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公开(公告)号：US08920836B2
公开(公告)日：2014-12-30
申请号：US10588978
申请日：2005-02-11
申请人： Geoffrey Gerard Hayes , Hassan Mohammad , Harjit Tamber , Malcolm Walden , Steve Whitelock , Helen Kathleen Danagher , Derek Allan Prater
发明人： Geoffrey Gerard Hayes , Hassan Mohammad , Harjit Tamber , Malcolm Walden , Steve Whitelock , Helen Kathleen Danagher , Derek Allan Prater
CPC分类号： A61K9/1694 , A61K9/0053 , A61K9/16 , A61K9/1635 , A61K9/1652 , A61K9/20 , A61K9/2013 , A61K9/2027 , A61K9/2054 , A61K9/2077 , A61K9/2086 , A61K9/2095 , A61K31/485 , B29B9/06 , B29K2033/12 , B29K2105/0085
摘要： A neutral poly(ethyl acrylate, methyl methacrylate) copolymer is employed as a carrier in the manufacture of pharmaceutical formulations containing an active ingredient. The formulations are preferably made by melt extrusion, and can have rubbery characteristics and can exhibit tamper resistance.
摘要翻译： 在制备含有活性成分的药物制剂中使用中性聚（丙烯酸乙酯，甲基丙烯酸甲酯）共聚物作为载体。 制剂优选通过熔融挤出制备，并且可以具有橡胶特性并且可表现出抗窜改性。
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公开(公告)号：US20120141583A1
公开(公告)日：2012-06-07
申请号：US13157093
申请日：2011-06-09
申请人： Richard O. Mannion , William H. Mckenna , Edward P. O'Donnell , Helen Kathleen Danagher , Geoffrey Gerard Hayes , Hassan Mohammad , Derek Allan Prater , Harjit Tamber , Malcom Walden , Steve Whitelock , Wolfgang Fleischer , Udo Hahn , Christof Spitzley , Christian Leuner
发明人： Richard O. Mannion , William H. Mckenna , Edward P. O'Donnell , Helen Kathleen Danagher , Geoffrey Gerard Hayes , Hassan Mohammad , Derek Allan Prater , Harjit Tamber , Malcom Walden , Steve Whitelock , Wolfgang Fleischer , Udo Hahn , Christof Spitzley , Christian Leuner
CPC分类号： A61K9/1694 , A61K9/0053 , A61K9/16 , A61K9/1635 , A61K9/1652 , A61K9/20 , A61K9/2013 , A61K9/2027 , A61K9/2054 , A61K9/2077 , A61K9/2086 , A61K9/2095 , A61K31/485 , B29B9/06 , B29K2033/12 , B29K2105/0085
摘要： Opioid controlled release formulation resistant to alcohol extraction of the opioid.
摘要翻译： 阿片样物质控释制剂耐酒精提取阿片样物质。
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公开(公告)号：US09603802B2
公开(公告)日：2017-03-28
申请号：US12241650
申请日：2008-09-30
申请人： Geoffrey Gerard Hayes , Vincenzo Martinelli , Hassan Mohammad , Derek Allan Prater , Harjit Tamber , Malcolm Walden , Steve Whitelock
发明人： Geoffrey Gerard Hayes , Vincenzo Martinelli , Hassan Mohammad , Derek Allan Prater , Harjit Tamber , Malcolm Walden , Steve Whitelock
IPC分类号： A61K9/16
CPC分类号： A61K9/1635 , A61K9/16 , A61K9/1694 , Y10T428/2982
摘要： The invention relates to a process for preparing a controlled release pharmaceutical extrudate using a melt extruder, wherein the melt extruder comprises a die-head supporting a die-plate in which orifices are located, and a cutter adjacent to the die-head, and wherein the cutter cuts the extruded mix as it emerges under pressure and still molten or softened from the orifices of the die-plate.
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公开(公告)号：US20090029170A1
公开(公告)日：2009-01-29
申请号：US12241650
申请日：2008-09-30
申请人： Geoffrey Gerard Hayes , Vincenzo Martinelli , Hassan Mohammad , Derek Allan Prater , Harjit Tamber , Malcolm Walden , Steve Whitelock
发明人： Geoffrey Gerard Hayes , Vincenzo Martinelli , Hassan Mohammad , Derek Allan Prater , Harjit Tamber , Malcolm Walden , Steve Whitelock
CPC分类号： A61K9/1635 , A61K9/16 , A61K9/1694 , Y10T428/2982
摘要： The invention relates to a process for preparing a controlled release pharmaceutical extrudate using a melt extruder,wherein the melt extruder comprises a die-head supporting a die-plate in which orifices are located, and a cutter adjacent to the die-head, and wherein the cutter cuts the extruded mix as it emerges under pressure and still molten or softened from the orifices of the die-plate.
摘要翻译： 本发明涉及一种使用熔体挤出机制备控释药物挤出物的方法，其中熔融挤出机包括支撑孔的模头和与模头相邻的切割器，其中 挤出的混合物在压力下出现时会切割挤出的混合物，并仍然从模板的孔口熔化或软化。
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公开(公告)号：US20080260815A1
公开(公告)日：2008-10-23
申请号：US11661478
申请日：2005-08-31
申请人： Geoffrey Gerard Hayes , Vincenzo Martinelli , Hassan Mohammad , Harjit Tamber , Malcolm Walden , Steve Whitelock
发明人： Geoffrey Gerard Hayes , Vincenzo Martinelli , Hassan Mohammad , Harjit Tamber , Malcolm Walden , Steve Whitelock
CPC分类号： B29C47/60 , A61K9/145 , A61K9/146 , A61K9/1617 , A61K9/1635 , A61K31/485 , B29C47/0011 , B29C47/6093
摘要： Extrusion of a mix containing a pharmaceutically active agent can be achieved using a plasticising excipient in an amount sufficient to act as plasticiser and also act as lubricant, thereby avoiding the need for inclusion of a lubricant. The invention provides multiparticulates with controlled release properties, substantially free of lubricant. The present invention is preferably directed to extruded multiparticulates containing an opioid such as oxycodone, an ammonium methacrylate copolymer such as Eudragit® RSPO, a plasticising excipient such as preferably stearyl alcohol and a water permeability modifier such as preferably Eudragit® RLPO. The obtained multiparticulates show a release rate profile which is pH-independent.
摘要翻译： 含有药物活性剂的混合物的挤出可以使用足够作为增塑剂的量的增塑赋形剂实现，并且还用作润滑剂，从而避免包含润滑剂的需要。 本发明提供了具有控制释放特性的多颗粒，基本上不含润滑剂。 本发明优选地涉及包含阿片样物质如挤压的多颗粒，例如羟考酮，甲基丙烯酸铵共聚物，例如RSPO，增塑赋形剂如优选硬脂醇，以及水分渗透性改进剂，例如优选RLPO。 所获得的多颗粒显示出与pH无关的释放速率分布。
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公开(公告)号：US09259872B2
公开(公告)日：2016-02-16
申请号：US11661478
申请日：2005-08-31
申请人： Geoffrey Gerard Hayes , Vincenzo Martinelli , Hassan Mohammad , Harjit Tamber , Malcolm Walden , Steve Whitelock
发明人： Geoffrey Gerard Hayes , Vincenzo Martinelli , Hassan Mohammad , Harjit Tamber , Malcolm Walden , Steve Whitelock
CPC分类号： B29C47/60 , A61K9/145 , A61K9/146 , A61K9/1617 , A61K9/1635 , A61K31/485 , B29C47/0011 , B29C47/6093
摘要： Extrusion of a mix containing a pharmaceutically active agent can be achieved using a plasticizing excipient in an amount sufficient to act as plasticizer and also act as lubricant, thereby avoiding the need for inclusion of a lubricant. The invention provides multiparticulates with controlled release properties, substantially free of lubricant. The present invention is preferably directed to extruded multiparticulates containing an opioid such as oxycodone, an ammonium methacrylate copolymer such as Eudragit® RSPO, a plasticizing excipient such as preferably stearyl alcohol and a water permeability modifier such as preferably Eudragit® RLPO. The obtained multiparticulates show a release rate profile which is pH-independent.
摘要翻译： 含有药物活性剂的混合物的挤出可以使用足够充当增塑剂的量的增塑赋形剂实现，并且还用作润滑剂，从而避免包含润滑剂的需要。 本发明提供了具有控制释放特性的多颗粒，基本上不含润滑剂。 本发明优选针对含有阿片样物质如氢可酮，甲基丙烯酸铵共聚物（如RS-RSPO），增塑赋形剂如硬脂醇和水溶性改良剂（例如优选RLPO）的挤出多颗粒。 所获得的多颗粒显示出与pH无关的释放速率分布。
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公开(公告)号：US20050191352A1
公开(公告)日：2005-09-01
申请号：US11056035
申请日：2005-02-11
申请人： Geoffrey Hayes , Vincenzo Martinelli , Hassan Mohammad , Derek Prater , Harjit Tamber , Malcolm Walden , Steve Whitelock
发明人： Geoffrey Hayes , Vincenzo Martinelli , Hassan Mohammad , Derek Prater , Harjit Tamber , Malcolm Walden , Steve Whitelock
CPC分类号： A61K9/1635 , A61K9/16 , A61K9/1694 , Y10T428/2982
摘要： The invention relates to a process for preparing a controlled release pharmaceutical extrudate using a melt extruder, wherein the melt extruder comprises a die-head supporting a die-plate in which orifices are located, and a cutter adjacent to the die-head, and wherein the cutter cuts the extruded mix as it emerges under pressure and still molten or softened from the orifices of the die-plate.
摘要翻译： 本发明涉及一种使用熔体挤出机制备控释药物挤出物的方法，其中熔融挤出机包括支撑孔的模头和与模头相邻的切割器，其中 挤出的混合物在压力下出现时会切割挤出的混合物，并仍然从模板的孔口熔化或软化。
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公开(公告)号：US20060165790A1
公开(公告)日：2006-07-27
申请号：US11314464
申请日：2005-12-20
申请人： Malcolm Walden , Geoffrey Hayes , Hassan Mohammad , Harjit Tamber , Steve Whitelock , Vincenzo Martinelli
发明人： Malcolm Walden , Geoffrey Hayes , Hassan Mohammad , Harjit Tamber , Steve Whitelock , Vincenzo Martinelli
IPC分类号： A61K31/485 , A61K9/22
CPC分类号： A61K9/1635 , A61K9/4808 , A61K31/485
摘要： Multipartulates of oxycodone can be made by extrusion of a blend which suitably contains (a) oxycodone, (b) water-insoluble ammonium methacrylate copolymer, (c) plasticiser, (d) lubricant and (e) water permeability modifier.
摘要翻译： 羟考酮的多部分可以通过挤出适合含有（a）羟考酮，（b）水不溶性甲基丙烯酸铵共聚物，（c）增塑剂，（d）润滑剂和（e）水渗透性改性剂）的共混物来制备。
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公开(公告)号：US20070259045A1
公开(公告)日：2007-11-08
申请号：US11574778
申请日：2006-01-27
申请人： Richard Mannion , William Mckenna , Edward O'Donnell , Helen Danagher , Geoffrey Hayes , Hassan Mohammad , Derek Prater , Harjit Tamber , Walden Malcolm , Steve Whitelock , Wolfgang Fleischer , Udo Hahn , Christof Spitzley , Christian Leuner
发明人： Richard Mannion , William Mckenna , Edward O'Donnell , Helen Danagher , Geoffrey Hayes , Hassan Mohammad , Derek Prater , Harjit Tamber , Walden Malcolm , Steve Whitelock , Wolfgang Fleischer , Udo Hahn , Christof Spitzley , Christian Leuner
IPC分类号： A61K9/00 , A61K31/44 , A61P29/00 , C07D471/00
CPC分类号： A61K9/1652 , A61K9/16 , A61K9/20 , A61K9/2054 , A61K9/2077 , A61K31/485 , A61K45/06
摘要： Disclosed in certain embodiments is a controlled release dosage form comprising a matrix comprising a pharmaceutically acceptable salt of an opioid analgesic in a controlled release material; wherein less than 25% of the opioid salt is released after 1 hour of in-vitro dissolution of the dosage form in 900 ml of Simulated Gastric Fluid with 20% ethanol using a USP Apparatus I (basket) apparatus at 100 rpm at 37 degrees C.°.
摘要翻译： 在某些实施方案中公开了控释剂型，其包含在控释材料中包含阿片样物质镇痛药的药学上可接受的盐的基质; 其中小于25％的阿片样物质盐在使用USP装置I（筐）装置的体外溶解于900ml含20％乙醇的模拟胃液1小时后以100rpm在37℃下释放 。
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公开(公告)号：US20120010231A1
公开(公告)日：2012-01-12
申请号：US13133472
申请日：2009-12-04
IPC分类号： A61K31/485 , A61P29/00 , C07D489/12
CPC分类号： C07D489/12 , A61K9/7023 , A61K31/485 , C07D489/02
摘要： The present invention provides a process for the preparation of a compound of formula (VI), or a salt or derivative thereof, wherein R1 and R2 are independently C1-8 alkyl and * represents a stereocentre.
摘要翻译： 本发明提供制备式（Ⅵ）化合物或其盐或衍生物的方法，其中R 1和R 2独立地为C 1-8烷基且*表示立体中心。
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