JP2013537530A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2013537530A5 JP2013537530A5 JP2013521947A JP2013521947A JP2013537530A5 JP 2013537530 A5 JP2013537530 A5 JP 2013537530A5 JP 2013521947 A JP2013521947 A JP 2013521947A JP 2013521947 A JP2013521947 A JP 2013521947A JP 2013537530 A5 JP2013537530 A5 JP 2013537530A5
- Authority
- JP
- Japan
- Prior art keywords
- rasagiline
- solvent
- mixture
- solid dispersion
- der
- 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- Withdrawn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
- 238000000034 method Methods 0.000 claims description 34
- RUOKEQAAGRXIBM-GFCCVEGCSA-N rasagiline Chemical compound C1=CC=C2[C@H](NCC#C)CCC2=C1 RUOKEQAAGRXIBM-GFCCVEGCSA-N 0.000 claims description 30
- 229960000245 rasagiline Drugs 0.000 claims description 30
- 239000007962 solid dispersion Substances 0.000 claims description 27
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical group OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 claims description 24
- 239000002904 solvent Substances 0.000 claims description 24
- 239000000203 mixture Substances 0.000 claims description 22
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 claims description 20
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 18
- 229920003168 pharmaceutical polymer Polymers 0.000 claims description 16
- KRKNYBCHXYNGOX-UHFFFAOYSA-K Citrate Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims description 15
- 150000003839 salts Chemical class 0.000 claims description 14
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims description 12
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 12
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 12
- 238000004519 manufacturing process Methods 0.000 claims description 7
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 6
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 6
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 6
- RYHBNJHYFVUHQT-UHFFFAOYSA-N 1,4-Dioxane Chemical compound C1COCCO1 RYHBNJHYFVUHQT-UHFFFAOYSA-N 0.000 claims description 4
- 229920001577 copolymer Polymers 0.000 claims description 4
- 239000012458 free base Substances 0.000 claims description 4
- 238000004108 freeze drying Methods 0.000 claims description 4
- 238000000227 grinding Methods 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 238000002390 rotary evaporation Methods 0.000 claims description 4
- 238000001238 wet grinding Methods 0.000 claims description 4
- 229920003132 hydroxypropyl methylcellulose phthalate Polymers 0.000 claims description 3
- 239000001267 polyvinylpyrrolidone Substances 0.000 claims description 3
- 208000018737 Parkinson disease Diseases 0.000 claims description 2
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 2
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 2
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 2
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 2
- 229940031704 hydroxypropyl methylcellulose phthalate Drugs 0.000 claims description 2
- 229920000639 hydroxypropylmethylcellulose acetate succinate Polymers 0.000 claims description 2
- 239000008247 solid mixture Substances 0.000 claims description 2
- 238000009837 dry grinding Methods 0.000 claims 2
- JIGUQPWFLRLWPJ-UHFFFAOYSA-N Ethyl acrylate Chemical compound CCOC(=O)C=C JIGUQPWFLRLWPJ-UHFFFAOYSA-N 0.000 claims 1
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- PNJWIWWMYCMZRO-UHFFFAOYSA-N pent‐4‐en‐2‐one Natural products CC(=O)CC=C PNJWIWWMYCMZRO-UHFFFAOYSA-N 0.000 claims 1
- 239000006185 dispersion Substances 0.000 description 3
- 229920003139 Eudragit® L 100 Polymers 0.000 description 2
- GDCRSXZBSIRSFR-UHFFFAOYSA-N ethyl prop-2-enoate;2-methylprop-2-enoic acid Chemical compound CC(=C)C(O)=O.CCOC(=O)C=C GDCRSXZBSIRSFR-UHFFFAOYSA-N 0.000 description 2
- 238000010298 pulverizing process Methods 0.000 description 2
- FYUWIEKAVLOHSE-UHFFFAOYSA-N ethenyl acetate;1-ethenylpyrrolidin-2-one Chemical compound CC(=O)OC=C.C=CN1CCCC1=O FYUWIEKAVLOHSE-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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)
| Publication Number | Publication Date |
|---|---|
| JP2013537530A JP2013537530A (ja) | 2013-10-03 |
| JP2013537530A5 true JP2013537530A5 (cg-RX-API-DMAC7.html) | 2014-09-18 |
Family
ID=45530490
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013521947A Withdrawn JP2013537530A (ja) | 2010-07-27 | 2011-07-27 | ラサギリンシトレートの分散物 |
Country Status (7)
| Country | Link |
|---|---|
| US (2) | US8691872B2 (cg-RX-API-DMAC7.html) |
| EP (1) | EP2598136A4 (cg-RX-API-DMAC7.html) |
| JP (1) | JP2013537530A (cg-RX-API-DMAC7.html) |
| AU (1) | AU2011282716A1 (cg-RX-API-DMAC7.html) |
| CA (1) | CA2806737A1 (cg-RX-API-DMAC7.html) |
| RU (1) | RU2013108256A (cg-RX-API-DMAC7.html) |
| WO (1) | WO2012015946A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2007217349B9 (en) * | 2006-02-21 | 2013-06-27 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline for the treatment of Multiple System Atrophy |
| EP2007369A4 (en) | 2006-04-03 | 2009-07-01 | Teva Pharma | USE OF RASAGILINE FOR THE TREATMENT OF LEG SYNDROME WITHOUT REST |
| US7750051B2 (en) * | 2006-12-14 | 2010-07-06 | Teva Pharmaceutical Industries, Ltd. | Crystalline solid rasagiline base |
| EP1987816A1 (de) * | 2007-04-30 | 2008-11-05 | Ratiopharm GmbH | Adsorbate eines Rasagilinsalzes mit einem wasserlöslichen Hilfsstoff |
| MX2010007601A (es) * | 2008-01-11 | 2010-08-03 | Teva Pharma | Formulaciones de rasagilina, su preparacion y uso. |
| US20100008983A1 (en) * | 2008-06-10 | 2010-01-14 | Muhammad Safadi | Rasagiline soft gelatin capsules |
| DK2451771T3 (da) | 2009-07-09 | 2014-09-08 | Ratiopharm Gmbh | Salte af rasagilin og farmaceutiske fremstillingsmåder heraf |
| 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 |
| CA2785501A1 (en) * | 2009-12-22 | 2011-07-21 | Teva Pharmaceutical Industries Ltd. | 3-keto-n-propargyl-1-aminoindan |
| EP2603212A4 (en) | 2010-07-27 | 2014-01-08 | Teva Pharma | USE OF RASAGILINE FOR THE TREATMENT OF SMOKING DISORDER |
| JP2013537530A (ja) | 2010-07-27 | 2013-10-03 | 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 | ラサギリンシトレートの分散物 |
| BR112014008555A2 (pt) | 2011-10-10 | 2017-04-18 | Teva Pharma | r(+)-n-formil-propargil-aminoindano |
| EA201490760A1 (ru) | 2011-10-10 | 2014-09-30 | Тева Фармасьютикал Индастриз Лтд. | R(+)-n-метилпропаргиламиноиндан |
| EP2884972A4 (en) | 2012-08-17 | 2016-05-11 | Teva Pharma | PARENTERAL FORMULATION OF RASAGILINE |
| WO2020098774A1 (zh) | 2018-11-16 | 2020-05-22 | 江苏恒瑞医药股份有限公司 | 一种包含parp抑制剂的药物组合物 |
| 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 |
|---|---|---|---|---|
| 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 |
| 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 |
| PT966435E (pt) | 1996-12-18 | 2005-06-30 | Yissum Res Dev Co | Derivados aminoindano |
| US7396860B2 (en) | 2002-11-15 | 2008-07-08 | Teva Pharmaceutical Industries, Ltd. | Use of rasagiline with or without riluzole to treat amyotrophic lateral sclerosis |
| US20070105912A1 (en) * | 2003-12-01 | 2007-05-10 | Per Holm | Pharmaceutical compositions comprising lercanidipine |
| 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 |
| RU2404746C2 (ru) | 2005-02-23 | 2010-11-27 | Тева Фармасьютикал Индастриз, Лтд. | Композиции разагилина с улучшенной однородностью содержимого |
| CN101622225B (zh) | 2005-11-17 | 2015-04-15 | 泰华制药工业有限公司 | 炔丙基氨基茚分离方法 |
| US7572834B1 (en) | 2005-12-06 | 2009-08-11 | Teva Pharmaceutical Industries, Ltd. | Rasagiline formulations and processes for their preparation |
| AU2007217349B9 (en) | 2006-02-21 | 2013-06-27 | 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 |
| EP2007369A4 (en) | 2006-04-03 | 2009-07-01 | Teva Pharma | USE OF RASAGILINE FOR THE TREATMENT OF LEG SYNDROME WITHOUT REST |
| EP1892233A1 (de) | 2006-08-18 | 2008-02-27 | Ratiopharm GmbH | Neue Salze des Wirkstoffs Rasagilin |
| US7750051B2 (en) | 2006-12-14 | 2010-07-06 | Teva Pharmaceutical Industries, Ltd. | Crystalline solid rasagiline base |
| CA2672452C (en) | 2006-12-14 | 2012-07-03 | Teva Pharmaceutical Industries Ltd. | Tannate salt of rasagiline |
| EP1987816A1 (de) | 2007-04-30 | 2008-11-05 | Ratiopharm GmbH | Adsorbate eines Rasagilinsalzes mit einem wasserlöslichen Hilfsstoff |
| EP2194780A4 (en) | 2007-09-05 | 2010-10-27 | Teva Pharma | METHOD FOR TREATING GLAUCOMA BY 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 |
| MX2010007601A (es) | 2008-01-11 | 2010-08-03 | Teva Pharma | Formulaciones de rasagilina, su preparacion y uso. |
| US20100008983A1 (en) | 2008-06-10 | 2010-01-14 | Muhammad Safadi | Rasagiline soft gelatin capsules |
| BRPI0909894A2 (pt) | 2008-06-13 | 2015-07-28 | Teva Pharma | "método de redução da velocidade de progressão de mal de parkinson em um paciente com mal de parkinson em estágio inicial, método de redução da velocidade de progressão de mal de parkinson, método de atraso da necessidade de terapia antiparkinsoniana sintomática em um paciente de mal de parkinson em estágio inicial, método de redução do risco de um paciente com mal de parkinson que necessita de terapia antiparkinsoniana, método de redução do declínio funcional de um paciente com mal de parkinson em estágio inicial, método de redução do declínio funcional em um paciente com mal de parkinson, método de tratamento de um paciente que exibe sinais iniciais de mal de parkinson, método de redução da fadiga em um paciente com mal de parkinson em estágio inicial, método de redução da velocidade de progressão clínica e tratamento de sintomas de mal de parkinson em um paciente com mal de parkinson, rasagilina ou um sal farmaceuticamente aceitável de rasagilina, composição farmacêutica. |
| US7968749B2 (en) | 2008-06-19 | 2011-06-28 | Teva Pharmaceutical Industries, Ltd. | Process for preparing and drying solid rasagiline base |
| US8334409B2 (en) | 2008-06-19 | 2012-12-18 | Teva Pharmaceutical Industries, Ltd. | Process for purifying rasagiline base |
| 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 |
| US20100189791A1 (en) | 2009-01-23 | 2010-07-29 | Teva Pharmaceutical Industries, Ltd. | Delayed release rasagiline malate formulation |
| DK2451771T3 (da) | 2009-07-09 | 2014-09-08 | Ratiopharm Gmbh | Salte af rasagilin og farmaceutiske fremstillingsmåder heraf |
| 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 |
| CA2785501A1 (en) | 2009-12-22 | 2011-07-21 | Teva Pharmaceutical Industries Ltd. | 3-keto-n-propargyl-1-aminoindan |
| EP2603212A4 (en) | 2010-07-27 | 2014-01-08 | Teva Pharma | USE OF RASAGILINE FOR THE TREATMENT OF SMOKING DISORDER |
| JP2013537530A (ja) | 2010-07-27 | 2013-10-03 | 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 | ラサギリンシトレートの分散物 |
| EP2632254A4 (en) | 2010-10-26 | 2015-08-05 | Teva Pharma | RASAGILIN ENRICHED IN DEUTERIUM |
| EA201490760A1 (ru) | 2011-10-10 | 2014-09-30 | Тева Фармасьютикал Индастриз Лтд. | R(+)-n-метилпропаргиламиноиндан |
| BR112014008555A2 (pt) | 2011-10-10 | 2017-04-18 | Teva Pharma | r(+)-n-formil-propargil-aminoindano |
| MX2014004196A (es) | 2011-10-10 | 2014-05-28 | Teva Pharma | Citramida de rasagilina. |
-
2011
- 2011-07-27 JP JP2013521947A patent/JP2013537530A/ja not_active Withdrawn
- 2011-07-27 AU AU2011282716A patent/AU2011282716A1/en not_active Abandoned
- 2011-07-27 US US13/192,082 patent/US8691872B2/en not_active Expired - Fee Related
- 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 CA CA2806737A patent/CA2806737A1/en not_active Abandoned
-
2014
- 2014-03-10 US US14/203,209 patent/US20140194510A1/en not_active Abandoned
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2013537530A5 (cg-RX-API-DMAC7.html) | ||
| JP2012515775A5 (cg-RX-API-DMAC7.html) | ||
| Yan et al. | Preparation and evaluation of taste-masked donepezil hydrochloride orally disintegrating tablets | |
| RU2013108256A (ru) | Дисперсии цитрата разагилина | |
| CN105832678A (zh) | 生物利用度提高的包含难溶性药物的微球及其制备方法 | |
| JP6148252B2 (ja) | 新規配合剤 | |
| WO2019151405A1 (ja) | 錠剤及びその製造方法 | |
| KR20170083509A (ko) | 바레니클린 또는 이의 약학적으로 허용가능한 염을 함유하는 맛 차폐된 구강 투여용 약학 제제 | |
| KR20070085894A (ko) | 핵산-함유 점착성 활성 성분을 포함한 다입자 투여 형태,및 이러한 투여 형태의 제조 방법 | |
| JP2019524724A (ja) | テコビリマットの経口用医薬組成物及びその調製法 | |
| CN102406939B (zh) | 提高难溶性药物溶解性能以提高生物利用度的方法 | |
| CN105640913B (zh) | 一种奥美沙坦酯片及其制备方法 | |
| ES2417330T3 (es) | Minicomprimidos farmacéuticos para la liberación sostenida de acetato de flecainida | |
| CN102028672B (zh) | 微孔海绵状药膜制剂及其制备方法 | |
| CN103735525A (zh) | 一种达泊西汀片剂及制备方法 | |
| JP5674671B2 (ja) | 塩酸シプロヘプタジン軟膏剤及びその製造方法 | |
| CN104706604A (zh) | 一种吡仑帕奈冻干口崩片及其制备方法 | |
| TW200822925A (en) | Amlodipine-contained particle and orally disintegrating tablet | |
| NO341321B1 (no) | Preparat for oral administrering av tamsulosin-hydroklorid og granul med kontrollert frigivelsesformulering omfattende det samme | |
| CN101854921B (zh) | 用于口服施用ppi的药物制剂 | |
| JP5297194B2 (ja) | 初期溶解率が改善されたプランルカスト固体分散体の薬剤学的組成物およびその製造方法 | |
| US20060286165A1 (en) | Taste-masked pharmaceutical particle, the preparation and use thereof | |
| CN103099803B (zh) | 一种增溶与同步溶出银杏内酯的方法 | |
| WO2012063498A2 (ja) | 新規なエキセメスタン固体分散体 | |
| WO2014006571A2 (en) | Extended-release pharmaceutical dosage forms of carbidopa and levodopa and processes of preparation thereof |