TWI798161B - 持續釋放的奧氮平調配物 - Google Patents
持續釋放的奧氮平調配物 Download PDFInfo
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- TWI798161B TWI798161B TW105130439A TW105130439A TWI798161B TW I798161 B TWI798161 B TW I798161B TW 105130439 A TW105130439 A TW 105130439A TW 105130439 A TW105130439 A TW 105130439A TW I798161 B TWI798161 B TW I798161B
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- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1629—Organic macromolecular compounds
- A61K9/1641—Organic macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyethylene glycol, poloxamers
- A61K9/1647—Polyesters, e.g. poly(lactide-co-glycolide)
-
- 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
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
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- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Dermatology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Proteomics, Peptides & Aminoacids (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Biological Depolymerization Polymers (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562221290P | 2015-09-21 | 2015-09-21 | |
| US62/221,290 | 2015-09-21 |
Publications (2)
| Publication Number | Publication Date |
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| TW201726144A TW201726144A (zh) | 2017-08-01 |
| TWI798161B true TWI798161B (zh) | 2023-04-11 |
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| TW105130439A TWI798161B (zh) | 2015-09-21 | 2016-09-21 | 持續釋放的奧氮平調配物 |
Country Status (21)
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018172850A1 (en) * | 2017-03-20 | 2018-09-27 | Teva Pharmaceuticals International Gmbh | Sustained release olanzapine formulaitons |
| CN111836615A (zh) * | 2018-01-05 | 2020-10-27 | 英倍尔药业股份有限公司 | 通过精密鼻装置的奥氮平的鼻内递送 |
| AU2020410549A1 (en) * | 2019-12-20 | 2022-04-14 | Alar Pharmaceuticals Inc. | Long-acting injectable formulations of ketamine pamoate salts |
| CN112587505A (zh) * | 2020-10-16 | 2021-04-02 | 长春斯菲尔生物科技有限公司 | 一种奥氮平双羟萘酸盐缓释微粒制剂及其制备方法 |
| WO2025188992A1 (en) * | 2024-03-06 | 2025-09-12 | Neurelis, Inc. | Oral film for rapid active delivery |
Family Cites Families (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7833543B2 (en) | 1995-06-07 | 2010-11-16 | Durect Corporation | High viscosity liquid controlled delivery system and medical or surgical device |
| EA002825B1 (ru) * | 1997-09-30 | 2002-10-31 | Эли Лилли Энд Компани | Препарат 2-метилтиенобензодиазепина |
| US6495164B1 (en) | 2000-05-25 | 2002-12-17 | Alkermes Controlled Therapeutics, Inc. I | Preparation of injectable suspensions having improved injectability |
| US7731947B2 (en) | 2003-11-17 | 2010-06-08 | Intarcia Therapeutics, Inc. | Composition and dosage form comprising an interferon particle formulation and suspending vehicle |
| DK1635875T3 (da) | 2003-06-26 | 2009-01-12 | Psivida Inc | In-situ-geldannende lægemiddeladministrationssystem |
| KR101242486B1 (ko) | 2004-01-12 | 2013-03-13 | 더 트러스티스 오브 더 유니버시티 오브 펜실베니아 | 장기 전달을 위한 제형 및 그의 이용 방법 |
| EP1576952A1 (en) | 2004-03-18 | 2005-09-21 | OctoPlus Technologies B.V. | Hydrogel microspheres with improved release profile |
| NL1026261C2 (nl) | 2004-05-25 | 2005-11-28 | Nanomi B V | Sproei inrichting met een nozzleplaat voorzien van structuren ter bevordering van self-breakup, een nozzleplaat, alsmede werkwijzen ter vervaardiging en toepassing van een dergelijke nozzleplaat. |
| NZ551990A (en) | 2004-06-04 | 2011-01-28 | Camurus Ab | Liquid depot formulations |
| AU2005307797B2 (en) * | 2004-11-16 | 2011-06-02 | Alkermes Pharma Ireland Limited | Injectable nanoparticulate olanzapine formulations |
| EP1874267A1 (en) * | 2005-04-13 | 2008-01-09 | Pfizer Products Inc. | Injectable depot formulations and methods for providing sustained release of poorly soluble drugs comprising nanoparticles |
| WO2006109183A1 (en) * | 2005-04-13 | 2006-10-19 | Pfizer Products Inc. | Injectable depot formulations and methods for providing sustained release of nanoparticle compositions |
| ATE552032T1 (de) * | 2005-07-14 | 2012-04-15 | Lithera Inc | Verbesserte lipolytikum-formulierung mit hinhaltender wirkstofffreigabe für die arealbehandlung von fettgewebe |
| US8852638B2 (en) | 2005-09-30 | 2014-10-07 | Durect Corporation | Sustained release small molecule drug formulation |
| US20070254832A1 (en) * | 2006-02-17 | 2007-11-01 | Pressler Milton L | Methods for the treatment of macular degeneration and related eye conditions |
| WO2007139744A2 (en) | 2006-05-23 | 2007-12-06 | Titan Pharmaceuticals, Inc. | Implantable polymeric device for sustained release of buprenorphine with minimal initial burst |
| KR20140109509A (ko) | 2006-07-11 | 2014-09-15 | 큐피에스 엘엘씨 | 펩타이드의 지속 방출 전달을 위한 의약 조성물 |
| FI20070174A0 (fi) | 2007-02-28 | 2007-02-28 | Delsitech Oy | Menetelmä silikakoostumusten valmistamiseksi, silikakoostumukset ja niiden käytöt |
| KR100805208B1 (ko) | 2007-03-27 | 2008-02-21 | 주식회사 펩트론 | 엑센딘 함유 서방성 제제 조성물, 엑센딘 함유 서방성미립구 및 이의 제조 방법 |
| EP2139458A4 (en) | 2007-04-19 | 2013-01-23 | Dong A Pharm Co Ltd | COMPOSITION OF BIODEGRADABLE MICROSPHERES WITH CONTROLLED RELEASE OF A GLUCOSE REGULATING PEPTIDE AND RELATED FORMULA |
| US10010612B2 (en) | 2007-05-25 | 2018-07-03 | Indivior Uk Limited | Sustained delivery formulations of risperidone compounds |
| ES2324009B1 (es) | 2007-11-23 | 2010-05-21 | Gp Pharm S.A. | Composicion farmaceutica de liberacion sostenida de somatostatina o un analogo suyo. |
| JP5222550B2 (ja) * | 2007-12-27 | 2013-06-26 | 財團法人工業技術研究院 | 徐放性組成物およびその製造方法 |
| US20090181068A1 (en) | 2008-01-14 | 2009-07-16 | Dunn Richard L | Low Viscosity Liquid Polymeric Delivery System |
| US20090263443A1 (en) * | 2008-04-18 | 2009-10-22 | Warsaw Orthopedics, Inc. | Methods for treating post-operative effects such as spasticity and shivering with clondine |
| EP2309982A2 (en) | 2008-06-03 | 2011-04-20 | Tolmar Therapeutics, Inc. | Controlled release copolymer formulation with improved release kinetics |
| KR101626632B1 (ko) | 2008-08-12 | 2016-06-01 | 노파르티스 아게 | 제약 조성물 |
| PT2355853T (pt) | 2008-10-10 | 2017-03-15 | Polyactiva Pty Ltd | Conjugados polímero biodegradável ¿ unidade bioativa |
| JP2012512175A (ja) | 2008-12-15 | 2012-05-31 | バインド バイオサイエンシズ インコーポレイテッド | 治療薬を徐放するための長時間循環性ナノ粒子 |
| US9561352B2 (en) | 2009-03-12 | 2017-02-07 | Delpor, Inc. | Implantable device for long-term delivery of drugs |
| EP2485712A1 (en) | 2009-10-06 | 2012-08-15 | Ascendis Pharma A/S | Subcutaneous paliperidone composition |
| DK3536333T3 (da) | 2010-01-04 | 2022-10-24 | Mapi Pharma Ltd | Depotsystem der omfatter glatirameracetat |
| EP2343046A1 (en) | 2010-01-08 | 2011-07-13 | Nirvana's Tree House B.V. | Functionalised triblock copolymers and compositions containing such polymers |
| LT2394663T (lt) * | 2010-05-31 | 2022-02-10 | Laboratorios Farmaceuticos Rovi, S.A. | Kompozicijos, skirtos įšvirkščiamiems in situ biologiškai skaidiems implantams |
| UA111162C2 (uk) | 2010-08-04 | 2016-04-11 | Флекшен Терап'Ютікс, Інк. | Ін'єкційна композиція ацетоніду триамцинолону для лікування болю |
| FR2968994B1 (fr) | 2010-12-17 | 2012-12-28 | Flamel Tech Sa | Procede de preparation de nanoparticules |
| CN103491946B (zh) | 2010-12-29 | 2016-08-10 | 美蒂森 | 可生物降解的药物释放组合物 |
| SI2717914T1 (sl) | 2011-06-10 | 2020-07-31 | Ramscor Inc. | Formulacije z zadržanim sproščanjem za dostavo proteinov v oko in postopki njihove priprave |
| MX350469B (es) | 2011-10-24 | 2017-09-07 | Endo Pharmaceuticals Solutions | Composiciones para el suministro de farmacos implantables y metodos para su tratamiento. |
| MX364864B (es) | 2012-01-23 | 2019-05-09 | Allergan Inc | Microesferas o microparticulas biodegradables o bioerosionables de liberacion progresiva suspendidas en una formulacion de farmaco inyectable de formacion de deposito solidificante. |
| CN103417492A (zh) * | 2012-05-25 | 2013-12-04 | 上海现代药物制剂工程研究中心有限公司 | 含有奥氮平的生物降解微球制剂及其制备方法 |
| US20140323517A1 (en) | 2013-04-30 | 2014-10-30 | Heron Therapeutics, Inc. | Compositions and methods for injection of a biodegradable polymer-based delivery system |
| WO2014202214A1 (en) | 2013-06-20 | 2014-12-24 | Pharmathen S.A. | Preparation of polylactide-polyglycolide microparticles having a sigmoidal release profile |
| CN103877005A (zh) * | 2014-03-26 | 2014-06-25 | 陈德香 | 一种复方奥氮平皮下埋植缓释剂 |
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2016
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- 2016-09-21 HU HUE16775424A patent/HUE063850T2/hu unknown
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- 2016-09-21 US US15/271,508 patent/US20170079985A1/en not_active Abandoned
- 2016-09-21 IL IL295161A patent/IL295161A/en unknown
- 2016-09-21 PT PT167754241T patent/PT3352735T/pt unknown
- 2016-09-21 CN CN202310947482.0A patent/CN116942677A/zh active Pending
- 2016-09-21 AU AU2016328958A patent/AU2016328958B2/en active Active
- 2016-09-21 PL PL16775424.1T patent/PL3352735T3/pl unknown
- 2016-09-21 MX MX2018003380A patent/MX2018003380A/es unknown
- 2016-09-21 JP JP2018515050A patent/JP2018527397A/ja active Pending
- 2016-09-21 EA EA201890788A patent/EA201890788A1/ru unknown
- 2016-09-21 EP EP16775424.1A patent/EP3352735B1/en active Active
- 2016-09-21 TW TW105130439A patent/TWI798161B/zh active
- 2016-09-21 ES ES16775424T patent/ES2960753T3/es active Active
- 2016-09-21 DK DK16775424.1T patent/DK3352735T3/da active
- 2016-09-21 CA CA2998504A patent/CA2998504C/en active Active
- 2016-09-21 NZ NZ740665A patent/NZ740665A/en unknown
- 2016-09-21 KR KR1020187007791A patent/KR20180054627A/ko not_active Ceased
- 2016-09-21 CN CN201680066464.XA patent/CN108289834A/zh active Pending
- 2016-09-21 AR ARP160102864A patent/AR106085A1/es not_active Application Discontinuation
- 2016-09-21 FI FIEP16775424.1T patent/FI3352735T3/fi active
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2018
- 2018-03-13 IL IL258086A patent/IL258086A/en unknown
- 2018-03-16 MX MX2022007315A patent/MX2022007315A/es unknown
- 2018-03-20 CL CL2018000727A patent/CL2018000727A1/es unknown
- 2018-05-17 US US15/982,449 patent/US20180264001A1/en not_active Abandoned
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2020
- 2020-06-29 IL IL275735A patent/IL275735A/en unknown
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2021
- 2021-07-01 JP JP2021110240A patent/JP2021167331A/ja active Pending
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2022
- 2022-06-23 US US17/847,685 patent/US20220323458A1/en not_active Abandoned
- 2022-07-18 AU AU2022206695A patent/AU2022206695A1/en not_active Abandoned
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2024
- 2024-04-01 US US18/623,327 patent/US20240238307A1/en not_active Abandoned
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