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公开(公告)号：EP1628664A2
公开(公告)日：2006-03-01
申请号：EP04754164.4
申请日：2004-06-03
发明人： BRITTAIN, Harry, A. , DICKASON, David, A. , HOTZ, Joyce , LYONS, Shawn, L. , RAMSTACK, Michael, J. , WRIGHT, Steven, G.
IPC分类号： A61K31/485
CPC分类号： A61K31/485 , C07B2200/13 , C07C19/03 , C07D489/06 , C07D489/08
摘要： This invention relates to the discovery of novel polymorphic forms of naltrexone, including solvates, hydrates, anhydrous and other crystalline forms and combinations thereof. These novel forms of naltrexone impart advantages in pharmaceutical formulations incorporating them, including sustained release, or long acting, formulations.
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公开(公告)号：EP1140029B1
公开(公告)日：2005-11-09
申请号：EP99965212.6
申请日：1999-12-10
CPC分类号： A61K9/1647 , A61K9/1694 , B01J13/02 , Y10T428/2982
摘要： An improved method for preparing microparticles that exhibit controlled release of an effective amount of an active agent over an extended period of time. More particularly, a method is provided for preparing microparticles having a selected release profile for release of active agent contained in the microparticles. By adjusting the degree of drying that is performed during the preparation of the microparticles, the release profile can be controlled. By performing no intermediate drying, an initial burst and a substantially linear release profile is achieved. By performing substantially complete intermediate drying, an initial lag phase and a substantially sigmoidal release profile is achieved.
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公开(公告)号：EP1231898A2
公开(公告)日：2002-08-21
申请号：EP00991722.0
申请日：2000-11-03
IPC分类号： A61K9/16
CPC分类号： A61K9/1694 , A61K9/1682 , Y10T428/2985
摘要： Apparatus and method for preparing microparticles. An emulsion is formed by combining two phases in a static mixing assembly (730). The static mixing assembly preferably includes a preblending static mixer (732) and a manifold (734). The emulsion flows out of the static mixing assembly into a quench liquid whereby droplets of the emulsion form microparticles. The residence time of the emulsion in the static mixing assembly is controlled to obtain a predetermined particle size distribution of the resulting microparticles.
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4.发明公开Preparation of biodegradable microparticles containing a biologically active agent 失效含有生物活性物质的生物可降解微粒的生产
公开(公告)号：EP0998917A1
公开(公告)日：2000-05-10
申请号：EP99122848.7
申请日：1994-11-18
IPC分类号： A61K9/16
CPC分类号： A61K9/1694 , A61K9/1647 , B01J13/06 , B01J13/08 , Y10S977/788 , Y10S977/898 , Y10S977/90
摘要： A process for preparing biodegradable microparticles comprising a biodegradable polymeric binder and a biologically active agent. A first phase, comprising the active agent and the polymer, and a second phase are pumped through a static mixer into a quench liquid to form microparticles containing the active agent. Preferably, a blend of at least two substantially non-toxic solvents, free of halogenated hydrocarbons, is used to dissolve or disperse the agent and dissolve the polymer.
摘要翻译： 一种用于制备可生物降解的微粒包含生物可降解的聚合粘合剂和生物活性剂的过程。 第一阶段中，包含活性剂和聚合物，和第二相通过静态混合器泵送至骤冷液体中以形成包含活性剂的微粒。 优选地，至少两个基本上无毒溶剂，不含卤化烃的共混物，用于溶解或分散剂和溶解聚合物。
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5.发明公开Preparation of biodegradable microparticles containing a biologically active agent 失效Herstellung生物降解药师Mikroteilchen，死亡生物制品公司Mittel enthalten
公开(公告)号：EP1649850A1
公开(公告)日：2006-04-26
申请号：EP05024791.5
申请日：1994-11-18
CPC分类号： A61K9/1694 , A61K9/1647 , B01J13/06 , B01J13/08 , Y10S977/788 , Y10S977/898 , Y10S977/90
摘要： A process of preparing biodegradable microparticles comprising a biodegradable polymeric binder and a biologically active agent. A first phase, comprising the active agent and the polymer, and a second phase are pumped through a static mixer into a quench liquid to form microparticles containing the active agent.
摘要翻译： 一种制备包含可生物降解的聚合物粘合剂和生物活性剂的可生物降解的微粒的方法。 将包含活性剂和聚合物的第一相和第二相通过静态混合器泵送到骤冷液体中以形成含有活性剂的微粒。
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公开(公告)号：EP0904063B1
公开(公告)日：2002-09-04
申请号：EP97923063.8
申请日：1997-05-06
CPC分类号： B01J13/04 , A61K9/1647 , A61K9/1694 , A61K9/5089 , A61K31/519 , Y10T428/2985
摘要： The invention provides a process for the preparation of biodegradable biocompatible microparticles, said process comprising: contacting microparticles comprising a biodegradable biocompatible polymer matrix containing an active (e.g. pharmaceutical or diagnostic) agent and an organic solvent with an aqueous solvent system whereby the content of said organic solvent in said particles is reduced to 2 % or less of the weight of said particles, said solvent system being such as to satisfy at least one of the conditions (a) that it is at an elevated temperature (e.g. from 25 to 40 °C) during at least part of the time that it is in contact with said particles, and (b) that it comprises water and water-miscible solvent for said organic solvent; and recovering said particles from said aqueous solvent system.
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7.发明公开POLY (LACTIDE-CO-GLYCOLIDE)-BASED SUSTAINED RELEASE MICROCAPSULES COMPRISING A POLYPEPTIDE AND A SUGAR 审中-公开MIKROKASPEL聚（丙交酯 - CO-GLYCODLID）的多肽和糖BASIS缓释
公开(公告)号：EP1734935A1
公开(公告)日：2006-12-27
申请号：EP05737702.0
申请日：2005-04-15
发明人： WRIGHT, Steven G. , CHRISTENSON, Troy , YEOH, Thean Y. , RICKEY, Michael E. , HOTZ, Joyce M. , KUMAR, Rajesh , COSTANTINO, Henry R. , SMITH, Christine , LOKENSGARD, David M.
CPC分类号： A61K47/34 , A61K9/0024 , A61K9/1623 , A61K9/1647 , A61K9/1694 , A61K38/2278 , A61K38/26 , A61K47/26 , A61K47/38
摘要： This invention relates to compositions for the sustained release of biologically active polypeptides, and methods of forming and using said compositions, for the sustained release of biologically active polypeptides. The sustained release compositions of this invention comprise a biocompatible polymer having dispersed therein, a biologically active polypeptide and a sugar.
摘要翻译： 本发明涉及组合物为生物活性多肽的持续释放，并形成和使用所说的组合物，对于生物活性多肽的持续释放的方法。 本发明的持续释放组合物包含具有分散在生物相容的聚合物在其中，有生物活性的多肽和糖。
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8.发明授权APPARATUS AND METHOD FOR PREPARING MICROPARTICLES USING IN-LINE SOLVENT EXTRACTION 有权一种面向in-在线溶剂萃取设备及其制造方法的微粒
公开(公告)号：EP1242053B1
公开(公告)日：2005-01-12
申请号：EP00990484.8
申请日：2000-11-03
IPC分类号： A61K9/16
CPC分类号： A61K9/1694 , A61K9/1647 , Y10T428/2989
摘要： An emulsion is formed by combining two phases in a static mixer (140, 235). The outflow of the blending static mixer (130,230). The emulsion is conbined with an extraction liquid in a blending static mixer is combined with additional extraction liquid. The additional extraction liquid and the outlfow of the blending static mixer can be combined in a vessel (160), or through the use of a static mixer manifold (240) that includes a plurality of static mixers.
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公开(公告)号：EP1420762A1
公开(公告)日：2004-05-26
申请号：EP02759445.6
申请日：2002-08-26
CPC分类号： A61K38/09 , A61K9/1641 , A61K9/1647 , A61K9/1682 , A61K9/1694 , A61K9/5089 , A61K31/519 , B01J8/025 , B01J13/08 , B01J13/12 , B01J13/206 , B01J14/00 , B01J19/121 , B01J19/122 , B01J19/2415 , B01J2219/0877
摘要： Methods for preparing microparticles having reduced residual solvent levels, Microparticles are contacted with a non-aqueous washing system to reduce the level of residual solvent in the microparticles, Preferred non-aqueous washing systems include 100% ethanol and a blend of ethanol and heptane. A solvent blend of a hardening solvent and a washing solvent can be used to harden and wash microparticles in a single step, thereby eliminating the need for a post-hardening wash step.
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公开(公告)号：EP1210942A3
公开(公告)日：2004-05-26
申请号：EP02075905.6
申请日：1997-05-06
IPC分类号： A61K9/16 , A61K9/50 , A61K31/517
CPC分类号： A61K9/1647 , A61K9/1694 , B01J13/02
摘要： The invention provides a particulate material comprising microparticles of a biodegradable biocompatible polymeric matrix containing an active agent and an organic solvent, said organic solvent being present in said microparticles at 2% or less of the total weight of said microparticles.
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