JP2015522534A5 - - Google Patents
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- Publication number
- JP2015522534A5 JP2015522534A5 JP2015511680A JP2015511680A JP2015522534A5 JP 2015522534 A5 JP2015522534 A5 JP 2015522534A5 JP 2015511680 A JP2015511680 A JP 2015511680A JP 2015511680 A JP2015511680 A JP 2015511680A JP 2015522534 A5 JP2015522534 A5 JP 2015522534A5
- Authority
- JP
- Japan
- Prior art keywords
- nimodipine
- microparticle
- delivery system
- polymorph form
- powder
- 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.)
- Granted
Links
- 238000000034 method Methods 0.000 claims description 53
- 239000011859 microparticle Substances 0.000 claims description 49
- UIAGMCDKSXEBJQ-IBGZPJMESA-N 3-o-(2-methoxyethyl) 5-o-propan-2-yl (4s)-2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate Chemical compound COCCOC(=O)C1=C(C)NC(C)=C(C(=O)OC(C)C)[C@H]1C1=CC=CC([N+]([O-])=O)=C1 UIAGMCDKSXEBJQ-IBGZPJMESA-N 0.000 claims description 40
- 239000000203 mixture Substances 0.000 claims description 36
- 229960000715 nimodipine Drugs 0.000 claims description 34
- 238000000634 powder X-ray diffraction Methods 0.000 claims description 34
- 238000009472 formulation Methods 0.000 claims description 18
- 238000001228 spectrum Methods 0.000 claims description 16
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 claims description 15
- 229920002988 biodegradable polymer Polymers 0.000 claims description 15
- 239000004621 biodegradable polymer Substances 0.000 claims description 15
- 229920000642 polymer Polymers 0.000 claims description 12
- 210000001627 cerebral artery Anatomy 0.000 claims description 11
- 238000013268 sustained release Methods 0.000 claims description 11
- 239000012730 sustained-release form Substances 0.000 claims description 11
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 claims description 9
- 238000001035 drying Methods 0.000 claims description 9
- 229920001710 Polyorthoester Polymers 0.000 claims description 7
- 150000008064 anhydrides Chemical class 0.000 claims description 7
- 238000010924 continuous production Methods 0.000 claims description 7
- 239000002745 poly(ortho ester) Substances 0.000 claims description 7
- 210000002330 subarachnoid space Anatomy 0.000 claims description 7
- 230000009969 flowable effect Effects 0.000 claims description 6
- 239000007787 solid Substances 0.000 claims description 6
- 239000002904 solvent Substances 0.000 claims description 6
- 230000001225 therapeutic effect Effects 0.000 claims description 6
- 206010047163 Vasospasm Diseases 0.000 claims description 5
- 210000001175 cerebrospinal fluid Anatomy 0.000 claims description 5
- 239000010419 fine particle Substances 0.000 claims description 5
- 239000011159 matrix material Substances 0.000 claims description 5
- 238000002360 preparation method Methods 0.000 claims description 5
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 4
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Polymers OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 claims description 4
- 229920000954 Polyglycolide Polymers 0.000 claims description 4
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 4
- 230000003111 delayed effect Effects 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 4
- 239000004094 surface-active agent Substances 0.000 claims description 4
- 239000003937 drug carrier Substances 0.000 claims description 3
- 239000000839 emulsion Substances 0.000 claims description 3
- 238000002156 mixing Methods 0.000 claims description 3
- 229920000747 poly(lactic acid) Polymers 0.000 claims description 3
- 239000000843 powder Substances 0.000 claims description 3
- 239000000725 suspension Substances 0.000 claims description 3
- 230000001839 systemic circulation Effects 0.000 claims description 3
- RKDVKSZUMVYZHH-UHFFFAOYSA-N 1,4-dioxane-2,5-dione Chemical compound O=C1COC(=O)CO1 RKDVKSZUMVYZHH-UHFFFAOYSA-N 0.000 claims description 2
- 201000006474 Brain Ischemia Diseases 0.000 claims description 2
- 206010008120 Cerebral ischaemia Diseases 0.000 claims description 2
- 238000001069 Raman spectroscopy Methods 0.000 claims description 2
- 230000015572 biosynthetic process Effects 0.000 claims description 2
- 208000029028 brain injury Diseases 0.000 claims description 2
- 206010008118 cerebral infarction Diseases 0.000 claims description 2
- 230000001054 cortical effect Effects 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 208000028867 ischemia Diseases 0.000 claims description 2
- JJTUDXZGHPGLLC-UHFFFAOYSA-N lactide Chemical compound CC1OC(=O)C(C)OC1=O JJTUDXZGHPGLLC-UHFFFAOYSA-N 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 238000003892 spreading Methods 0.000 claims description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 2
- 239000006185 dispersion Substances 0.000 claims 3
- 238000002844 melting Methods 0.000 claims 3
- 230000008018 melting Effects 0.000 claims 3
- 229920000742 Cotton Polymers 0.000 claims 1
- 208000001953 Hypotension Diseases 0.000 claims 1
- 238000000113 differential scanning calorimetry Methods 0.000 claims 1
- 230000036543 hypotension Effects 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 238000000185 intracerebroventricular administration Methods 0.000 claims 1
- 230000002688 persistence Effects 0.000 claims 1
- 238000011200 topical administration Methods 0.000 claims 1
- 239000012867 bioactive agent Substances 0.000 description 11
- 150000001875 compounds Chemical class 0.000 description 6
- 239000000243 solution Substances 0.000 description 4
- 238000002347 injection Methods 0.000 description 3
- 239000007924 injection Substances 0.000 description 3
- 238000012986 modification Methods 0.000 description 3
- 230000004048 modification Effects 0.000 description 3
- 239000002245 particle Substances 0.000 description 3
- 238000009826 distribution Methods 0.000 description 2
- 230000000694 effects Effects 0.000 description 2
- 208000001286 intracranial vasospasm Diseases 0.000 description 2
- 206010063648 Cerebral artery stenosis Diseases 0.000 description 1
- 230000006931 brain damage Effects 0.000 description 1
- 231100000874 brain damage Toxicity 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000012530 fluid Substances 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 230000000144 pharmacologic effect Effects 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261644523P | 2012-05-09 | 2012-05-09 | |
| US61/644,523 | 2012-05-09 | ||
| US13/800,480 US9399019B2 (en) | 2012-05-09 | 2013-03-13 | Polymorph compositions, methods of making, and uses thereof |
| US13/800,480 | 2013-03-13 | ||
| PCT/US2013/040265 WO2013169979A2 (en) | 2012-05-09 | 2013-05-09 | Polymorph compositions, methods of making, and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015522534A JP2015522534A (ja) | 2015-08-06 |
| JP2015522534A5 true JP2015522534A5 (enExample) | 2016-04-21 |
| JP6338573B2 JP6338573B2 (ja) | 2018-06-06 |
Family
ID=49548793
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015511680A Expired - Fee Related JP6338573B2 (ja) | 2012-05-09 | 2013-05-09 | 多形体組成物、その製造方法及びその使用 |
Country Status (15)
| Country | Link |
|---|---|
| US (2) | US9399019B2 (enExample) |
| EP (1) | EP2846775A4 (enExample) |
| JP (1) | JP6338573B2 (enExample) |
| KR (1) | KR101784260B1 (enExample) |
| CN (1) | CN104955445A (enExample) |
| AU (1) | AU2013259476B2 (enExample) |
| BR (1) | BR112014027965A2 (enExample) |
| CA (2) | CA2961123A1 (enExample) |
| GB (1) | GB2517096A (enExample) |
| HK (2) | HK1202264A1 (enExample) |
| IL (1) | IL235262A0 (enExample) |
| NZ (1) | NZ629727A (enExample) |
| RU (1) | RU2014149362A (enExample) |
| SG (1) | SG11201407266PA (enExample) |
| WO (1) | WO2013169979A2 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10092524B2 (en) * | 2008-06-11 | 2018-10-09 | Edge Therapeutics, Inc. | Compositions and their use to treat complications of aneurysmal subarachnoid hemorrhage |
| US9399019B2 (en) * | 2012-05-09 | 2016-07-26 | Evonik Corporation | Polymorph compositions, methods of making, and uses thereof |
| CA2986692A1 (en) * | 2015-05-29 | 2016-12-08 | Edge Therapeutics, Inc. | Compositions and methods for reducing visual loss |
| WO2017176914A1 (en) * | 2016-04-07 | 2017-10-12 | Edge Therapeutics, Inc. | Formulations of site-specific, microparticulate compositions and their use to improve outcome after aneurysmal subarachnoid hemorrhage |
| CN105944152B (zh) * | 2016-06-13 | 2019-02-12 | 龙岩紫荆创新研究院 | 可吸收防粘医用膜的制备方法 |
| WO2018039039A1 (en) * | 2016-08-23 | 2018-03-01 | Edge Therapeutics, Inc. | Scalable microparticulate formulations containing polymorphic nimodipine form 2 prepared by a solvent evaporation process |
| WO2019018306A1 (en) * | 2017-07-17 | 2019-01-24 | Edge Therapeutics, Inc. | ADVANCED MICROPARTICULAR FORMULATIONS CONTAINING FORM 2 OF MICRONIZED POLYMORPHIC NIMODIPINE |
| JP2021535932A (ja) * | 2018-09-08 | 2021-12-23 | 江蘇九旭海天薬業有限公司 | ニモジピン注射用組成物及びその調製方法 |
| CN113227250B (zh) * | 2018-10-04 | 2024-01-30 | 亚历山德拉·乌尼诺夫 | 无聚氯乙烯的芳香的基于亲脂的聚合物的塑料溶胶 |
| KR102181231B1 (ko) * | 2018-11-22 | 2020-11-20 | 주식회사 메디포럼제약 | 로티고틴 함유 고분자 미립자의 제조방법 |
Family Cites Families (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2117571C3 (de) | 1971-04-10 | 1979-10-11 | Bayer Ag, 5090 Leverkusen | Unsymmetrische 1,4-Dihydropyridin-33-dicarbonsäureester, Verfahren zu ihrer Herstellung sowie ihre Verwendung als Arzneimittel |
| US3932645A (en) | 1971-04-10 | 1976-01-13 | Farbenfabriken Bayer Ag | Pharmaceutical compositions containing unsymmetrical esters of 1,4-dihydropyridine 3,5-dicarboxylic acid |
| US4757128A (en) | 1986-08-01 | 1988-07-12 | Massachusetts Institute Of Technology | High molecular weight polyanhydride and preparation thereof |
| ATE133087T1 (de) | 1989-05-04 | 1996-02-15 | Southern Res Inst | Einkapselungsverfahren |
| US5650489A (en) | 1990-07-02 | 1997-07-22 | The Arizona Board Of Regents | Random bio-oligomer library, a method of synthesis thereof, and a method of use thereof |
| DE4130173A1 (de) | 1991-09-11 | 1993-03-18 | Bayer Ag | Pharmazeutische zubereitungen mit einer speziellen kristallmodifikation des 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-3,5-pyridindicarbonsaeure-isopropyl-(2-methoxyethyl)-esters |
| IT1255792B (it) | 1992-08-05 | 1995-11-16 | Bayer Italia Spa | Composizioni farmaceutiche per la somministrazione orale di diidropiridine in forma di bevanda |
| US5399665A (en) | 1992-11-05 | 1995-03-21 | Massachusetts Institute Of Technology | Biodegradable polymers for cell transplantation |
| EP0740791A4 (en) | 1994-01-05 | 2000-04-05 | Arqule Inc | SYSTEMATIC MODULAR PRODUCTION OF AMINIMID AND OXAZOLONE-BASED MOLECULES WITH SELECTED PROPERTIES |
| US5712171A (en) | 1995-01-20 | 1998-01-27 | Arqule, Inc. | Method of generating a plurality of chemical compounds in a spatially arranged array |
| US5968542A (en) | 1995-06-07 | 1999-10-19 | Southern Biosystems, Inc. | High viscosity liquid controlled delivery system as a device |
| US5747058A (en) | 1995-06-07 | 1998-05-05 | Southern Biosystems, Inc. | High viscosity liquid controlled delivery system |
| JP2909418B2 (ja) | 1995-09-18 | 1999-06-23 | 株式会社資生堂 | 薬物の遅延放出型マイクロスフイア |
| EP0932399B1 (en) | 1996-03-12 | 2006-01-04 | PG-TXL Company, L.P. | Water soluble paclitaxel prodrugs |
| KR100236771B1 (ko) | 1997-04-01 | 2000-02-01 | 성재갑 | 히아루론산을 이용한 약물의 서방성 미세입자 제형 |
| US6123956A (en) | 1997-07-10 | 2000-09-26 | Keith Baker | Methods for universally distributing therapeutic agents to the brain |
| US6224794B1 (en) | 1998-05-06 | 2001-05-01 | Angiotech Pharmaceuticals, Inc. | Methods for microsphere production |
| US6455526B1 (en) * | 1998-12-16 | 2002-09-24 | Aventis Pharmaceuticals, Inc. | Biodegradable polymer encapsulated pharmaceutical compositions and method for preparing the same |
| US6869551B2 (en) * | 2001-03-30 | 2005-03-22 | Picoliter Inc. | Precipitation of solid particles from droplets formed using focused acoustic energy |
| US20040235801A1 (en) | 2001-10-25 | 2004-11-25 | Jean-Pierre Julien | Therapy for stroke |
| US20070207211A1 (en) | 2003-04-10 | 2007-09-06 | Pr Pharmaceuticals, Inc. | Emulsion-based microparticles and methods for the production thereof |
| JP2007515392A (ja) | 2003-04-10 | 2007-06-14 | ピーアール ファーマシューティカルズ，インコーポレイテッド | エマルジョンベースの微粒子の製造のための方法 |
| US7279579B2 (en) | 2003-06-04 | 2007-10-09 | Alkermes, Inc. | Polymorphic forms of naltrexone |
| CA2533592C (en) | 2003-07-23 | 2015-11-10 | Pr Pharmaceuticals, Inc. | Controlled release compositions |
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| WO2006084005A2 (en) | 2005-02-02 | 2006-08-10 | University Of Vermont And State Agricultural College | Emergence of a r-type ca2+channel(cav2.3) contributes to cerebral artery constriction following subarachnoid hemorrhage |
| US20060217340A1 (en) | 2005-03-23 | 2006-09-28 | University Of Vermont And State Agricultural College | Methods and products for treating hypertension by modulation of TRPC3 channel activity |
| CN101045054A (zh) | 2006-03-29 | 2007-10-03 | 上海医药工业研究院 | 尼莫地平纳米混悬剂冻干组合物、其制备方法及应用 |
| WO2008132710A2 (en) | 2007-05-01 | 2008-11-06 | Sigmoid Pharma Limited | Pharmaceutical nimodipine compositions |
| US20120164226A1 (en) | 2007-06-11 | 2012-06-28 | Leuthner Brian A | Compositions and Methods for Improving Prognosis of a Human with Subarachnoid Hemorrhage |
| KR101554250B1 (ko) * | 2007-06-11 | 2015-09-18 | 알. 로치 맥도날드 | 뇌혈관 연축의 예방을 위한 약물 전달 시스템 |
| JP5502751B2 (ja) | 2007-12-20 | 2014-05-28 | エボニック コーポレイション | 低残留溶媒濃度を有する微粒子を調製するためのプロセス |
| US20100008968A1 (en) | 2008-06-26 | 2010-01-14 | Lampe John W | Method for treating cardiovascular diseases using rho kinase inhibitor compounds |
| EP2331082B1 (en) | 2008-09-11 | 2021-01-06 | Evonik Corporation | Solvent extraction microencapsulation with tunable extraction rates |
| EP2334288B1 (en) | 2008-09-18 | 2021-05-19 | Evonik Corporation | Microencapsulation process with solvent and salt |
| CN101416963A (zh) | 2008-12-02 | 2009-04-29 | 沈阳万爱普利德医药科技有限公司 | 注射用尼莫地平冻干亚微乳剂及其制备方法 |
| US20100216948A1 (en) | 2009-01-23 | 2010-08-26 | Tipton Arthur J | Polymer mixtures comprising polymers having different non-repeating units and methods for making and using same |
| WO2010085609A2 (en) | 2009-01-23 | 2010-07-29 | Surmodics Pharmaceuticals, Inc. | Controlled release systems from polymer blends |
| US20130059008A1 (en) | 2009-01-23 | 2013-03-07 | Jeffrey L. Atkinson | Drying methods for tuning microparticle properties |
| CN101485632B (zh) | 2009-02-11 | 2011-05-18 | 西安德天药业股份有限公司 | 尼莫地平脂质微球注射液及其制备方法 |
| US20100291027A1 (en) | 2009-05-14 | 2010-11-18 | Jason Campbell | Hyaluronic acid (ha) injection vehicle |
| WO2011087689A2 (en) | 2009-12-22 | 2011-07-21 | Surmodics Pharmaceuticals,Inc. | Emulsion-based process for preparing microparticles and workhead assembly for use with same |
| GB2490084A (en) | 2010-02-22 | 2012-10-17 | Edge Therapeutics Inc | Methods and compositions to treat hemorrhagic conditions of the brain |
| US9504643B2 (en) | 2010-03-29 | 2016-11-29 | Evonik Corporation | Compositions and methods for improved retention of a pharmaceutical composition at a local administration site |
| SG10201602665UA (en) | 2011-04-05 | 2016-05-30 | Edge Therapeutics | Intraventricular Drug Delivery System For Improving Outcome After A Brain Injury Affecting Cerebral Blood Flow |
| CN102274176B (zh) | 2011-08-04 | 2013-11-20 | 上海天氏利医药科技有限公司 | 一种尼莫地平注射液的组合物及其制备方法与应用 |
| US9399019B2 (en) * | 2012-05-09 | 2016-07-26 | Evonik Corporation | Polymorph compositions, methods of making, and uses thereof |
-
2013
- 2013-03-13 US US13/800,480 patent/US9399019B2/en not_active Expired - Fee Related
- 2013-05-09 KR KR1020147034606A patent/KR101784260B1/ko not_active Expired - Fee Related
- 2013-05-09 GB GB1418703.3A patent/GB2517096A/en not_active Withdrawn
- 2013-05-09 RU RU2014149362A patent/RU2014149362A/ru not_active Application Discontinuation
- 2013-05-09 HK HK15102813.4A patent/HK1202264A1/xx unknown
- 2013-05-09 EP EP13787017.6A patent/EP2846775A4/en not_active Withdrawn
- 2013-05-09 WO PCT/US2013/040265 patent/WO2013169979A2/en not_active Ceased
- 2013-05-09 HK HK15108503.6A patent/HK1207824A1/xx unknown
- 2013-05-09 CA CA2961123A patent/CA2961123A1/en not_active Abandoned
- 2013-05-09 NZ NZ629727A patent/NZ629727A/en not_active IP Right Cessation
- 2013-05-09 SG SG11201407266PA patent/SG11201407266PA/en unknown
- 2013-05-09 CN CN201380023989.1A patent/CN104955445A/zh active Pending
- 2013-05-09 BR BR112014027965A patent/BR112014027965A2/pt not_active Application Discontinuation
- 2013-05-09 CA CA2872887A patent/CA2872887C/en not_active Expired - Fee Related
- 2013-05-09 AU AU2013259476A patent/AU2013259476B2/en not_active Ceased
- 2013-05-09 JP JP2015511680A patent/JP6338573B2/ja not_active Expired - Fee Related
- 2013-07-16 US US13/943,547 patent/US8821944B1/en not_active Expired - Fee Related
-
2014
- 2014-10-22 IL IL235262A patent/IL235262A0/en unknown
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