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1. 发明申请

US20130142877A1 PHARMACEUTICAL DOSAGE FORM COMPRISING ONE OR MORE ANTIRETROVIRAL ACTIVE INGREDIENTS 审中-公开
标题翻译：包含一种或多种抗血小板活性成分的药物剂型
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。

2. 发明申请

US20080206324A1 PELLETS HAVING AN ACTIVE COMPOUND MATRIX AND A POLYMER COATING, AND A PROCESS FOR THE PRODUCTION OF THE PELLETS 审中-公开
标题翻译：具有活性化合物基质和聚合物涂料的片剂以及生产小片剂的方法
公开(公告)号：US20080206324A1
公开(公告)日：2008-08-28
申请号：US12030377
申请日：2008-02-13
申请人： Andreas Gryczke , Hans-Ulrich Petereit , Christian Meier , Kathrin Nollenberger , Christian Brunnengraber , Andreas Klosendorf , Reinhard Menzel
发明人： Andreas Gryczke , Hans-Ulrich Petereit , Christian Meier , Kathrin Nollenberger , Christian Brunnengraber , Andreas Klosendorf , Reinhard Menzel
IPC分类号： A61K9/48 , A61K9/14 , A61K9/32
CPC分类号： A61K9/1635 , A61K9/5026 , A61K31/52
摘要： An active compound-containing pellet has a polymer coating of an anionic (meth)acrylate copolymer and a pharmaceutically active substance, embedded in a polymer matrix of one or more polymers, a particle size in the range from 300 to 1100 μm, a friability of at most 0.1%, measured using 200 g of pellets in a screening machine having a 200 μm screen, a screening diameter of 20 cm and 1.5 mm shaking amplitude at a shaking frequency of 50 l/sec for 10 min in the presence of six rubber cubes having a 1.8 cm edge length, with the proviso that the pellet releases no more than 10% of the active compound in a release test according to USP in artificial gastric juice at pH 1.2 after 120 min.
摘要翻译：含活性化合物的颗粒具有嵌入在一种或多种聚合物的聚合物基质中的阴离子（甲基）丙烯酸酯共聚物和药物活性物质的聚合物涂层，粒度在300至1100μm的范围内，脆性在具有200μm筛网的筛选机中使用200g粒料测量，至少0.1％，筛选直径为20cm和1.5mm，振荡频率为50l / sec，在六个橡胶存在下摇动10分钟具有1.8厘米边缘长度的立方体，条件是在120分钟后pH 1.2的人造胃液中，根据USP的释放试验中，颗粒释放不超过10％的活性化合物。

3. 发明申请

US20090011007A1 Pharmaceutical Compositions Containing Mixtures of Polymers and Active Agents Poorly Soluble in Water 审中-公开
标题翻译：含有聚合物和活性剂混合物的药物组合物难溶于水
公开(公告)号：US20090011007A1
公开(公告)日：2009-01-08
申请号：US12159538
申请日：2007-01-17
申请人： Christian Meier , Kathrin Nollenberger , Andreas Gryczke , Hans-Ulrich Petereit , Jennifer Dressman
发明人： Christian Meier , Kathrin Nollenberger , Andreas Gryczke , Hans-Ulrich Petereit , Jennifer Dressman
IPC分类号： A61K9/48 , A61K47/00 , A61K47/38 , A61K31/4418 , A61K9/14 , A61K9/20
CPC分类号： A61K9/2027 , A61K9/1635 , A61K9/1652 , A61K9/2054 , A61K9/2077 , A61K9/5084
摘要： The invention relates to a pharmaceutical composition comprising a mixture of at least one cationic, water-soluble (meth)acrylate copolymer, at least one water-insoluble polymer and at least one active ingredient having a solubility in demineralized water of 3.3 g/l or less, characterized in that the water-insoluble polymer and the active ingredient are present in a ratio of at most 3.5 to 1 parts by weight, and the pharmaceutical composition has the property of releasing the active ingredient present in a medium buffered to pH 1.2 in dissolved form in a concentration which, after 2 hours at pH 1.2, corresponds to at least sixteen times the solubility value of the active ingredient alone at pH 1.2.
摘要翻译：本发明涉及药物组合物，其包含至少一种阳离子，水溶性（甲基）丙烯酸酯共聚物，至少一种水不溶性聚合物和在软化水中溶解度为3.3g / l的至少一种活性成分的混合物或其特征在于，水不溶性聚合物和活性成分以至多3.5至1重量份的比例存在，并且药物组合物具有释放缓冲至pH 1.2的培养基中存在的活性成分的性质溶解形式的浓度，其在pH2.2下2小时后对应于在pH1.2下单独的活性成分的溶解度值的至少十六倍。

4. 发明申请

US20120208832A1 PROCESS FOR CONVERTING A SOLID (METH)ACRYLATE COPOLYMER INTO A DISPERSED FORM BY MEANS OF A DISPERSING AGENT 有权
标题翻译：通过分散剂将固体（甲基）丙烯酸酯共聚物转化成分散形式的方法
公开(公告)号：US20120208832A1
公开(公告)日：2012-08-16
申请号：US13504527
申请日：2009-11-16
申请人： Erna Roth , Ruediger Alexowsky , Hans-Ulrich Petereit , Kathrin Nollenberger , Christian Meier
发明人： Erna Roth , Ruediger Alexowsky , Hans-Ulrich Petereit , Kathrin Nollenberger , Christian Meier
IPC分类号： A61K47/32 , C08K5/11 , C08K5/1535 , A61P11/00 , C08K5/41 , C09D105/00 , A61K31/522 , C08L5/00 , C08K5/06
CPC分类号： C08J3/03 , A61K9/284 , A61K9/5026 , A61K9/5089 , C08J3/05 , C08J2333/14
摘要： The present invention provides a process for converting a solid (meth)acrylate copolymer into a dispersed form by preparing an aqueous dispersion comprising the components (a) a (meth)acrylate copolymer which is composed of free-radical polymerized methyl methacrylate, ethylacrylate and a salt of 2-trimethylammoniumethyl methacrylate, present in solid form as a powder or as a granulate, (b) up to 50% by weight calculated on the (meth)acrylate copolymer (a) of a dispersing agent selected from the groups of (b) i) plasticizers in combination with emulsifiers and/or (b) ii) pharmaceutically acceptable carbohydrates having 6 to 18 carbon atoms with a functional group and (c) water by mixing the components (a), (b) and (c) to give a suspension which becomes an aqueous dispersion during the conversion of the solid (meth)acrylate copolymer into the dispersed form, characterized in that, the (meth)acrylate copolymer is converted into the dispersed form by means of the presence of the dispersing agent at a temperature of less than 50° C.
摘要翻译：本发明提供了一种将固体（甲基）丙烯酸酯共聚物转化成分散形式的方法，其中制备含有（a）（甲基）丙烯酸酯共聚物的组分的水性分散体，该组分由自由基聚合的甲基丙烯酸甲酯，丙烯酸乙酯和以甲基丙烯酸2-三甲基铵乙酯为盐，粉末形式为固体形式，或以颗粒形式存在，（b）按（b）所示的分散剂的（甲基）丙烯酸酯共聚物（a）计算的至多50重量％）i）与乳化剂组合的增塑剂和/或（b）ii）具有官能团的具有6至18个碳原子的药学上可接受的碳水化合物和（c）通过将组分（a），（b）和（c）得到在将固体（甲基）丙烯酸酯共聚物转化成分散形式时成为水分散体的悬浮液，其特征在于，通过存在分散体将（甲基）丙烯酸酯共聚物转化为分散形式 g试剂在低于50℃的温度下

5. 发明授权

US09284416B2 Process for converting a solid (meth)acrylate copolymer into a dispersed form by means of a dispersing agent 有权
标题翻译：通过分散剂将固体（甲基）丙烯酸酯共聚物转化为分散形式的方法
公开(公告)号：US09284416B2
公开(公告)日：2016-03-15
申请号：US13504527
申请日：2009-11-16
申请人： Erna Roth , Ruediger Alexowsky , Hans-Ulrich Petereit , Kathrin Nollenberger , Christian Meier
发明人： Erna Roth , Ruediger Alexowsky , Hans-Ulrich Petereit , Kathrin Nollenberger , Christian Meier
IPC分类号： A61K47/32 , C08K5/11 , C08K5/1535 , A61P11/00 , C08K5/41 , C09D105/00 , A61K31/522 , C08L5/00 , C08K5/06 , C08J3/03 , A61K9/50 , C08J3/05 , A61K9/28
CPC分类号： C08J3/03 , A61K9/284 , A61K9/5026 , A61K9/5089 , C08J3/05 , C08J2333/14
摘要： The present invention provides a process for converting a solid (meth)acrylate copolymer into a dispersed form by preparing an aqueous dispersion comprising the components (a) a (meth)acrylate copolymer which is composed of free-radical polymerized methyl methacrylate, ethylacrylate and a salt of 2-trimethylammoniumethyl methacrylate, present in solid form as a powder or as a granulate, (b) up to 50% by weight calculated on the (meth)acrylate copolymer (a) of a dispersing agent selected from the groups of (b) i) plasticizers in combination with emulsifiers and/or (b) ii) pharmaceutically acceptable carbohydrates having 6 to 18 carbon atoms with a functional group and (c) water by mixing the components (a), (b) and (c) to give a suspension which becomes an aqueous dispersion during the conversion of the solid (meth)acrylate copolymer into the dispersed form, characterized in that, the (meth)acrylate copolymer is converted into the dispersed form by means of the presence of the dispersing agent at a temperature of less than 50° C.
摘要翻译：本发明提供了一种将固体（甲基）丙烯酸酯共聚物转化成分散形式的方法，其中制备含有（a）（甲基）丙烯酸酯共聚物的组分的水性分散体，该组分由自由基聚合的甲基丙烯酸甲酯，丙烯酸乙酯和以甲基丙烯酸2-三甲基铵乙酯为盐，粉末形式为固体形式，或以颗粒形式存在，（b）按（b）所示的分散剂的（甲基）丙烯酸酯共聚物（a）计算的至多50重量％）i）与乳化剂组合的增塑剂和/或（b）ii）具有官能团的具有6至18个碳原子的药学上可接受的碳水化合物和（c）通过将组分（a），（b）和（c）得到在将固体（甲基）丙烯酸酯共聚物转化成分散形式时成为水分散体的悬浮液，其特征在于，通过存在分散体将（甲基）丙烯酸酯共聚物转化为分散形式 g试剂在低于50℃的温度下

6. 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。

7. 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。

8. 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。

9. 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。

10. 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.

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