RU2420268C2 - Способ программируемой плавучей доставки - Google Patents
Способ программируемой плавучей доставки Download PDFInfo
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- RU2420268C2 RU2420268C2 RU2009112396/15A RU2009112396A RU2420268C2 RU 2420268 C2 RU2420268 C2 RU 2420268C2 RU 2009112396/15 A RU2009112396/15 A RU 2009112396/15A RU 2009112396 A RU2009112396 A RU 2009112396A RU 2420268 C2 RU2420268 C2 RU 2420268C2
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| US7201920B2 (en) | 2003-11-26 | 2007-04-10 | Acura Pharmaceuticals, Inc. | Methods and compositions for deterring abuse of opioid containing dosage forms |
| WO2009153635A1 (en) * | 2008-06-19 | 2009-12-23 | University Of Witwatersrand, Johannesburg | A chronotherapeutic pharmaceutical dosage form |
| ZA200903858B (en) * | 2008-06-19 | 2013-10-30 | Univ Of Witwatesrand Johannesburg | Pharmaceutical dosage form |
| CA2638240C (en) * | 2008-08-29 | 2010-02-02 | Alexander Macgregor | Method of treating dysglycemia and glucose excursions |
| CA2767143A1 (en) * | 2009-07-06 | 2011-01-13 | Kyorin Pharmaceutical Co., Ltd. | Tablet having hollow structure |
| US8901113B2 (en) | 2009-09-30 | 2014-12-02 | Acura Pharmaceuticals, Inc. | Methods and compositions for deterring abuse |
| US20110177231A1 (en) * | 2010-01-16 | 2011-07-21 | Alexander Grinberg | Nano-, Micro-, Macro- Encapsulation And Release Of Materials |
| US20110200671A1 (en) * | 2010-02-17 | 2011-08-18 | Sun Pharma Advanced Research Company Ltd. | Method of treating a disease condition susceptible to baclofen therapy |
| EP2415460A1 (de) * | 2010-08-03 | 2012-02-08 | ratiopharm GmbH | Orale Darreichungsform von Pregabalin |
| GB201102148D0 (en) | 2011-02-08 | 2011-03-23 | Ucl Business Plc | Layered bodies, compositions containing them and processes for producing them |
| BR112014000773A8 (pt) * | 2011-07-14 | 2017-10-03 | Apet Holding B V | Composições de nicotinamida e uso terapêutico das mesmas |
| ES2691982T3 (es) | 2012-11-30 | 2018-11-29 | Acura Pharmaceuticals, Inc. | Liberación autorregulada de un principio activo farmacéutico |
| US8859005B2 (en) | 2012-12-03 | 2014-10-14 | Intercontinental Great Brands Llc | Enteric delivery of functional ingredients suitable for hot comestible applications |
| KR102241487B1 (ko) | 2013-02-20 | 2021-04-16 | 주식회사 종근당 | 제어방출 펠릿으로 된 약제학적 조성물 |
| US20160242632A1 (en) * | 2013-10-22 | 2016-08-25 | Ganyu Lu | System and Method for Capsule Device with Multiple Phases of Density |
| WO2015145461A1 (en) | 2014-03-26 | 2015-10-01 | Sun Pharma Advanced Research Company Ltd. | Abuse deterrent immediate release biphasic matrix solid dosage form |
| CN106714893B (zh) | 2014-06-11 | 2021-01-01 | 麻省理工学院 | 自组装的驻留装置及相关方法 |
| US20170266112A1 (en) | 2014-06-11 | 2017-09-21 | Massachusetts Institute Of Technology | Residence structures and related methods |
| WO2017040607A1 (en) | 2015-08-31 | 2017-03-09 | Acura Pharmaceuticals, Inc. | Methods and compositions for self-regulated release of active pharmaceutical ingredient |
| HK1258050A1 (zh) | 2015-10-23 | 2019-11-01 | Lyndra Therapeutics, Inc. | 用於治疗剂缓释的胃驻留系统及其使用方法 |
| WO2017100367A1 (en) | 2015-12-08 | 2017-06-15 | Lyndra, Inc. | Geometric configurations for gastric residence systems |
| AU2017268840B2 (en) | 2016-05-27 | 2022-02-10 | Lyndra Therapeutics, Inc. | Materials architecture for gastric residence systems |
| WO2018064630A1 (en) | 2016-09-30 | 2018-04-05 | Lyndra, Inc. | Gastric residence systems for sustained delivery of adamantane-class drugs |
| US11534404B2 (en) * | 2016-10-06 | 2022-12-27 | Sucampo Ag | Multilayer beads for pharmaceutical use |
| CA3066658A1 (en) | 2017-06-09 | 2018-12-13 | Lyndra, Inc. | Gastric residence systems with release rate-modulating films |
| WO2019025869A1 (en) * | 2017-07-31 | 2019-02-07 | Teva Pharmaceutical Industries Limited | GALENIC FORMS WITH CONTROLLED RELEASE MANUFACTURED IN ADDITIVE MANNER |
| CA3086153A1 (en) | 2017-12-18 | 2019-06-27 | Tris Pharma, Inc. | Modified release drug powder composition comprising gastro-retentive raft forming systems having trigger pulse drug release |
| US11337920B2 (en) | 2017-12-18 | 2022-05-24 | Tris Pharma, Inc. | Pharmaceutical composition comprising GHB gastro-retentive raft forming systems having trigger pulse drug release |
| CA3085941A1 (en) | 2017-12-18 | 2019-06-27 | Tris Pharma, Inc. | Ghb pharmaceutical compositions comprising a floating interpenetrating polymer network forming system |
| JP7000148B2 (ja) * | 2017-12-27 | 2022-01-19 | 日本化薬株式会社 | ダサチニブを有効成分とする医薬組成物 |
| EP4013401A4 (en) | 2019-08-12 | 2023-07-12 | Massachusetts Institute of Technology | Articles and methods for administration of therapeutic agents |
| TWI763036B (zh) * | 2020-09-14 | 2022-05-01 | 王子賓 | 可膨脹微膠囊 |
| BR112023018524A2 (pt) | 2021-03-15 | 2023-11-21 | Epitomee Medical Ltd | Dispositivos expansíveis para entrega de agentes ativos aos tecidos |
| KR20250112750A (ko) | 2022-09-21 | 2025-07-24 | 이피토미 메디칼 엘티디 | 제어 가능하게 붕해될 수 있는 자체-확장가능한 섭취형 디바이스 |
| NL2033549B1 (en) * | 2022-11-17 | 2024-05-28 | Taiwan Mercury Medical Corp | Metformin tablet for relieving pain and reducing inflammation and manufacturing method thereof |
| AU2024265092A1 (en) * | 2023-05-03 | 2025-11-20 | Dark Canyon Laboratories, Llc | A floating drug delivery system for solid forms of salts used in bowel cleansing products |
Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999001112A1 (en) * | 1997-07-01 | 1999-01-14 | Astra Aktiebolag (Publ) | Multiple unit effervescent dosage form |
| WO2001058424A1 (en) * | 2000-02-09 | 2001-08-16 | West Pharmaceutical Services Drug Delivery & Clinical Research Centre Limited | Floating drug delivery composition |
| EP1574534A1 (en) * | 2004-03-11 | 2005-09-14 | Rohm And Haas Company | Polymer carriers and process |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
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| JPS5512411B2 (enExample) * | 1974-03-12 | 1980-04-02 | ||
| JPS5134879A (en) * | 1974-09-19 | 1976-03-24 | Eisai Co Ltd | Bishochukuryushinoseizoho |
| US5002772A (en) * | 1988-05-31 | 1991-03-26 | Pfizer Inc. | Gastric retention system for controlled drug release |
| NZ233403A (en) * | 1989-04-28 | 1992-09-25 | Mcneil Ppc Inc | Simulated capsule-like medicament |
| JPH03101615A (ja) * | 1989-09-14 | 1991-04-26 | Sumitomo Pharmaceut Co Ltd | 胃内滞留型持続性製剤 |
| IT1246382B (it) * | 1990-04-17 | 1994-11-18 | Eurand Int | Metodo per la cessione mirata e controllata di farmaci nell'intestino e particolarmente nel colon |
| US5314696A (en) * | 1991-06-27 | 1994-05-24 | Paulos Manley A | Methods for making and administering a blinded oral dosage form and blinded oral dosage form therefor |
| UA60318C2 (uk) * | 1997-03-26 | 2003-10-15 | Янссен Фармацевтика Н.В. | Пілюля, яка має ядро, покрите протигрибковим агентом і полімером, та спосіб її виготовлення |
| US5895663A (en) * | 1997-07-31 | 1999-04-20 | L. Perrigo Company | Pseudoephedrine hydrochloride extended-release tablets |
| US6050796A (en) | 1998-05-18 | 2000-04-18 | General Motors Corporation | Vane pump |
| JP2002370970A (ja) * | 2001-06-12 | 2002-12-24 | Sanwa Kagaku Kenkyusho Co Ltd | 胃内浮遊型固形製剤及びその製造方法 |
| JP4426286B2 (ja) * | 2001-07-10 | 2010-03-03 | 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 | 0次、0次−二相性、上昇型又は下降型薬物放出のための薬物送達システム |
| US7763663B2 (en) * | 2001-12-19 | 2010-07-27 | University Of Massachusetts | Polysaccharide-containing block copolymer particles and uses thereof |
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- 2007-09-03 ZA ZA200901162A patent/ZA200901162B/xx unknown
- 2007-09-03 US US12/439,775 patent/US8277843B2/en not_active Expired - Fee Related
- 2007-09-03 RU RU2009112396/15A patent/RU2420268C2/ru not_active IP Right Cessation
- 2007-09-03 EP EP07866696A patent/EP2068844A4/en not_active Withdrawn
- 2007-09-03 BR BRPI0716481-5A2A patent/BRPI0716481A2/pt not_active IP Right Cessation
- 2007-09-03 KR KR1020097006969A patent/KR20090065524A/ko not_active Ceased
- 2007-09-03 CA CA002661172A patent/CA2661172A1/en not_active Abandoned
- 2007-09-03 WO PCT/IN2007/000392 patent/WO2008062440A2/en not_active Ceased
- 2007-09-03 JP JP2009526263A patent/JP2010502591A/ja active Pending
- 2007-09-03 AU AU2007323018A patent/AU2007323018B2/en not_active Ceased
- 2007-09-03 MX MX2009002371A patent/MX2009002371A/es unknown
- 2007-09-04 CL CL200702562A patent/CL2007002562A1/es unknown
- 2007-09-04 AR ARP070103903A patent/AR062644A1/es not_active Application Discontinuation
-
2009
- 2009-02-19 IL IL197121A patent/IL197121A0/en unknown
- 2009-02-19 NO NO20090807A patent/NO20090807A/no not_active Application Discontinuation
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO1999001112A1 (en) * | 1997-07-01 | 1999-01-14 | Astra Aktiebolag (Publ) | Multiple unit effervescent dosage form |
| WO2001058424A1 (en) * | 2000-02-09 | 2001-08-16 | West Pharmaceutical Services Drug Delivery & Clinical Research Centre Limited | Floating drug delivery composition |
| EP1574534A1 (en) * | 2004-03-11 | 2005-09-14 | Rohm And Haas Company | Polymer carriers and process |
Also Published As
| Publication number | Publication date |
|---|---|
| BRPI0716481A2 (pt) | 2014-03-18 |
| WO2008062440A3 (en) | 2008-07-31 |
| RU2009112396A (ru) | 2010-10-20 |
| CL2007002562A1 (es) | 2008-02-08 |
| KR20090065524A (ko) | 2009-06-22 |
| NO20090807A (no) | 2009-06-04 |
| CN101511346A (zh) | 2009-08-19 |
| MX2009002371A (es) | 2009-03-12 |
| AU2007323018B2 (en) | 2011-02-03 |
| CA2661172A1 (en) | 2008-05-29 |
| AU2007323018A1 (en) | 2008-05-29 |
| CN101511346B (zh) | 2012-07-04 |
| EP2068844A4 (en) | 2013-01-23 |
| WO2008062440A2 (en) | 2008-05-29 |
| JP2010502591A (ja) | 2010-01-28 |
| IL197121A0 (en) | 2009-11-18 |
| AR062644A1 (es) | 2008-11-19 |
| EP2068844A2 (en) | 2009-06-17 |
| US20100015224A1 (en) | 2010-01-21 |
| US8277843B2 (en) | 2012-10-02 |
| ZA200901162B (en) | 2010-06-30 |
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| MM4A | The patent is invalid due to non-payment of fees |
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