) or biodegradable polymers (e.g. poly (lactide-co-glycolide) or lipids .
  • the active ingredient dissolution can be improved by known galenic methods (e.g. dissolving in a suitable solvent, embedding in carrier materials, reducing the particle size by physical or chemical methods - also nanoparticles, nanocrystals, encapsulation in colloidal carrier particles, such as liposomes, lipid or polymer nanoparticles ) and the active ingredient is added or incorporated into the product in this form.
  • galenic methods e.g. dissolving in a suitable solvent, embedding in carrier materials, reducing the particle size by physical or chemical methods - also nanoparticles, nanocrystals, encapsulation in colloidal carrier particles, such as liposomes, lipid or polymer nanoparticles
  • Oral hygiene used for oral use or ingestion become .
  • the contents can be solid, semi-solid or liquid.
  • the active ingredient or the active ingredient processed as described above can be dissolved and / or dispersed in a liquid and then filled into the capsule in liquid form.
  • the solid filling material can be in powder or granule form or also in the form of small tablets or pellets or rapidly disintegrating matrix systems.
  • the contents can also contain auxiliary substances. These include e.g. Flavors, flavors, sweeteners, disintegrants, wetting agents, colorants, flow regulators, fillers, binders.
  • An effervescent set can also be used to help the capsule contents disintegrate more quickly or to improve taste and stimulate salivation.
  • Auxiliaries known to the person skilled in the art can also be added, which improve the mouthfeel of the dosage form.
  • the invention also relates to processes for producing the dosage form according to the invention.
  • the capsule shells can be produced by known capsule production methods, analogous to the production of soft or hard capsules. This includes, for example, the immersion process, in which capsule-shaped metal pins are immersed in a liquid which contains the capsule materials / auxiliary substances, the liquid adheres to the surface of the pin and the capsule shells are obtained after drying.
  • the capsule materials and other auxiliary substances are described in a solvent or solvent mixture (preferably containing water) dissolved or dispersed.
  • the capsule shells can also be produced by immersing the pins in the melt and then cooling them.
  • the size and shape of the capsule shell is determined by the size and shape of the pins.
  • the capsules are manufactured by means of injection molding, in which the capsule mass is introduced into preformed forms.
  • the capsules can be filled with the contents and sealed by the process known to the person skilled in the art.
  • Capsule-shaped dip sticks (capsule size 00) were placed in a heated, autoclaved gelatin solution (20-40%) in the
  • Glycerol and sorbitol was dissolved, immersed and pulled out again. After drying, the capsule halves were pulled off, cut and put together. The capsule shells disintegrated in the oral cavity in less than 30 seconds.
  • Capsule-shaped dip sticks (capsule size 00) were immersed in an autoclaved gelatin solution (20-40%) in which glycerol and sorbitol were dissolved and fine air bubbles were dispersed, and pulled out again. After drying, the capsule halves were peeled off, cut, and put together. The capsule shells disintegrated in the oral cavity in less than 30 seconds.
  • the capsules produced according to Example 1 or 2 were filled with a mixture of lactose and microencapsulated paracetamol (taste masked, coated with ethyl cellulose) before the capsule shells were put together.
  • the capsules disintegrated in the oral cavity in less than 30 seconds.
  • the capsules produced according to Example 1 or 2 were filled with a mixture of microcrystalline cellulose, effervescent salt and propranolol HCl sustained release pellets (coated with ethyl cellulose) before the capsule shells were put together.
  • the capsules disintegrated in the oral cavity in less than 30 seconds.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nutrition Science (AREA)
  • Physiology (AREA)
  • Zoology (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne une capsule pour l'administration de principes actifs, comprenant au moins une macromolécule soluble et/ou se décomposant rapidement dans des fluides aqueux ou bien un mélange constitué d'au moins deux de ces macromolécules, la capsule se décomposant rapidement dans les orifices corporels.
EP00943585A 1999-05-10 2000-05-10 Forme galenique pour administration dans des orifices corporels Withdrawn EP1178777A2 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE19922537 1999-05-10
DE1999122537 DE19922537A1 (de) 1999-05-10 1999-05-10 Darreichungsform zur Applikation in Körperöffnungen
PCT/DE2000/001512 WO2000067723A2 (fr) 1999-05-10 2000-05-10 Forme galenique pour administration dans des orifices corporels

Publications (1)

Publication Number Publication Date
EP1178777A2 true EP1178777A2 (fr) 2002-02-13

Family

ID=7908255

Family Applications (1)

Application Number Title Priority Date Filing Date
EP00943585A Withdrawn EP1178777A2 (fr) 1999-05-10 2000-05-10 Forme galenique pour administration dans des orifices corporels

Country Status (4)

Country Link
EP (1) EP1178777A2 (fr)
AU (1) AU5802800A (fr)
DE (2) DE19922537A1 (fr)
WO (1) WO2000067723A2 (fr)

Families Citing this family (10)

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Publication number Priority date Publication date Assignee Title
GB0114746D0 (en) * 2001-06-16 2001-08-08 Boots Co Plc Medicinal composition
NO20021592D0 (no) 2002-04-04 2002-04-04 Fmc Biopolymer As Polysakkaridkapsler og fremgangsmåte ved fremstilling derav
US9254270B2 (en) 2002-10-01 2016-02-09 Banner Life Sciences Llc Enteric soft capsules
ES2500316T3 (es) 2002-10-01 2014-09-30 Banner Pharmacaps, Inc. Composición entérica para la fabricación de una cubierta de cápsula blanda
US20060275361A1 (en) * 2005-06-03 2006-12-07 Cadbury Adams Usa Llc. Rapidly dissolving gelatin compositions and products made therefrom
EP1991196B1 (fr) 2006-03-03 2016-10-12 Fmc Corporation Procédé et appareil de préparation de capsules.
US9272123B2 (en) 2013-12-16 2016-03-01 Esther Gallant Device and method for inserting lubricating capsule
US10058447B2 (en) 2013-12-16 2018-08-28 Esther Gallant Lubricating condom
US9775814B2 (en) 2014-06-20 2017-10-03 Patheon Softgels Inc. Enteric soft capsule compositions
CN104758271A (zh) * 2015-03-16 2015-07-08 中华生物科技有限公司 纤维素胶与红藻卡帕胶复配的植物空心胶囊及制备方法

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GB2077691B (en) * 1980-06-05 1983-11-02 Shinetsu Chemical Co Medicament capsules for rectal administration
JPS572218A (en) * 1980-06-05 1982-01-07 Shionogi & Co Ltd Capsule agent for rectal administration
DK242083D0 (da) * 1983-05-27 1983-05-27 Hansens Chr Bio Syst Vaginalkapsler
DE3529694A1 (de) * 1985-08-20 1987-02-26 Scherer Gmbh R P Gelatinekapseln und verfahren zu ihrer herstellung
KR880701098A (ko) * 1986-04-01 1988-07-25 로버어트 에이 아미테이지 메틸프레드니솔론/소디움 카르복시메틸 전분 정제 조성물
DE3738236A1 (de) * 1987-11-11 1989-05-24 Euro Celtique Sa Beisskapsel
US4935243A (en) * 1988-12-19 1990-06-19 Pharmacaps, Inc. Chewable, edible soft gelatin capsule
JPH03255024A (ja) * 1990-03-05 1991-11-13 Tokai Capsule Kk 口中易溶軟カプセル剤
BE1007402A5 (nl) * 1993-03-26 1995-06-06 Adir Nasale farmaceutische preparaten met progestagene stof.
MX9706062A (es) * 1995-02-08 1997-10-31 Yamanouchi Europ Bv FORMAS DE DOSIFICACION ORAL CONTENIENDO UN ANTIBIOTICO DE beta -LACTAMA.
RU2102981C1 (ru) * 1996-07-31 1998-01-27 Акционерное общество открытого типа "Нижегородский химико-фармацевтический завод" Состав желатиновых масс для получения ректокапсул
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Non-Patent Citations (1)

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Also Published As

Publication number Publication date
DE19922537A1 (de) 2000-11-16
WO2000067723A2 (fr) 2000-11-16
AU5802800A (en) 2000-11-21
WO2000067723A3 (fr) 2001-05-31
DE10081194D2 (de) 2002-04-25

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