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1. 发明授权

US09011907B2 Coated pharmaceutical or nutraceutical preparation with enhanced pulsed active substance release 有权
标题翻译：具有增强脉冲活性物质释放的涂层药物或营养制剂
公开(公告)号：US09011907B2
公开(公告)日：2015-04-21
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： A61K9/64 , A61K9/20 , A61K9/50
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％，以及（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的（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）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。

2. 发明申请

US20100255092A1 COATED PHARMACEUTICAL OR NUTRACEUTICAL PREPARATION WITH ACCELERATED CONTROLLED ACTIVE SUBSTANCE RELEASE 审中-公开
标题翻译：加速控制的活性物质释放的包装药物或营养制剂
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。

3. 发明申请

US20100291202A1 COATED PHARMACEUTICAL OR NUTRACEUTICAL PREPARATION WITH ENHANCED PULSED ACTIVE SUBSTANCE RELEASE 有权
标题翻译：具有增强脉冲活性物质释放的包衣制药或营养制剂
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。

4. 发明申请

US20100247639A1 COATED PHARMACEUTICAL OR NUTRACEUTICAL PREPARATION WITH ENHANCED ACTIVE SUBSTANCE RELEASE IN THE COLON 有权
标题翻译：涂层药物或营养制剂与增强活性物质释放在殖民地
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。

5. 发明授权

US08465769B2 Pharmaceutical composition with controlled active ingredient release for active ingredients with good solubility in water 有权
标题翻译：具有控制活性成分释放活性成分，具有良好溶解性的药物组合物
公开(公告)号：US08465769B2
公开(公告)日：2013-06-18
申请号：US11695848
申请日：2007-04-03
申请人： Hans-Ulrich Petereit , Hema Ravishankar , Shradda Bodinge
发明人： Hans-Ulrich Petereit , Hema Ravishankar , Shradda Bodinge
IPC分类号： 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％的丙烯酸或甲基丙烯酸的C 1〜C 4 - 烷基酯和7〜2重量％的具有季铵基的（甲基）丙烯酸酯单体的自由基聚合单元组成，烷基，其中所述活性成分在20℃下在水中的溶解度为至少10g / l，并且所述涂层包含平均粒度在1至50μm之间的二氧化硅颗粒。

6. 发明申请

US20100221324A1 PH-DEPENDENT CONTROLLED RELEASE PHARMACEUTICAL COMPOSITION FOR NON-OPIOIDS WITH RESISTANCE AGAINST THE INFLUENCE OF ETHANOL 有权
标题翻译：对依赖于乙醇的影响的非依赖性药物的PH依赖性控制释放药物组合物
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。

7. 发明申请

US20080152719A1 Multiparticulate Pharmaceutical Form Comprising Pellets With a Matrix Which Influences the Delivery of a Modulatory Substance 审中-公开
标题翻译：含有影响调节物质输送的基质的颗粒的多微粒药物形式
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。

8. 发明授权

US09237760B2 Coated pharmaceutical or nutraceutical preparation with enhanced active substance release in the colon 有权
标题翻译：在结肠中具有增强的活性物质释放的涂覆的药物或营养制剂
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。

9. 发明授权

US09700520B2 PH-dependent controlled release pharmaceutical opioid composition with resistance against the influence of ethanol 有权
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.

10. 发明授权

US09555006B2 PH-dependent controlled release pharmaceutical composition for non-opioids with resistance against the influence of ethanol 有权
标题翻译：对依赖乙醇影响的非阿片样物质的PH依赖性控释药物组合物
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。

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