WO1999037308A1 - Procede pour la preparation d'une forme medicamenteuse se dissolvant rapidement dans la bouche et contenant de l'acarbose comme principe actif - Google Patents

Procede pour la preparation d'une forme medicamenteuse se dissolvant rapidement dans la bouche et contenant de l'acarbose comme principe actif Download PDF

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Publication number
WO1999037308A1
WO1999037308A1 PCT/EP1999/000131 EP9900131W WO9937308A1 WO 1999037308 A1 WO1999037308 A1 WO 1999037308A1 EP 9900131 W EP9900131 W EP 9900131W WO 9937308 A1 WO9937308 A1 WO 9937308A1
Authority
WO
WIPO (PCT)
Prior art keywords
acarbose
mouth
producing
medicament
active agent
Prior art date
Application number
PCT/EP1999/000131
Other languages
German (de)
English (en)
Inventor
Johanna Berberich
Carola PÖRTNER
Original Assignee
Bayer Aktiengesellschaft
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 Bayer Aktiengesellschaft filed Critical Bayer Aktiengesellschaft
Priority to AU25171/99A priority Critical patent/AU2517199A/en
Publication of WO1999037308A1 publication Critical patent/WO1999037308A1/fr

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7008—Compounds having an amino group directly attached to a carbon atom of the saccharide radical, e.g. D-galactosamine, ranimustine
    • 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
    • A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
    • A61K9/0007—Effervescent
    • 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
    • A61K9/20—Pills, tablets, discs, rods
    • A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms

Definitions

  • Acarbose is the first representative of the class of alpha-glucosidase inhibitors, which, by inhibiting the alpha-glucosidase enzymes, delays the cleavage of sucrose, dextrin and starches in the intestine and thus smoothes the blood sugar level
  • the method according to the invention describes the composition and production of rapidly disintegrating tablets which dissolve in the mouth by contact with the saliva
  • the active ingredient is granulated alone or with parts of the filler with the aid of dry compaction and sieving and compressed to flat wafers on a conventional tablet press
  • Particularly suitable fillers are water-insoluble auxiliaries, for example calcium phosphate or microcrystalline cellulose
  • the proportion of the active ingredient in the formulation is preferably 40-90%, the proportion of fillers and auxiliaries 10-60%.
  • Acarbose, milk sugar and microcrystalline cellulose are mixed in a suitable container.
  • the cross-linked polyvinylpyrollidone and the magnesium stearate are added and mixed again.
  • the ready-to-press mixture is pressed on a conventional tablet press into tablets which have a diameter of 12 mm.
  • the height of the tablets is less than 2 mm.
  • the tablet disintegrates in less than 2 minutes.
  • Acarbose, calcium hydrogen phosphate and sodium bicarbonate are mixed in a suitable container. After dry compaction and subsequent sieving, the citric acid is added.
  • the ready-to-press mixture is compressed in a conventional tablet press to tablets which have a diameter of 12 mm.
  • the height of the tablets is less than 2 mm.
  • the tablet disintegrates in less than 2 minutes.

Landscapes

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

Abstract

L'invention concerne un procédé pour la préparation d'un comprimé se dissolvant rapidement dans la bouche, caractérisé en ce qu'un adjuvant accélérant la dissolution est associé à une forme de comprimé non classique présentant une surface particulièrement grande.
PCT/EP1999/000131 1998-01-24 1999-01-12 Procede pour la preparation d'une forme medicamenteuse se dissolvant rapidement dans la bouche et contenant de l'acarbose comme principe actif WO1999037308A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU25171/99A AU2517199A (en) 1998-01-24 1999-01-12 Method for producing a medicament which quickly dissolves in the mouth and whichcontains acarbose as an active agent

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE1998102700 DE19802700A1 (de) 1998-01-24 1998-01-24 Verfahren zur Herstellung einer im Mund schnell zerfallenden Arzneiform, die als Wirkstoff Acarbose enthält
DE19802700.1 1998-01-24

Publications (1)

Publication Number Publication Date
WO1999037308A1 true WO1999037308A1 (fr) 1999-07-29

Family

ID=7855589

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1999/000131 WO1999037308A1 (fr) 1998-01-24 1999-01-12 Procede pour la preparation d'une forme medicamenteuse se dissolvant rapidement dans la bouche et contenant de l'acarbose comme principe actif

Country Status (3)

Country Link
AU (1) AU2517199A (fr)
DE (1) DE19802700A1 (fr)
WO (1) WO1999037308A1 (fr)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003070227A1 (fr) * 2002-02-21 2003-08-28 Lts Lohmann Therapie-Systeme Ag Preparation pharmaceutique a gout masque se presentant sous la forme de films ou de plaques
WO2011134962A3 (fr) * 2010-04-27 2012-05-03 Bayer Pharma Aktiengesellschaft Comprimé à désintégration orale contenant de l'acarbose
KR101421330B1 (ko) * 2008-12-17 2014-07-18 사토 세이야쿠 가부시키가이샤 붕괴정
CN104013590A (zh) * 2014-05-09 2014-09-03 万特制药(海南)有限公司 一种含阿卡波糖的药物组合物及其制备方法
WO2016097170A1 (fr) * 2014-12-17 2016-06-23 Empros Pharma Ab Composition à libération modifiée d'orlistat et d'acarbose pour le traitement d'obésité et de troubles métaboliques associés
WO2018064795A1 (fr) * 2016-10-05 2018-04-12 Boai Nky Pharmaceuticals Ltd. Compositions de comprimés contenant de la polyvinylpyrrolidone réticulée et leur utilisation dans des applications de boisson

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2367900A (en) * 1998-12-18 2000-07-03 Bayer Corporation Chewable drug delivery system
RU2010128019A (ru) * 2007-12-08 2012-01-20 Байер Шеринг Фарма Акциенгезельшафт (DE) Пероральная диспергируемая таблетка
TR201100150A2 (tr) * 2011-01-06 2012-07-23 Bi̇lgi̇ç Mahmut Suda çözünür dozaj formları
WO2013115745A1 (fr) * 2012-01-31 2013-08-08 Mahmut Bilgic Procédé de préparation de compositions pharmaceutiques (effervescentes) contenant un inhibiteur de l'apha-glucosidase (p. ex. voglibose) et de la metformine

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0226121A2 (fr) * 1985-12-13 1987-06-24 Bayer Ag Composition contenant de l'acarbose très pure
EP0638317A1 (fr) * 1993-08-05 1995-02-15 F. Hoffmann-La Roche Ag Composition pharmaceutique

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0226121A2 (fr) * 1985-12-13 1987-06-24 Bayer Ag Composition contenant de l'acarbose très pure
EP0638317A1 (fr) * 1993-08-05 1995-02-15 F. Hoffmann-La Roche Ag Composition pharmaceutique

Cited By (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2003070227A1 (fr) * 2002-02-21 2003-08-28 Lts Lohmann Therapie-Systeme Ag Preparation pharmaceutique a gout masque se presentant sous la forme de films ou de plaques
US7615235B2 (en) 2002-02-21 2009-11-10 Lts Lohmann Therapie-Systeme Ag Film-shaped or wafer-shaped pharmaceutical preparation with masked taste
KR101421330B1 (ko) * 2008-12-17 2014-07-18 사토 세이야쿠 가부시키가이샤 붕괴정
WO2011134962A3 (fr) * 2010-04-27 2012-05-03 Bayer Pharma Aktiengesellschaft Comprimé à désintégration orale contenant de l'acarbose
CN104013590A (zh) * 2014-05-09 2014-09-03 万特制药(海南)有限公司 一种含阿卡波糖的药物组合物及其制备方法
CN107405309A (zh) * 2014-12-17 2017-11-28 安普洛德制药公司 用于治疗肥胖症和相关代谢紊乱的奥利司他和阿卡波糖的调释组合物
WO2016097170A1 (fr) * 2014-12-17 2016-06-23 Empros Pharma Ab Composition à libération modifiée d'orlistat et d'acarbose pour le traitement d'obésité et de troubles métaboliques associés
CN107405309B (zh) * 2014-12-17 2019-04-16 安普洛德制药公司 用于治疗肥胖症和相关代谢紊乱的奥利司他和阿卡波糖的调释组合物
EA033448B1 (ru) * 2014-12-17 2019-10-31 Empros Pharma Ab Композиция орлистата и акарбозы с модифицированным высвобождением для лечения ожирения и связанных метаболических нарушений
US10561617B2 (en) 2014-12-17 2020-02-18 Empros Pharma Ab Modified release composition of orlistat and acarbose for the treatment of obesity and related metabolic disorders
EP3943076A3 (fr) * 2014-12-17 2022-04-13 Empros Pharma AB Composition à libération modifiée d'orlistat et d'acarbose pour le traitement de l'obésité
US11975105B2 (en) 2014-12-17 2024-05-07 Empros Pharma Ab Modified release composition of orlistat and acarbose for the treatment of obesity and related metabolic disorders
WO2018064795A1 (fr) * 2016-10-05 2018-04-12 Boai Nky Pharmaceuticals Ltd. Compositions de comprimés contenant de la polyvinylpyrrolidone réticulée et leur utilisation dans des applications de boisson
CN109803931A (zh) * 2016-10-05 2019-05-24 博爱新开源医疗科技集团股份有限公司 含有交联聚乙烯吡咯烷酮的片剂组合物及其在饮料应用中的用途
US11535740B2 (en) 2016-10-05 2022-12-27 Boai Nky Medical Holdings Ltd. Tablet compositions containing crosslinked polyvinylpyrrolidone and their use in beverage applications

Also Published As

Publication number Publication date
AU2517199A (en) 1999-08-09
DE19802700A1 (de) 1999-07-29

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