EP1007007A1 - Formulation a base d'acide ascorbique, caracterisee par une meilleure stabilite des couleurs - Google Patents

Formulation a base d'acide ascorbique, caracterisee par une meilleure stabilite des couleurs

Info

Publication number
EP1007007A1
EP1007007A1 EP98943755A EP98943755A EP1007007A1 EP 1007007 A1 EP1007007 A1 EP 1007007A1 EP 98943755 A EP98943755 A EP 98943755A EP 98943755 A EP98943755 A EP 98943755A EP 1007007 A1 EP1007007 A1 EP 1007007A1
Authority
EP
European Patent Office
Prior art keywords
preparation according
weight
ascorbic acid
cellulose
sugar alcohols
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Withdrawn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
EP98943755A
Other languages
German (de)
English (en)
Inventor
Eugen Schwarz
Gernot Möschl
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.)
Merck Patent GmbH
Original Assignee
Merck Patent GmbH
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 Merck Patent GmbH filed Critical Merck Patent GmbH
Publication of EP1007007A1 publication Critical patent/EP1007007A1/fr
Withdrawn legal-status Critical Current

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/365Lactones
    • A61K31/375Ascorbic acid, i.e. vitamin C; Salts thereof
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23GCOCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
    • A23G3/00Sweetmeats; Confectionery; Marzipan; Coated or filled products
    • A23G3/34Sweetmeats, confectionery or marzipan; Processes for the preparation thereof
    • A23G3/346Finished or semi-finished products in the form of powders, paste or liquids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/0012Galenical forms characterised by the site of application
    • A61K9/0053Mouth and digestive tract, i.e. intraoral and peroral administration
    • A61K9/0056Mouth 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2013Organic compounds, e.g. phospholipids, fats
    • A61K9/2018Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/02Nutrients, e.g. vitamins, minerals
    • AHUMAN NECESSITIES
    • A23FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
    • A23GCOCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF
    • A23G2200/00COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF containing organic compounds, e.g. synthetic flavouring agents
    • A23G2200/04COCOA; COCOA PRODUCTS, e.g. CHOCOLATE; SUBSTITUTES FOR COCOA OR COCOA PRODUCTS; CONFECTIONERY; CHEWING GUM; ICE-CREAM; PREPARATION THEREOF containing organic compounds, e.g. synthetic flavouring agents containing vitamins, antibiotics, other medicaments

Definitions

  • the invention relates to a new formulation based on ascorbic acid with an improved taste, which is directly compressible and has an improved color stability.
  • lozenges and especially chewable tablets are increasingly being offered in the area of nutritional supplements (vitamin and mineral supplementation). Furthermore, one tries to produce solid ones
  • Formulations increasingly use directly compressible active ingredients (DC active ingredients) in order to reduce production costs.
  • DC active ingredients directly compressible active ingredients
  • the invention thus relates to preparations containing ascorbic acid in a directly compressible form with an improved taste.
  • the invention therefore also relates to a process for the preparation of ascorbic acid-containing solid preparations in directly compressible form with an improved taste, characterized in that a) an aqueous solution is prepared containing
  • the invention furthermore relates to formulations which contain directly compressible ascorbic acid and which, in addition to at least one sugar alcohol, contain up to 1.5% by weight of one or more binders from the group cellulose, methyl cellulose, hydroxymethyl propyl cellulose, carboxymethyl cellulose, starch, maltodextrin and gum arabic.
  • the total amount of sugar alcohol used is to be selected so that 1.5 to 15% by weight, in particular 2 to 10% by weight, are present in the pulverulent substance mixture produced by the process according to the invention.
  • sugar alcohols from the group C 4 - C12 sugar alcohols are suitable for the preparation of the preparations containing ascorbic acid.
  • Particularly suitable sugar alcohols are in particular those from the group of erythritol, xylitol, mannitol and lactitol.
  • Lactitol based on 0.5 to 2.0 parts of sorbitol may be included.
  • composition according to the invention is therefore obtainable by dissolving at least one sugar alcohol in water and dissolving or suspending the ascorbic acid and spraying the aqueous mixture obtained in an air stream at a temperature of from room temperature to 180 ° C., preferably 60 to 140 ° C., drawing off air streams containing steam, and fluidized bed treatment, the fluidized bed having a low and variable height.
  • the homogeneous particles that form are discharged in solid form. Up to 1% by weight of the particles formed are returned to the process.
  • solid dosage forms can be produced directly from the preparations according to the invention described above without further processing, such as, for. B. Compresses.
  • the solid ascorbic acid preparations obtainable by spray granulation or spray fluidized bed granulation can also be mixed in a simple manner with one or more active ingredients and processed into tablet formulations.
  • these formulations can be processed into products that can be sold to the customer for self-medication.
  • These include, among other things, pain relievers in tablet form, cold remedies, such as throat tablets and lozenges. In such lozenges, the improved properties are noticeable by a smoother surface not only immediately after production, but also during sucking.
  • formulations according to the invention can be incorporated particularly advantageously into corresponding chewable tablets, since on the one hand they can be compressed without much energy expenditure, and on the other hand lead to improved chewing behavior due to the improved taste profile.
  • the preparations according to the invention can also be used to produce food supplements in a simple manner, both in tablet form and in any other manner known to the person skilled in the art.
  • the powdery, directly compressible ascorbic acid preparations can also be incorporated into a wide variety of confectionery products, such as lozenges, chewing gum or other confectionery products
  • the ascorbic acid formulations according to the invention in addition to an improved taste and direct compressibility, also lead to better storage stability of the products produced.
  • tablet formulations in which ascorbic acid is contained and to which binders have been added in order to achieve sufficient tablet hardness tend to yellow.
  • corresponding products which are manufactured using the preparations according to the invention have no discoloration, even after storage for several months. This is particularly the case if non-hygroscopic sugar alcohols, such as mannitol, are used to prepare the preparations. Satisfactory tablet hardness is also achieved without the addition of binders.
  • products are obtained which have reduced abrasion in experiments.

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Nutrition Science (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Physiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Zoology (AREA)
  • Diabetes (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Food Science & Technology (AREA)
  • Polymers & Plastics (AREA)
  • Medicinal Preparation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Confectionery (AREA)

Abstract

L'invention concerne une nouvelle formulation à base d'acide ascorbique qui a une meilleure image gustative, une meilleure stabilité des couleurs et une forme directement compressible.
EP98943755A 1997-07-31 1998-07-21 Formulation a base d'acide ascorbique, caracterisee par une meilleure stabilite des couleurs Withdrawn EP1007007A1 (fr)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE19733094 1997-07-31
DE19733094A DE19733094A1 (de) 1997-07-31 1997-07-31 Formulierung auf der Basis von Ascorbinsäure mit verbesserter Farbstabilität
PCT/EP1998/004556 WO1999006029A1 (fr) 1997-07-31 1998-07-21 Formulation a base d'acide ascorbique, caracterisee par une meilleure stabilite des couleurs

Publications (1)

Publication Number Publication Date
EP1007007A1 true EP1007007A1 (fr) 2000-06-14

Family

ID=7837556

Family Applications (1)

Application Number Title Priority Date Filing Date
EP98943755A Withdrawn EP1007007A1 (fr) 1997-07-31 1998-07-21 Formulation a base d'acide ascorbique, caracterisee par une meilleure stabilite des couleurs

Country Status (6)

Country Link
EP (1) EP1007007A1 (fr)
JP (1) JP2001511442A (fr)
CN (1) CN1265584A (fr)
CA (1) CA2298624A1 (fr)
DE (1) DE19733094A1 (fr)
WO (1) WO1999006029A1 (fr)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3770145A1 (fr) 2019-07-24 2021-01-27 Basf Se Processus de production continue soit d'acroléine soit d'acide acrylique comme produit cible à partir de propène

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE250415T1 (de) 1999-12-22 2003-10-15 Hoffmann La Roche Arzneizusammensetzung enthaltend ascorbinsäure und pektin
SE0100822D0 (sv) * 2001-03-09 2001-03-09 Astrazeneca Ab Method II to obtain microparticles
SE0100824D0 (sv) * 2001-03-09 2001-03-09 Astrazeneca Ab Method III to obtain microparticles
WO2003020265A2 (fr) 2001-09-03 2003-03-13 Dsm Ip Assets B.V. Compositions contenant une pectine et de l'acide ascorbique
DE102008004893A1 (de) * 2008-01-17 2009-07-23 Add Technologies Ltd. Trägerpellets, Verfahren zu deren Herstellung und deren Verwendung

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3293132A (en) * 1963-03-25 1966-12-20 Merck & Co Inc Spray dried vitamin compositions and method of preparation
NL184308C (nl) * 1975-07-24 1989-06-16 Takeda Chemical Industries Ltd Werkwijze voor het bereiden van l-ascorbienzuurgranules.
DE2706660A1 (de) * 1977-02-17 1978-08-24 Merck Patent Gmbh Ascorbinsaeure enthaltende granulate und verfahren zu ihrer herstellung
JPS5759803A (en) * 1980-09-30 1982-04-10 Takeda Chem Ind Ltd Granule of l-sodium ascorbate, its preparation, and tablet comprising it
CA1279574C (fr) * 1985-04-17 1991-01-29 Jeffrey L. Finnan Procede de lubrification de poudres de vitamines hydrosolubles

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
See references of WO9906029A1 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3770145A1 (fr) 2019-07-24 2021-01-27 Basf Se Processus de production continue soit d'acroléine soit d'acide acrylique comme produit cible à partir de propène
WO2021013640A1 (fr) 2019-07-24 2021-01-28 Basf Se Procédé de production continue d'acroléine ou d'acide acrylique en tant que produit cible à partir de propène

Also Published As

Publication number Publication date
CA2298624A1 (fr) 1999-02-11
JP2001511442A (ja) 2001-08-14
DE19733094A1 (de) 1999-02-04
CN1265584A (zh) 2000-09-06
WO1999006029A1 (fr) 1999-02-11

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