公开(公告)号：US20110217383A1

公开(公告)日：2011-09-08

申请号：US13062591

申请日：2008-09-24

申请人： Hans Bär ,  Thomas Fürst ,  Gerhard Renner ,  Michael Gottschalk

发明人： Hans Bär ,  Thomas Fürst ,  Gerhard Renner ,  Michael Gottschalk

IPC分类号： A61K9/50 ,  A61K9/00 ,  A61P25/32 ,  A61P25/36 ,  A61K31/485 ,  A61K31/137 ,  A61K31/222 ,  A61K31/451 ,  A61K31/5377 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/439 ,  A61K31/24 ,  A61K31/4535 ,  A61K31/55 ,  A61K31/445 ,  A61P25/04 ,  B29C43/20

CPC分类号： A61K9/5078

摘要： The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising a core, and an opioid, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40 95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer, and ii) 5 60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250 % by weight of a non-porous inert lubricant, 1 to 35 % by weight of a neutral cellulosic compound and 1 to 25 % by weight of an emulsifier, each calculated on dry weight of the polymer mixture.

摘要翻译： 本发明涉及一种pH依赖性控释药物组合物，其包含核心和阿片样物质，其中所述核心至少涂覆一层涂层，以控制药物组合物的释放，其中所述涂层包含： i）40 95重量％，基于聚合物混合物的干重，至少一种水不溶性基本上中性的乙烯基聚合物，和ii）基于聚合物混合物的干重计，60重量％的至少一种 阴离子聚合物或共聚物，其不溶于低于pH 4.0的缓冲介质，并且至少可溶于pH 7.0至pH 8.0，其特征在于，所述涂层还包含110至250重量％的无孔惰性润滑剂 ，1至35重量％的中性纤维素化合物和1至25重量％的乳化剂，其各自以聚合物混合物的干重计算。

公开(公告)号：US20110229562A1

公开(公告)日：2011-09-22

申请号：US13120112

申请日：2008-09-24

申请人： Hans Bär ,  Thomas Fürst ,  Gerhard Renner ,  Michael Gottschalk

发明人： Hans Bär ,  Thomas Fürst ,  Gerhard Renner ,  Michael Gottschalk

IPC分类号： A61K9/48 ,  B29C43/02 ,  A61K9/00 ,  A61K9/36 ,  A61K9/14 ,  A61K31/138

CPC分类号： A61K9/5078

摘要： The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising at least one pharmaceutical active ingredient, with the exception of opioids, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40-95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer or copolymer, and ii) 5-60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250% by weight of a non-porous inert lubricant, 1 to 35% by weight of at least one neutral cellulosic compound and 1 to 25% by weight of at least one emulsifier, each calculated on dry weight of the polymer mixture.

摘要翻译： 本发明涉及pH依赖性控释药物组合物，其包含除阿片样物质以外的至少一种药物活性成分，其中核心至少涂覆一层涂层，以控制药物组合物的释放，其中涂层 至少一种不溶于水的基本上中性的乙烯基聚合物或共聚物，和ii）5-60重量％，基于干燥的聚合物混合物，i）40-95重量％，基于聚合物混合物的干重， 聚合物混合物的重量，至少一种阴离子聚合物或共聚物，其不溶于低于pH 4.0的缓冲介质中并且可溶于至少在7.0至8.0的范围内，其特征在于所述涂层还包含110至250 重量％的无孔惰性润滑剂，1至35重量％的至少一种中性纤维素化合物和1至25重量％的至少一种乳化剂，其各自以聚合物混合物的干重计算。

公开(公告)号：US09757343B2

公开(公告)日：2017-09-12

申请号：US13062591

申请日：2008-09-24

申请人： Hans Bär ,  Thomas Fürst ,  Gerhard Renner ,  Michael Gottschalk

发明人： Hans Bär ,  Thomas Fürst ,  Gerhard Renner ,  Michael Gottschalk

IPC分类号： A61K9/50

CPC分类号： A61K9/5078

摘要： The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising a core, and an opioid, wherein the core is coated at least by one coating layer, controlling the release of the pharmaceutical composition, wherein the coating layer comprises a polymer mixture of i) 40-95% by weight, based on dry weight of the polymer mixture, of at least one water insoluble essentially neutral vinyl polymer, and ii) 5-60% by weight, based on dry weight of the polymer mixture, of at least one anionic polymer or copolymer, which is insoluble in a buffered medium below pH 4.0 and soluble at least in the range from pH 7.0 to pH 8.0, characterized in that the coating layer further comprises 110 to 250% by weight of a non-porous inert lubricant, 1 to 35% by weight of a neutral cellulosic compound and 1 to 25% by weight of an emulsifier, each calculated on dry weight of the polymer mixture.

公开(公告)号：US09730899B2

公开(公告)日：2017-08-15

申请号：US13256694

申请日：2009-03-18

申请人： Hans Bär ,  Thomas Fürst ,  Gerhard Renner ,  Michael Gottschalk

发明人： Hans Bär ,  Thomas Fürst ,  Gerhard Renner ,  Michael Gottschalk

IPC分类号： A61K9/52 ,  A61K9/14 ,  A61K31/485 ,  A61K9/50

CPC分类号： A61K9/5078

摘要： The invention relates to a controlled release pharmaceutical composition, comprising a core, comprising a pharmaceutical active ingredient, whereby the core is coated by an ethanol resistance conferring coating layer which has the effect of conferring the release profile of the pharmaceutical active ingredient to be resistant against the influence of ethanol, whereby the ethanol resistance conferring coating layer comprises at least 70% by weight of a mixture of a polymeric portion a) and an excipients portion b), with the polymeric portion a) is consisting of a water insoluble essentially neutral vinyl polymer or vinyl copolymer and the excipients portion b) is consisting of the excipients b1) 100 to 250% by weight of a non-porous inert lubricant, b2) 1 to 35% by weight of a cellulosic compound, b3) 0.1 to 25% by weight of an emulsifier and additionally or alternatively to b3), b4) 0.1 to 30% by weight of a plasticizer whereby the excipients of the excipients portion b) are each calculated on the dry weight of the polymer portion a).