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- Withdrawn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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- A—HUMAN NECESSITIES
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- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/13—Amines
- A61K31/135—Amines having aromatic rings, e.g. ketamine, nortriptyline
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K31/00—Medicinal preparations containing organic active ingredients
- 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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- A—HUMAN NECESSITIES
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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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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
- A61K9/16—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
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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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- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- 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
- A61K9/19—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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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- 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
- A61P25/16—Anti-Parkinson drugs
Landscapes
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- Life Sciences & Earth Sciences (AREA)
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- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
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- Psychology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
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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 |
Publications (2)
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| JP2013537530A true JP2013537530A (ja) | 2013-10-03 |
| JP2013537530A5 JP2013537530A5 (enExample) | 2014-09-18 |
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| JP2013521947A Withdrawn JP2013537530A (ja) | 2010-07-27 | 2011-07-27 | ラサギリンシトレートの分散物 |
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| US (2) | US8691872B2 (enExample) |
| EP (1) | EP2598136A4 (enExample) |
| JP (1) | JP2013537530A (enExample) |
| AU (1) | AU2011282716A1 (enExample) |
| CA (1) | CA2806737A1 (enExample) |
| RU (1) | RU2013108256A (enExample) |
| 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 |
|---|---|---|---|---|
| JP5701485B2 (ja) * | 2006-02-21 | 2015-04-15 | 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 | 多系統萎縮症の治療のためのラサギリンの使用 |
| CA2646250A1 (en) * | 2006-04-03 | 2007-10-18 | Teva Pharmaceutical Industries Ltd. | Use of rasagiline for the treatment of restless legs syndrome |
| ZA200903903B (en) * | 2006-12-14 | 2010-08-25 | Teva Pharma | Crystalline solid rasagiline base |
| EP1987816A1 (de) * | 2007-04-30 | 2008-11-05 | Ratiopharm GmbH | Adsorbate eines Rasagilinsalzes mit einem wasserlöslichen Hilfsstoff |
| US20090181086A1 (en) * | 2008-01-11 | 2009-07-16 | Muhammad Safadi | Rasagiline formulations, their preparation and use |
| WO2009151594A1 (en) * | 2008-06-10 | 2009-12-17 | Teva Pharmaceutical Industries, Ltd. | Rasagiline soft gelatin capsules |
| SI2451771T1 (sl) | 2009-07-09 | 2014-10-30 | Ratiopharm Gmbh | Soli rasagilina in njihovi farmacevtski pripravki |
| JP2013507352A (ja) * | 2009-10-09 | 2013-03-04 | 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 | 進行性核上性麻痺の治療のためのラサギリンの使用 |
| AU2010341499A1 (en) * | 2009-12-22 | 2012-08-09 | Teva Pharmaceutical Industries Ltd. | 3-keto-N-propargyl-1-aminoindan |
| AU2011282716A1 (en) | 2010-07-27 | 2013-03-14 | Teva Pharmaceutical Industries Ltd. | Dispersions of rasagiline citrate |
| CA2806740A1 (en) | 2010-07-27 | 2012-02-02 | Teva Pharmaceutical Industries Ltd. | Use of rasagiline for the treatment of olfactory dysfunction |
| WO2013055687A2 (en) | 2011-10-10 | 2013-04-18 | Teva Pharmaceutical Industries Ltd. | R(+)-n-formyl-propargyl-aminoindan |
| JP2014534197A (ja) | 2011-10-10 | 2014-12-18 | 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 | Ｒ（＋）−ｎ−メチル−プロパルギルアミノインダン |
| US9308182B2 (en) | 2012-08-17 | 2016-04-12 | Teva Pharmaceutical Industries, Ltd. | Parenteral formulations of rasagiline |
| EP4284336A1 (en) | 2021-01-30 | 2023-12-06 | 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 |
|---|---|---|---|---|
| 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 |
| 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 |
| IL99759A (en) | 1991-10-16 | 1997-06-10 | Teva Pharma | Mono-fluorinated derivatives of n-propargyl-1-aminoindan, their preparation and pharmaceutical compositions containing them |
| 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 |
| DE69738275T2 (de) | 1996-12-18 | 2008-08-28 | Teva Pharmaceutical Industries Ltd. | Aminoindanderivate |
| SI1567152T1 (sl) | 2002-11-15 | 2013-10-30 | Teva Pharmaceutical Industries Ltd. | Uporaba rasagilina z riluzolom za zdravljenje amiotrofične lateralne skleroze |
| KR20060125824A (ko) * | 2003-12-01 | 2006-12-06 | 라이프사이클 파마 에이/에스 | 레르카니디핀을 포함한 약학적 조성물 |
| WO2006014973A2 (en) | 2004-07-26 | 2006-02-09 | Teva Pharmaceutical Industries, Ltd. | Pharmaceutical dosage forms including rasagiline |
| US20090111892A1 (en) | 2004-11-24 | 2009-04-30 | Shulamit Patashnik | Rasagiline Orally Disintegrating Compositions |
| CA2901244A1 (en) | 2005-02-23 | 2006-08-31 | Teva Pharmaceutical Industries, Ltd. | Rasagiline formulations of improved content uniformity |
| EP1954667B1 (en) | 2005-11-17 | 2017-02-08 | 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 |
| JP5701485B2 (ja) | 2006-02-21 | 2015-04-15 | 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 | 多系統萎縮症の治療のためのラサギリンの使用 |
| 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 |
| CA2646250A1 (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 |
| JP5356248B2 (ja) | 2006-12-14 | 2013-12-04 | 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 | ラサギリンのタンニン酸塩 |
| ZA200903903B (en) | 2006-12-14 | 2010-08-25 | Teva Pharma | Crystalline solid rasagiline base |
| EP1987816A1 (de) | 2007-04-30 | 2008-11-05 | Ratiopharm GmbH | Adsorbate eines Rasagilinsalzes mit einem wasserlöslichen Hilfsstoff |
| AU2008296908B2 (en) | 2007-09-05 | 2014-01-09 | Teva Pharmaceutical Industries, Ltd. | Method of treating glaucoma using rasagiline |
| 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 |
| US20090181086A1 (en) | 2008-01-11 | 2009-07-16 | Muhammad Safadi | Rasagiline formulations, their preparation and use |
| WO2009151594A1 (en) | 2008-06-10 | 2009-12-17 | Teva Pharmaceutical Industries, Ltd. | Rasagiline soft gelatin capsules |
| JP2011522892A (ja) * | 2008-06-13 | 2011-08-04 | 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 | パーキンソン病緩和のためのラサギリン |
| AU2009260733B2 (en) | 2008-06-19 | 2015-01-29 | Teva Pharmaceutical Industries, Ltd. | Process for purifying rasagiline base |
| MX2010013875A (es) | 2008-06-19 | 2011-01-20 | Teva Pharma | Proceso para preparar y secar base de rasagilina solida. |
| 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 |
| US20100189790A1 (en) | 2009-01-23 | 2010-07-29 | Teva Pharmaceutical Industries, Ltd. | Delayed release rasagiline formulation |
| SI2451771T1 (sl) | 2009-07-09 | 2014-10-30 | Ratiopharm Gmbh | Soli rasagilina in njihovi farmacevtski pripravki |
| JP2013507352A (ja) | 2009-10-09 | 2013-03-04 | 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 | 進行性核上性麻痺の治療のためのラサギリンの使用 |
| AU2010341499A1 (en) | 2009-12-22 | 2012-08-09 | Teva Pharmaceutical Industries Ltd. | 3-keto-N-propargyl-1-aminoindan |
| CA2806740A1 (en) | 2010-07-27 | 2012-02-02 | Teva Pharmaceutical Industries Ltd. | Use of rasagiline for the treatment of olfactory dysfunction |
| AU2011282716A1 (en) | 2010-07-27 | 2013-03-14 | Teva Pharmaceutical Industries Ltd. | Dispersions of rasagiline citrate |
| US20120101168A1 (en) | 2010-10-26 | 2012-04-26 | Eliezer Bahar | Deuterium enriched rasagiline |
| WO2013055687A2 (en) | 2011-10-10 | 2013-04-18 | Teva Pharmaceutical Industries Ltd. | R(+)-n-formyl-propargyl-aminoindan |
| CN103857389A (zh) | 2011-10-10 | 2014-06-11 | 泰华制药工业有限公司 | 雷沙吉兰柠檬酰胺 |
| JP2014534197A (ja) | 2011-10-10 | 2014-12-18 | 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 | Ｒ（＋）−ｎ−メチル−プロパルギルアミノインダン |
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- 2011-07-27 AU AU2011282716A patent/AU2011282716A1/en not_active Abandoned
- 2011-07-27 EP EP11813128.3A patent/EP2598136A4/en not_active Withdrawn
- 2011-07-27 CA CA2806737A patent/CA2806737A1/en not_active Abandoned
- 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 WO PCT/US2011/045569 patent/WO2012015946A1/en not_active Ceased
- 2011-07-27 US US13/192,082 patent/US8691872B2/en not_active Expired - Fee Related
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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 |
|---|---|
| US8691872B2 (en) | 2014-04-08 |
| WO2012015946A1 (en) | 2012-02-02 |
| EP2598136A4 (en) | 2015-03-25 |
| AU2011282716A1 (en) | 2013-03-14 |
| RU2013108256A (ru) | 2014-09-10 |
| CA2806737A1 (en) | 2012-02-02 |
| US20120059058A1 (en) | 2012-03-08 |
| EP2598136A1 (en) | 2013-06-05 |
| WO2012015946A8 (en) | 2013-01-31 |
| US20140194510A1 (en) | 2014-07-10 |
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