JP2013537530A - ラサギリンシトレートの分散物 - Google Patents
ラサギリンシトレートの分散物 Download PDFInfo
- Publication number
- JP2013537530A JP2013537530A JP2013521947A JP2013521947A JP2013537530A JP 2013537530 A JP2013537530 A JP 2013537530A JP 2013521947 A JP2013521947 A JP 2013521947A JP 2013521947 A JP2013521947 A JP 2013521947A JP 2013537530 A JP2013537530 A JP 2013537530A
- Authority
- JP
- Japan
- Prior art keywords
- rasagiline
- solid dispersion
- mixture
- solvent
- citrate
- 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- Withdrawn
Links
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- 229960000245 rasagiline Drugs 0.000 title claims abstract description 95
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 title claims abstract description 55
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- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 39
- 239000002904 solvent Substances 0.000 claims description 33
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- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical group OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 21
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- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
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- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
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- A61K31/185—Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
- A61K31/205—Amine addition salts of organic acids; Inner quaternary ammonium salts, e.g. betaine, carnitine
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- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1635—Organic macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
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- A—HUMAN NECESSITIES
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- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1652—Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin
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- A—HUMAN NECESSITIES
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- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
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- A61P25/00—Drugs for disorders of the nervous system
- A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
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| US40036910P | 2010-07-27 | 2010-07-27 | |
| US61/400,369 | 2010-07-27 | ||
| PCT/US2011/045569 WO2012015946A1 (en) | 2010-07-27 | 2011-07-27 | Dispersion of rasagiline citrate |
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| JP2013537530A true JP2013537530A (ja) | 2013-10-03 |
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| WO (1) | WO2012015946A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2022507562A (ja) * | 2018-11-16 | 2022-01-18 | 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 | Ｐａｒｐインヒビタを含む医薬組成物 |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US8809310B2 (en) * | 2006-02-21 | 2014-08-19 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of multiple system atrophy |
| WO2007117431A2 (en) | 2006-04-03 | 2007-10-18 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of restless legs syndrome |
| CN101557706B (zh) * | 2006-12-14 | 2013-08-07 | 泰华制药工业有限公司 | 雷沙吉兰碱结晶固体 |
| EP1987816A1 (de) * | 2007-04-30 | 2008-11-05 | Ratiopharm GmbH | Adsorbate eines Rasagilinsalzes mit einem wasserlöslichen Hilfsstoff |
| CA2711817A1 (en) * | 2008-01-11 | 2009-07-16 | Teva Pharmaceutical Industries Ltd. | Rasagiline formulations, their preparation and use |
| WO2009151594A1 (en) * | 2008-06-10 | 2009-12-17 | Teva Pharmaceutical Industries, Ltd. | Rasagiline soft gelatin capsules |
| PT2451771E (pt) | 2009-07-09 | 2014-09-19 | Ratiopharm Gmbh | Sais de rasagilina e suas preparações farmacêuticas |
| AU2010304755A1 (en) * | 2009-10-09 | 2012-05-24 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of Progressive Supranuclear Palsy |
| CA2785501A1 (en) * | 2009-12-22 | 2011-07-21 | Teva Pharmaceutical Industries Ltd. | 3-keto-n-propargyl-1-aminoindan |
| EP2598136A4 (en) | 2010-07-27 | 2015-03-25 | Teva Pharma | DISPERSIONS OF RASAGILINE CITRATE |
| RU2587330C2 (ru) | 2010-07-27 | 2016-06-20 | Тева Фармасьютикал Индастриз Лтд. | Применение разагилина для лечения обонятельной дисфункции |
| EA201490760A1 (ru) | 2011-10-10 | 2014-09-30 | Тева Фармасьютикал Индастриз Лтд. | R(+)-n-метилпропаргиламиноиндан |
| EA201490761A1 (ru) | 2011-10-10 | 2014-11-28 | Тева Фармасьютикал Индастриз Лтд. | R(+)-n-формилпропаргиламиноиндан |
| AR092168A1 (es) | 2012-08-17 | 2015-03-25 | Teva Pharma | Formulaciones parenterales de rasagilina |
| WO2022162612A1 (en) | 2021-01-30 | 2022-08-04 | Intas Pharmaceuticals Ltd. | An orodispersible pharmaceutical solid dosage form of rasagiline |
| EP4035654A1 (en) | 2021-01-30 | 2022-08-03 | Intas Pharmaceuticals Limited | An orodispersible pharmaceutical solid dosage form of rasagiline |
Family Cites Families (39)
| Publication number | Priority date | Publication date | Assignee | Title |
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| US5744500A (en) | 1990-01-03 | 1998-04-28 | Teva Pharmaceutical Industries, Ltd. | Use of R-enantiomer of N-propargyl-1-aminoindan, salts, and compositions thereof |
| IL92952A (en) | 1990-01-03 | 1994-06-24 | Teva Pharma | R-enantiomers of n-propargyl-1-aminoindan compounds, their preparation and pharmaceutical compositions containing them |
| IL112819A (en) | 1991-10-16 | 2001-11-25 | Teva Pharma | Fluorinated 1-aminoindan compounds and a process for their preparation |
| IL115357A (en) | 1995-09-20 | 2000-01-31 | Teva Pharma | Stable compositions containing N-propargyl-1-aminoindan and polyhydric alcohols |
| IL118836A (en) | 1996-07-11 | 2001-01-11 | Teva Pharma | Pharmaceutical compositions comprising s-(-)-n-propargyl-1-aminoindan |
| WO1998027055A1 (en) | 1996-12-18 | 1998-06-25 | Teva Pharmaceutical Industries, Ltd. | Aminoindan derivatives |
| US7396860B2 (en) | 2002-11-15 | 2008-07-08 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline with or without riluzole to treat amyotrophic lateral sclerosis |
| AU2004294674B2 (en) * | 2003-12-01 | 2009-02-26 | Recordati Ireland Limited | Pharmaceutical compositions comprising lercanidipine |
| AU2005269416B2 (en) | 2004-07-26 | 2011-07-28 | Teva Pharmaceutical Industries, Ltd. | Pharmaceutical dosage forms including rasagiline |
| ZA200704917B (en) | 2004-11-24 | 2008-11-26 | Teva Pharma | Rasagiline orally disintegrating compositions |
| CA2600011C (en) | 2005-02-23 | 2015-11-10 | Teva Pharmaceutical Industries Ltd. | Rasagiline formulations of improved content uniformity |
| CA2630037C (en) | 2005-11-17 | 2015-03-31 | Teva Pharmaceutical Industries Ltd. | Methods for isolating propargylated aminoindans |
| US7572834B1 (en) | 2005-12-06 | 2009-08-11 | Teva Pharmaceutical Industries, Ltd. | Rasagiline formulations and processes for their preparation |
| US8809310B2 (en) | 2006-02-21 | 2014-08-19 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of multiple system atrophy |
| CN101032474B (zh) | 2006-03-06 | 2011-02-16 | 重庆医药工业研究院有限责任公司 | 一种治疗或预防神经系统疾病的雷沙吉兰透皮贴片及其制备方法 |
| WO2007117431A2 (en) | 2006-04-03 | 2007-10-18 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of restless legs syndrome |
| EP1892233A1 (de) | 2006-08-18 | 2008-02-27 | Ratiopharm GmbH | Neue Salze des Wirkstoffs Rasagilin |
| ZA200903904B (en) | 2006-12-14 | 2010-08-25 | Teva Pharma | Tannate salt of rasagiline |
| CN101557706B (zh) | 2006-12-14 | 2013-08-07 | 泰华制药工业有限公司 | 雷沙吉兰碱结晶固体 |
| EP1987816A1 (de) | 2007-04-30 | 2008-11-05 | Ratiopharm GmbH | Adsorbate eines Rasagilinsalzes mit einem wasserlöslichen Hilfsstoff |
| JP2010538067A (ja) | 2007-09-05 | 2010-12-09 | テバ ファーマシューティカル インダストリーズ リミティド | ラサギリンを使用する緑内障の治療方法 |
| US8188149B2 (en) | 2007-09-17 | 2012-05-29 | Teva Pharmaceutical Industries, Ltd. | Use of R(+)-N-propargy1-1-aminoindan to treat or prevent hearing loss |
| CA2711817A1 (en) | 2008-01-11 | 2009-07-16 | Teva Pharmaceutical Industries Ltd. | Rasagiline formulations, their preparation and use |
| WO2009151594A1 (en) | 2008-06-10 | 2009-12-17 | Teva Pharmaceutical Industries, Ltd. | Rasagiline soft gelatin capsules |
| US20090312436A1 (en) | 2008-06-13 | 2009-12-17 | Ruth Levy | Rasagiline for parkinson's disease modification |
| AU2009260733B2 (en) | 2008-06-19 | 2015-01-29 | Teva Pharmaceutical Industries, Ltd. | Process for purifying rasagiline base |
| JP2011524907A (ja) | 2008-06-19 | 2011-09-08 | テバ ファーマシューティカル インダストリーズ リミティド | 固体ラサギリン塩基を調製および乾燥する方法 |
| DE102008064061A1 (de) * | 2008-12-19 | 2010-06-24 | Ratiopharm Gmbh | Feste Zusammensetzung mit dem Wirkstoff Rasagilin |
| EP2218444A3 (en) * | 2009-01-23 | 2010-08-25 | Teva Pharmaceutical Industries, Ltd. | Delayed release rasagiline formulation |
| US8080584B2 (en) | 2009-01-23 | 2011-12-20 | Teva Pharmaceuticals Industries, Ltd. | Delayed release rasagiline citrate formulation |
| PT2451771E (pt) | 2009-07-09 | 2014-09-19 | Ratiopharm Gmbh | Sais de rasagilina e suas preparações farmacêuticas |
| AU2010304755A1 (en) | 2009-10-09 | 2012-05-24 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of Progressive Supranuclear Palsy |
| CA2785501A1 (en) | 2009-12-22 | 2011-07-21 | Teva Pharmaceutical Industries Ltd. | 3-keto-n-propargyl-1-aminoindan |
| RU2587330C2 (ru) | 2010-07-27 | 2016-06-20 | Тева Фармасьютикал Индастриз Лтд. | Применение разагилина для лечения обонятельной дисфункции |
| EP2598136A4 (en) | 2010-07-27 | 2015-03-25 | Teva Pharma | DISPERSIONS OF RASAGILINE CITRATE |
| WO2012058219A2 (en) | 2010-10-26 | 2012-05-03 | Teva Pharmaceutical Industries Ltd. | Deuterium enriched rasagiline |
| EA201490760A1 (ru) | 2011-10-10 | 2014-09-30 | Тева Фармасьютикал Индастриз Лтд. | R(+)-n-метилпропаргиламиноиндан |
| BR112014008550A2 (pt) | 2011-10-10 | 2017-04-18 | Teva Pharma | citramida rasagilina |
| EA201490761A1 (ru) | 2011-10-10 | 2014-11-28 | Тева Фармасьютикал Индастриз Лтд. | R(+)-n-формилпропаргиламиноиндан |
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- 2011-07-27 EP EP11813128.3A patent/EP2598136A4/en not_active Withdrawn
- 2011-07-27 WO PCT/US2011/045569 patent/WO2012015946A1/en not_active Ceased
- 2011-07-27 RU RU2013108256/15A patent/RU2013108256A/ru not_active Application Discontinuation
- 2011-07-27 JP JP2013521947A patent/JP2013537530A/ja not_active Withdrawn
- 2011-07-27 CA CA2806737A patent/CA2806737A1/en not_active Abandoned
- 2011-07-27 US US13/192,082 patent/US8691872B2/en not_active Expired - Fee Related
- 2011-07-27 AU AU2011282716A patent/AU2011282716A1/en not_active Abandoned
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2014
- 2014-03-10 US US14/203,209 patent/US20140194510A1/en not_active Abandoned
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2022507562A (ja) * | 2018-11-16 | 2022-01-18 | 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 | Ｐａｒｐインヒビタを含む医薬組成物 |
| JP7469304B2 (ja) | 2018-11-16 | 2024-04-16 | 江▲蘇▼恒瑞医▲薬▼股▲フン▼有限公司 | Ｐａｒｐインヒビタを含む医薬組成物 |
| US12318385B2 (en) | 2018-11-16 | 2025-06-03 | Jiangsu Hengrui Medicine Co., Ltd. | Pharmaceutical composition comprising PARP inhibitors |
Also Published As
| Publication number | Publication date |
|---|---|
| EP2598136A1 (en) | 2013-06-05 |
| EP2598136A4 (en) | 2015-03-25 |
| WO2012015946A8 (en) | 2013-01-31 |
| AU2011282716A1 (en) | 2013-03-14 |
| US20140194510A1 (en) | 2014-07-10 |
| CA2806737A1 (en) | 2012-02-02 |
| US8691872B2 (en) | 2014-04-08 |
| WO2012015946A1 (en) | 2012-02-02 |
| US20120059058A1 (en) | 2012-03-08 |
| RU2013108256A (ru) | 2014-09-10 |
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|---|---|---|---|
| A521 | Request for written amendment filed |
Free format text: JAPANESE INTERMEDIATE CODE: A523 Effective date: 20140728 |
|
| A621 | Written request for application examination |
Free format text: JAPANESE INTERMEDIATE CODE: A621 Effective date: 20140728 |
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| A761 | Written withdrawal of application |
Free format text: JAPANESE INTERMEDIATE CODE: A761 Effective date: 20150622 |