WO2005117899A1 - Composition pharmaceutique comprenant de la tibolone et son procede de production - Google Patents

Composition pharmaceutique comprenant de la tibolone et son procede de production Download PDF

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Publication number
WO2005117899A1
WO2005117899A1 PCT/GB2005/002158 GB2005002158W WO2005117899A1 WO 2005117899 A1 WO2005117899 A1 WO 2005117899A1 GB 2005002158 W GB2005002158 W GB 2005002158W WO 2005117899 A1 WO2005117899 A1 WO 2005117899A1
Authority
WO
WIPO (PCT)
Prior art keywords
cyclodextrin
tibolone
composition
composition according
inclusion complex
Prior art date
Application number
PCT/GB2005/002158
Other languages
English (en)
Inventor
Amar Lulla
Geena Malhotra
Sankarnarayanan Anand
Original Assignee
Cipla Limited
Turner, Craig, Robert
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 Cipla Limited, Turner, Craig, Robert filed Critical Cipla Limited
Publication of WO2005117899A1 publication Critical patent/WO2005117899A1/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
    • A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/57—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of two carbon atoms, e.g. pregnane or progesterone
    • 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
    • A61K9/2004—Excipients; Inactive ingredients
    • A61K9/2022—Organic macromolecular compounds
    • A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/12—Drugs for genital or sexual disorders; Contraceptives for climacteric disorders

Definitions

  • EP 0 707 848 B1 by de Haan, Pieter et al dated January 09, 2002 teaches a solid pharmaceutical composition comprising a water insoluble non-cross linked polymeric excipient capable of binding water and less than 7% by weight of an oil or oily substance having a mean particle size greater than 150 micrometer and a process for the preparation of said solid composition.
  • the document also teaches to include a stabiliser selected from the group consisting of antioxidants, chelating agents and their mixtures. Therefore, the document also claims to have increasing stability with such a formulation.
  • cyclodextrins are typically formed, alpha, beta and gamma cyclodextrin, which contain six, seven and eight glucose molecules in the ring respectively. These can all be used in the present invention.
  • HPBCD Hydroxypropyl beta-cyclodextrin
  • BCD beta-cyclodextrin
  • This modification results in greater solubility of HPBCD and it complexes more readily as compared to BCD.
  • the blend was lubricated with magnesium stearate.
  • Example 1 Comparing Example 1 with 8 from Table 1 and Table 2 it can be understood that using beta-cyclodextrin and hydroxy propyl betacyclodextrin as a part of carrier stabilises tibolone and has better dissolution characteristics than with formulation having 60% starch as a part of carrier.

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  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Preparation (AREA)

Abstract

L'invention concerne une composition pharmaceutique comprenant de la tibolone, un amidon soluble dans l'eau et éventuellement un autre excipient pharmaceutiquement acceptable. Des compositions préférées de l'invention comprennent un complexe d'inclusion de tibolone et un amidon soluble dans l'eau, en particulier de la cyclodextrine. L'invention concerne un procédé pour fabriquer un comprimé comprenant une composition de l'invention. Ce procédé consiste à: mélanger la cyclodextrine de tibolone, un excipient et un désintégrant; effectuer une granulation à l'aide d'un liant; lubrifier les granules à l'aide d'un agent de lubrification; et comprimer les granules pour former les comprimés. Dans un autre mode de réalisation, un procédé de fabrication d'une composition de l'invention consiste à: ajouter un solvant à un prémélange comprenant de la tibolone et une cyclodextrine; mélanger les ingrédients pour permettre au complexe de se former; et formuler ce mélange avec des excipients pharmaceutiquement acceptables pour former une forme dosifiée finale.
PCT/GB2005/002158 2004-06-02 2005-06-01 Composition pharmaceutique comprenant de la tibolone et son procede de production WO2005117899A1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN617MU2004 2004-06-02
IN617/MUM/2004 2004-06-02

Publications (1)

Publication Number Publication Date
WO2005117899A1 true WO2005117899A1 (fr) 2005-12-15

Family

ID=34969120

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GB2005/002158 WO2005117899A1 (fr) 2004-06-02 2005-06-01 Composition pharmaceutique comprenant de la tibolone et son procede de production

Country Status (1)

Country Link
WO (1) WO2005117899A1 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009012733A3 (fr) * 2007-07-25 2009-04-02 Zentiva As Procédé de fabrication de formulation pharmaceutique comprimée contenant de la tibolone
US20100137424A1 (en) * 2007-01-22 2010-06-03 Mostafa Akbarieh Pharmaceutical compositions comprising nebivolol or a nebivolol analogue
CN103083276A (zh) * 2013-01-16 2013-05-08 青岛正大海尔制药有限公司 一种快速崩解的维生素c泡腾片及其制备方法
WO2017191266A1 (fr) 2016-05-04 2017-11-09 Mithra Pharmaceuticals S.A. Utilisation d'alcools de sucre dans des compositions de tibolone
CN113425687A (zh) * 2021-06-02 2021-09-24 京津冀联创药物研究（北京）有限公司 一种中药配方颗粒及其制备方法

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996002277A1 (fr) * 1994-07-20 1996-02-01 Schering Aktiengesellschaft Formes de medicaments solides contenant des clathrates d'hormones sexuelles steroidiennes
WO1998047517A1 (fr) * 1997-04-22 1998-10-29 Akzo Nobel N.V. Compositions stabilisees a base de tibolone
WO2000023460A1 (fr) * 1998-10-16 2000-04-27 Akzo Nobel N.V. COMPOSITION A DEGRE ELEVE DE PURETE RENFERMANT (7α,17α)-17-HYDROXY-7-METHYL-19-NOR-17-PREGN-5(10)-EN-20-YN-3-ONE
WO2003032924A2 (fr) * 2001-10-18 2003-04-24 Ivax Corporation Nouvelles formulations de tibolone
WO2004012712A1 (fr) * 2002-08-02 2004-02-12 Balance Pharmaceuticals, Inc. Methodes et compositions servant au traitement des troubles gynecologiques benins, a la contraception et a l'hormonotherapie de substitution

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996002277A1 (fr) * 1994-07-20 1996-02-01 Schering Aktiengesellschaft Formes de medicaments solides contenant des clathrates d'hormones sexuelles steroidiennes
WO1998047517A1 (fr) * 1997-04-22 1998-10-29 Akzo Nobel N.V. Compositions stabilisees a base de tibolone
WO2000023460A1 (fr) * 1998-10-16 2000-04-27 Akzo Nobel N.V. COMPOSITION A DEGRE ELEVE DE PURETE RENFERMANT (7α,17α)-17-HYDROXY-7-METHYL-19-NOR-17-PREGN-5(10)-EN-20-YN-3-ONE
WO2003032924A2 (fr) * 2001-10-18 2003-04-24 Ivax Corporation Nouvelles formulations de tibolone
WO2004012712A1 (fr) * 2002-08-02 2004-02-12 Balance Pharmaceuticals, Inc. Methodes et compositions servant au traitement des troubles gynecologiques benins, a la contraception et a l'hormonotherapie de substitution

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
THORSTEINN LOFTSSON ET AL: "Pharmaceutical Applications of Cyclodextrins. 1. Drug Solubilization and Stabilization", JOURNAL OF PHARMACEUTICAL SCIENCES, AMERICAN PHARMACEUTICAL ASSOCIATION. WASHINGTON, US, vol. 85, no. 10, October 1996 (1996-10-01), pages 1017 - 1025, XP002080430, ISSN: 0022-3549 *

Cited By (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20100137424A1 (en) * 2007-01-22 2010-06-03 Mostafa Akbarieh Pharmaceutical compositions comprising nebivolol or a nebivolol analogue
US10117939B2 (en) 2007-01-22 2018-11-06 Mylan Pharmaceuticals Ulc Pharmaceutical compositions comprising nebivolol or a nebivolol analogue
WO2009012733A3 (fr) * 2007-07-25 2009-04-02 Zentiva As Procédé de fabrication de formulation pharmaceutique comprimée contenant de la tibolone
EA018755B1 (ru) * 2007-07-25 2013-10-30 Зентива, К.С. Способ изготовления прессованного фармацевтического препарата, содержащего тиболон
CN103083276A (zh) * 2013-01-16 2013-05-08 青岛正大海尔制药有限公司 一种快速崩解的维生素c泡腾片及其制备方法
CN103083276B (zh) * 2013-01-16 2014-07-02 青岛正大海尔制药有限公司 一种快速崩解的维生素c泡腾片及其制备方法
WO2017191266A1 (fr) 2016-05-04 2017-11-09 Mithra Pharmaceuticals S.A. Utilisation d'alcools de sucre dans des compositions de tibolone
US10736907B2 (en) 2016-05-04 2020-08-11 Novalon S.A. Use of sugar-alcohols in tibolone compositions
AU2017260799B2 (en) * 2016-05-04 2022-11-24 Novalon S.A. Use of sugar-alcohols in tibolone compositions
CN113425687A (zh) * 2021-06-02 2021-09-24 京津冀联创药物研究（北京）有限公司 一种中药配方颗粒及其制备方法
CN113425687B (zh) * 2021-06-02 2022-09-16 京津冀联创药物研究（北京）有限公司 一种中药配方颗粒及其制备方法

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