公开(公告)号：US20100291202A1

公开(公告)日：2010-11-18

申请号：US12742945

申请日：2008-02-01

申请人： Hema Ravishankar ,  Shradda Bodinge ,  Hans-Ulrich Petereit

发明人： Hema Ravishankar ,  Shradda Bodinge ,  Hans-Ulrich Petereit

IPC分类号： A61K47/32 ,  A61K9/22 ,  A61K9/52 ,  A61P43/00

CPC分类号： A61K9/5078 ,  A61K9/2081

摘要： The present invention relates to a pharmaceutical or nutraceutical preparation comprising a) a core containing a pharmaceutically or nutraceutically active substance and a substance that acts in a modulatory manner with regard of the release of pharmaceutically or nutraceutically active substances; and b) a controlling layer surrounding the core comprising i) 55 to 92% by weight based on the total weight of (meth)acrylic copolymers present in the layer of one or a mixture of a plurality of (meth)acrylate copolymers composed of 80 to 98% by weight based on the weight of the (meth)acrylic copolymer of structural units derived from C1 to C4 alkyl esters of (meth)acrylic acid and 2 to 20% by weight based on the weight of the (meth)acrylic copolymer of structural units derived from (meth)acrylate monomers with a quaternary ammonium group in the alkyl radical; and ii) 8 to 45% by weight based on the total weight of (meth)acrylic copolymers present in the layer of one or a mixture of a plurality of (meth)acrylate copolymers composed of more than 5 to 59% by weight based on the weight of the copolymer of structural units derived from acrylic acid or methacrylic acid and to tablets or capsules comprising same.

摘要翻译： 本发明涉及一种药物或营养制剂，其包含a）含有药学上或营养活性物质的核心和在释放药学或营养活性物质方面以调节方式起作用的物质; 和b）围绕芯的控制层，其包含i）55至92重量％，基于存在于由80重量份组成的多个（甲基）丙烯酸酯共聚物的一种或多种混合物的层中的（甲基）丙烯酸共聚物的总重量 至（甲基）丙烯酸共聚物的重量比为基于（甲基）丙烯酸的C1至C4烷基酯的结构单元的（甲基）丙烯酸共聚物的重量计为98重量％，基于（甲基）丙烯酸共聚物的重量为2至20重量％ 衍生自烷基中具有季铵基团的（甲基）丙烯酸酯单体的结构单元; 和ii）8至45重量％，基于存在于由多于5至59重量％组成的多个（甲基）丙烯酸酯共聚物的一种或多种（甲基）丙烯酸酯共聚物的层中的（甲基）丙烯酸共聚物）的总重量，基于 衍生自丙烯酸或甲基丙烯酸的结构单元的共聚物与包含其的片剂或胶囊的重量。

公开(公告)号：US20100247639A1

公开(公告)日：2010-09-30

申请号：US12742842

申请日：2008-02-01

申请人： Hema Ravishankar ,  Shradda Bodinge ,  Hans-Ulrich Petereit

发明人： Hema Ravishankar ,  Shradda Bodinge ,  Hans-Ulrich Petereit

IPC分类号： A61K9/00 ,  A61K9/32 ,  A61K9/48 ,  A61K31/606

CPC分类号： A23P10/30 ,  A23L27/72 ,  A61K9/5078

摘要： The present invention relates to a pharmaceutical or nutraceutical preparation comprising a) a core containing a pharmaceutically or nutraceutically active substance; and b) an inner controlling layer surrounding the core comprising i) one or a mixture of a plurality of (meth)acrylate copolymers bearing a cationic group or a group that can be converted to a cationic group; and ii) one or a mixture of a plurality of polymers or copolymers bearing an anionic group or group that can be converted to an anionic group; and c) an outer controlling layer comprising one or a mixture of a plurality of polymers or copolymers bearing an anionic group or group that can be converted to an anionic group and to tablets or capsules comprising same.

摘要翻译： 本发明涉及药物或营养制剂，其包含a）含有药学或营养活性物质的核心; 和b）围绕所述芯的内部控制层，包括i）一个或多个带有阳离子基团的甲基丙烯酸酯共聚物或可转化为阳离子基团的基团的混合物; 和ii）可以转化成阴离子基团的多个带有阴离子基团或基团的聚合物或共聚物的一种或多种混合物; 和c）包含一个或多个带有阴离子基团的聚合物或共聚物的混合物或可以转化成阴离子基团的外部控制层和包含其的片剂或胶囊的外部控制层。

公开(公告)号：US20100221324A1

公开(公告)日：2010-09-02

申请号：US12678429

申请日：2007-09-25

申请人： Hans-Ulrich Petereit ,  Hema Ravishankar ,  Ashwini Samel

发明人： Hans-Ulrich Petereit ,  Hema Ravishankar ,  Ashwini Samel

IPC分类号： A61K9/14 ,  A61K9/00 ,  A61K31/138 ,  A61K9/22 ,  A61K9/58

CPC分类号： A61K9/5078 ,  A61K9/501 ,  A61K9/5026

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 contains 110 to 250% by weight, calculated on dry weight of the polymer mixture, of a non-porous inert lubricant and the is present in an amount of at least 60% by weight calculated on the weight of core.

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， 聚合物混合物的至少一种阴离子聚合物或共聚物的重量，其不溶于低于pH 4.0的缓冲介质并且可溶于至少在7.0至8.0的范围内。 其特征在于，所述涂层还包含110-250重量％，以聚合物混合物的干重计算的非多孔惰性润滑剂，并且其含量以至少60重量％的量存在，以重量计 核心。

公开(公告)号：US20080152719A1

公开(公告)日：2008-06-26

申请号：US11815677

申请日：2006-03-03

申请人： Hans-Ulrich Petereit ,  Rosario Lizio ,  Hema Ravishankar ,  Ashwini Samel

发明人： Hans-Ulrich Petereit ,  Rosario Lizio ,  Hema Ravishankar ,  Ashwini Samel

IPC分类号： A61K9/16

CPC分类号： A61K9/5078 ,  A61K9/2081 ,  A61K9/5015 ,  A61K9/5026

摘要： The invention relates to a multiparticulate pharmaceutical form, comprising pellets with a multilayer structure for controlled active ingredient release, comprising a) optionally a neutral core (nonpareilles), b) an inner controlling layer comprising a substance having a modulating effect, which is embedded in a matrix which influences the delivery of the modulatory substance and which comprises pharmaceutically usable polymers, waxes, resins and/or proteins, and where appropriate an active ingredient, c) an active ingredient layer comprising an active pharmaceutical ingredient and, where appropriate, a substance having a modulating effect, d) an outer controlling layer comprising at least 60% by weight of one or a mixture of a plurality of (meth) acrylate copolymers where the outer controlling layer has a thickness from 20 to less than 55 μm and contains 0,1 to 10% by weight of glycerol monostearate, where the multiparticulate pharmaceutical form contains 20 to 60% by weight of the pellets, which are compressed in mixture with 80 to 40% by weight of an outer phase which consists from 50 to 100% by weight of a cellulose or a derivate of cellulose and optionally 0 to 50% by weight of further pharmaceutical excipients.

摘要翻译： 本发明涉及多颗粒药物形式，其包含具有用于受控活性成分释放的多层结构的颗粒，其包含a）任选的中性核心（非矫正剂），b）包含调节作用的物质的内部控制层，其嵌入 影响调节物质递送的基质，其包含药学上可用的聚合物，蜡，树脂和/或蛋白质，以及适当的活性成分，c）包含活性药物成分和适当的物质的活性成分层 具有调节作用，d）包含至少60重量％的多个（甲基）丙烯酸酯共聚物中的一种或多种（甲基）丙烯酸酯共聚物的混合物的外部控制层，其中外部控制层具有20至小于55μm的厚度并且包含0 ，1至10重量％的甘油单硬脂酸酯，其中多颗粒药物形式包含20至60重量％的p 它们与80至40重量％的外相一起被压制，所述外相由50-100重量％的纤维素或纤维素衍生物和任选的0至50重量％的其它药用赋形剂组成。

公开(公告)号：US09700520B2

公开(公告)日：2017-07-11

申请号：US12678406

申请日：2007-09-25

申请人： Hans-Ulrich Petereit ,  Hema Ravishankar ,  Ashwini Samel

发明人： Hans-Ulrich Petereit ,  Hema Ravishankar ,  Ashwini Samel

IPC分类号： A61K9/50

CPC分类号： A61K9/5078 ,  A61K9/501 ,  A61K9/5026

摘要： The invention relates to a pH-dependent controlled release pharmaceutical composition, comprising a core, comprising at least one pharmaceutical active ingredient, which is 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 contains 110 to 250% by weight, calculated on dry weight of the polymer mixture, of a non-porous inert lubricant and the coating layer is present in an amount of at least 60% by weight calculated on the weight of core.

公开(公告)号：US09555006B2

公开(公告)日：2017-01-31

申请号：US12678429

申请日：2007-09-25

申请人： Hans-Ulrich Petereit ,  Hema Ravishankar ,  Ashwini Samel

发明人： Hans-Ulrich Petereit ,  Hema Ravishankar ,  Ashwini Samel

IPC分类号： A61K9/50

CPC分类号： A61K9/5078 ,  A61K9/501 ,  A61K9/5026

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 contains 110 to 250% by weight, calculated on dry weight of the polymer mixture, of a non-porous inert lubricant and the is present in an amount of at least 60% by weight calculated on the weight of core.

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， 聚合物混合物的至少一种阴离子聚合物或共聚物的重量，其不溶于低于pH 4.0的缓冲介质并且可溶于至少在7.0至8.0的范围内。 其特征在于，所述涂层还包含110-250重量％，以聚合物混合物的干重计算的非多孔惰性润滑剂，并且其含量以至少60重量％的量存在，以重量计 核心。

公开(公告)号：US20130142877A1

公开(公告)日：2013-06-06

申请号：US13696746

申请日：2011-03-03

申请人： Pravin Nalawade ,  Smitha Shetty ,  Hema Ravishankar ,  Shripad Gadhinglajkar ,  Andreas Gryczke ,  Hans-Ulrich Petereit ,  Kathrin Nollenberger

发明人： Pravin Nalawade ,  Smitha Shetty ,  Hema Ravishankar ,  Shripad Gadhinglajkar ,  Andreas Gryczke ,  Hans-Ulrich Petereit ,  Kathrin Nollenberger

IPC分类号： A61K47/32 ,  A61K31/427 ,  A61K31/513

CPC分类号： A61K31/513 ,  A61K9/145 ,  A61K9/146 ,  A61K9/1635 ,  A61K9/4866 ,  A61K31/427

摘要： The invention relates to a pharmaceutical dosage form comprising one or more antiretroviral active ingredients in the form of a solid dispersion or solid solution in a matrix, wherein said matrix comprises an amino(meth)acrylate copolymer, characterized in that the matrix does not contain any essential amounts of pharmaceutically acceptable surfactants with an HLB value from 12 to 18 and in that the matrix comprises a mono carboxylic acid or an alcohol with 12 to 22 carbon atoms or both.

摘要翻译： 本发明涉及药物剂型，其包含一种或多种基质中固体分散体或固体溶液形式的抗逆转录病毒活性成分，其中所述基质包含氨基（甲基）丙烯酸酯共聚物，其特征在于所述基质不含任何 必需量的HLB值为12至18的药学上可接受的表面活性剂，并且基质包含单羧酸或具有12至22个碳原子的醇或两者。

公开(公告)号：US20100255092A1

公开(公告)日：2010-10-07

申请号：US12742263

申请日：2008-02-01

申请人： Hema Ravishankar ,  Hans-Ulrich Petereit ,  Shradda Bodinge

发明人： Hema Ravishankar ,  Hans-Ulrich Petereit ,  Shradda Bodinge

IPC分类号： A61K9/32 ,  A61K9/00 ,  A61K31/522 ,  A61P43/00

CPC分类号： A61K9/5026 ,  A61K9/5078

摘要： The present invention relates to pharmaceutical or nutraceutical preparations comprising a) a core containing a pharmaceutically or nutraceutically active substance; and b) a controlling layer surrounding the core comprising i) 55 to 92% by weight based on the total weight of (meth)acrylic copolymers present in the layer of one or a mixture of a plurality of (meth)acrylate copolymers composed of 80 to 98% by weight based on the weight of the (meth)acrylic copolymer of structural units derived from Ci to C4 alkyl esters of (meth)acrylic acid and 2 to 20% by weight based on the weight of the (meth)acrylic copolymer of structural units derived from (meth)acrylate monomers with a quaternary ammonium group in the alkyl radical; and ii) 8 to 45% by weight based on the total weight of (meth)acrylic copolymers present in the layer of one or a mixture of a plurality of (meth)acrylate copolymers composed of more than 5 to 59% by weight based on the weight of the copolymer of structural units derived from acrylic acid or methacrylic acid, and to tablets and capsules containing same.

摘要翻译： 本发明涉及药物或营养制剂，其包含a）含有药学或营养物质活性物质的核心; 和b）围绕芯的控制层，其包含i）55至92重量％，基于存在于由80重量份组成的多个（甲基）丙烯酸酯共聚物的一种或多种混合物的层中的（甲基）丙烯酸共聚物的总重量 至（甲基）丙烯酸共聚物的重量比为基于（甲基）丙烯酸的C 1〜C 4烷基酯的结构单元的（甲基）丙烯酸共聚物的重量为98重量％，基于（甲基）丙烯酸共聚物的重量为2〜20重量％ 衍生自烷基中具有季铵基团的（甲基）丙烯酸酯单体的结构单元; 和ii）8至45重量％，基于存在于由多于5至59重量％组成的多个（甲基）丙烯酸酯共聚物的一种或多种（甲基）丙烯酸酯共聚物的层中的（甲基）丙烯酸共聚物）的总重量，基于 衍生自丙烯酸或甲基丙烯酸的结构单元的共聚物的重量，以及含有它们的片剂和胶囊的重量。

公开(公告)号：US20080044470A1

公开(公告)日：2008-02-21

申请号：US11695848

申请日：2007-04-03

申请人： Hans-Ulrich Petereit ,  Hema Ravishankar ,  Shraddh Bodinge

发明人： Hans-Ulrich Petereit ,  Hema Ravishankar ,  Shraddh Bodinge

IPC分类号： A61K47/08 ,  A61K47/12 ,  A61K9/28 ,  A61K9/48

CPC分类号： A61K9/5078 ,  A61K9/5026

摘要： A pharmaceutical preparation comprising: a) a core with an active ingredient and with an organic acid and/or the salt of an organic acid; and b) a coating which envelops the core and which comprises a polymer content of (meth)acrylate copolymers which have not more than 15% by weight of cationic or anionic groups, and which comprises at least 60% by weight of a (meth)acrylate copolymer which is composed of free-radically polymerized units of 93 to 98% by weight C1- to C4-alkyl esters of acrylic or of methacrylic acid and 7 to 2% by weight (meth)acrylate monomers having a quaternary ammonium group in the alkyl radical, wherein the active ingredient has a solubility in water of at least 10 g/l at 20° C. and the coating comprises silicon dioxide particles having an average particle size in the range from 1 to 50 μm.

摘要翻译： 一种药物制剂，其包含：a）具有活性成分和有机酸和/或有机酸盐的核心; 和b）包封芯的涂层，其包含具有不超过15重量％的阳离子或阴离子基团的（甲基）丙烯酸酯共聚物的聚合物含量，并且其包含至少60重量％的（甲基）丙烯酸酯共聚物， 丙烯酸酯共聚物，其由93至98重量％的C 1〜C 4 - 丙烯酸或甲基丙烯酸的C 4 - 烷基酯的自由基聚合单元和7至 2重量％的在烷基中具有季铵基团的（甲基）丙烯酸酯单体，其中活性成分在20℃下在水中的溶解度至少为10g / l，并​​且涂层包含具有平均值的二氧化硅颗粒 粒径在1〜50μm的范围内。

公开(公告)号：US09237760B2

公开(公告)日：2016-01-19

申请号：US12742842

申请日：2008-02-01

申请人： Hema Ravishankar ,  Shraddha Bodinge ,  Hans-Ulrich Petereit

发明人： Hema Ravishankar ,  Shraddha Bodinge ,  Hans-Ulrich Petereit

IPC分类号： A61K9/00 ,  A61K9/28 ,  A61K9/48 ,  A23L1/00 ,  A23L1/22 ,  A61K9/50

CPC分类号： A23P10/30 ,  A23L27/72 ,  A61K9/5078

摘要： The present invention relates to a pharmaceutical or nutraceutical preparation comprising a) a core containing a pharmaceutically or nutraceutically active substance; and b) an inner controlling layer surrounding the core comprising i) one or a mixture of a plurality of (meth)acrylate copolymers bearing a cationic group or a group that can be converted to a cationic group; and ii) one or a mixture of a plurality of polymers or copolymers bearing an anionic group or group that can be converted to an anionic group; and c) an outer controlling layer comprising one or a mixture of a plurality of polymers or copolymers bearing an anionic group or group that can be converted to an anionic group and to tablets or capsules comprising same.

摘要翻译： 本发明涉及药物或营养制剂，其包含a）含有药学或营养活性物质的核心; 和b）围绕所述芯的内部控制层，包括i）一个或多个带有阳离子基团的甲基丙烯酸酯共聚物或可转化为阳离子基团的基团的混合物; 和ii）可以转化成阴离子基团的多个带有阴离子基团或基团的聚合物或共聚物的一种或多种混合物; 和c）包含一个或多个带有阴离子基团的聚合物或共聚物的混合物或可以转化成阴离子基团的外部控制层和包含其的片剂或胶囊的外部控制层。