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公开(公告)号：US08765152B2
公开(公告)日：2014-07-01
申请号：US13580033
申请日：2010-02-25
申请人： Rosario Lizio , Michael Gottschalk , Michael Damm , Norbert Windhab , Melanie Liefke , Guenter Schmitt , Erna Roth , Ruediger Alexowsky
发明人： Rosario Lizio , Michael Gottschalk , Michael Damm , Norbert Windhab , Melanie Liefke , Guenter Schmitt , Erna Roth , Ruediger Alexowsky
CPC分类号： A61K9/1676 , A61K9/5026 , A61K9/5042 , A61K9/5078 , A61K31/727 , A61K38/11 , A61K38/168
摘要： The invention relates to a pharmaceutical or nutraceutical formulation comprising a core, comprising an active pharmaceutical or nutraceutical ingredient, a penetration promoter and a bioavailability promoting agent, and a polymeric coating for the gastrointestinal targeted release of the active ingredient, characterized in that the bioavailability promoting agent is a pharmaceutically acceptable inhibitor of proteolytic enzymes, which increases the oral bioavailability of the active ingredient by a factor of at least five, compared to a corresponding formulation without the bioavailability promoting agent.
摘要翻译： 本发明涉及包含核心的药物或营养制剂，其包含活性药物或营养成分，渗透促进剂和生物利用度促进剂，以及用于胃肠靶向释放活性成分的聚合物涂层，其特征在于所述生物利用度促进 药剂是药学上可接受的蛋白水解酶抑制剂，与没有生物利用度促进剂的相应制剂相比，其将活性成分的口服生物利用度提高至少5倍。
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公开(公告)号：US20120315334A1
公开(公告)日：2012-12-13
申请号：US13580033
申请日：2010-02-25
申请人： Rosario Lizio , Michael Gottschalk , Michael Damm , Norbert Windhab , Melanie Liefke , Guenter Schmitt , Erna Roth , Ruediger Alexowsky
发明人： Rosario Lizio , Michael Gottschalk , Michael Damm , Norbert Windhab , Melanie Liefke , Guenter Schmitt , Erna Roth , Ruediger Alexowsky
IPC分类号： A61K9/00 , A61K31/7088 , A61K9/14 , A61K38/11 , A61K31/727 , A61K38/02 , A61K31/715
CPC分类号： A61K9/1676 , A61K9/5026 , A61K9/5042 , A61K9/5078 , A61K31/727 , A61K38/11 , A61K38/168
摘要： The invention relates to a pharmaceutical or nutraceutical formulation comprising a core, comprising an active pharmaceutical or nutraceutical ingredient, a penetration promoter and a bioavailability promoting agent, and a polymeric coating for the gastrointestinal targeted release of the active ingredient, characterized in that the bioavailability promoting agent is a pharmaceutically acceptable inhibitor of proteolytic enzymes, which increases the oral bioavailability of the active ingredient by a factor of at least five, compared to a corresponding formulation without the bioavailability promoting agent.
摘要翻译： 本发明涉及包含核心的药物或营养制剂，其包含活性药物或营养成分，渗透促进剂和生物利用度促进剂，以及用于胃肠靶向释放活性成分的聚合物涂层，其特征在于所述生物利用度促进 药剂是药学上可接受的蛋白水解酶抑制剂，与没有生物利用度促进剂的相应制剂相比，其将活性成分的口服生物利用度提高至少5倍。
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公开(公告)号：US20090041842A1
公开(公告)日：2009-02-12
申请号：US11815632
申请日：2005-12-15
CPC分类号： C08F220/18 , A61K9/2846 , A61K9/5026
摘要： The invention relates to a partly neutralised anionic (meth)acrylate copolymer consisting of radically polymerised units containing 25-95% by weight (meth)acrylic acid C1 to C4 alkylesters and 5-75% by weight (meth)acrylate monomer with an anionic group, wherein 0.1 to 25% contained anionic groups are neutralised by a base. Said invention is characterised in that said base is embodied in the form of an cationic organic base whose molecular weight is greater than 150. A medical form containing said partly neutralised anionic (meth)acrylate copolymer and the use of said partly neutralised anionic (meth)acrylate copolymer for producing a medical form rapidly releasing an active substance having a determined pH value are also disclosed.
摘要翻译： 本发明涉及部分中和的阴离子（甲基）丙烯酸酯共聚物，其由含有25-95重量％（甲基）丙烯酸C1至C4烷基酯和5-75重量％（甲基）丙烯酸酯单体的自由基聚合单元组成，具有阴离子基团 ，其中0.1〜25％的阴离子基团被碱中和。 所述发明的特征在于所述碱以分子量大于150的阳离子有机碱的形式实施。含有所述部分中和的阴离子（甲基）丙烯酸酯共聚物的医用形式以及所述部分中和的阴离子（甲基）丙烯酸酯共聚物的用途， 丙烯酸酯共聚物，用于制备快速释放具有确定的pH值的活性物质的医用形式。
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公开(公告)号：US08431157B2
公开(公告)日：2013-04-30
申请号：US11815632
申请日：2005-12-15
CPC分类号： C08F220/18 , A61K9/2846 , A61K9/5026
摘要： The invention relates to a partly neutralized anionic (meth)acrylate copolymer consisting of radically polymerized units containing 25-95% by weight (meth)acrylic acid C1 to C4 alkylesters and 5-75% by weight (meth)acrylate monomer with an anionic group, wherein 0.1 to 25% contained anionic groups are neutralized by a base. Said invention is characterized in that said base is embodied in the form of an cationic organic base whose molecular weight is greater than 150. A medical form containing said partly neutralized anionic (meth)acrylate copolymer and the use of said partly neutralized anionic (meth)acrylate copolymer for producing a medical form rapidly releasing an active substance having a determined pH value are also disclosed.
摘要翻译： 本发明涉及一种部分中和的阴离子（甲基）丙烯酸酯共聚物，它由含25-95％（重量）（甲基）丙烯酸C1至C4烷基酯和5-75％（重量）（甲基）丙烯酸阴离子基团单体的自由基聚合单元组成 ，其中0.1〜25％的阴离子基团被碱中和。 所述发明的特征在于所述碱以分子量大于150的阳离子有机碱的形式实施。含有所述部分中和的阴离子（甲基）丙烯酸酯共聚物的医用形式以及所述部分中和的阴离子（甲基）丙烯酸酯共聚物的用途， 丙烯酸酯共聚物，用于制备快速释放具有确定的pH值的活性物质的医用形式。
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5.发明申请公开(公告)号：US20070026082A1
公开(公告)日：2007-02-01
申请号：US10564096
申请日：2004-07-15
申请人： Rosario Lizio , Hans-Ulrich Petereit , Erna Roth , Ines Andres , Michael Damm
发明人： Rosario Lizio , Hans-Ulrich Petereit , Erna Roth , Ines Andres , Michael Damm
CPC分类号： A61K9/5026 , A61K9/1629 , A61K9/1652 , A61K9/1676 , A61K9/5078 , A61K38/00
摘要： The invention relates to an oral, multiparticle pharmaceutical dosage form containing pellets, the size of which ranges from 50 to 2500 μm and which essentially consist of: a) an inner matrix layer containing an active substance which is a peptide or a protein, including the derivatives or conjugates thereof, and which is embedded in a matrix consisting of a polymer with mucoadhesive effect, and b) an outer film coating essentially consisting of an anionic polymer or copolymer, which can be optionally formulated with pharmaceutically conventional adjuvants, more particularly softening agents.
摘要翻译： 本发明涉及含有丸粒的口服多颗粒药物剂型，其粒径范围为50-2500μm，其基本上由以下组成：a）包含肽或蛋白质的活性物质的内基质层，包括 衍生物或共轭物，并且其嵌入由具有粘膜粘附作用的聚合物组成的基质中，以及b）基本上由阴离子聚合物或共聚物组成的外膜包衣，其可以任选地与药学上常规的佐剂配制，更特别的是软化剂 。
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公开(公告)号：US10113050B2
公开(公告)日：2018-10-30
申请号：US13322159
申请日：2009-07-30
摘要： A powdery or granulated composition, containing: (a) a copolymer containing, in polymerized form, a C1- to C4-alkyl ester of acrylic or methacrylic acid and an alkyl(meth)acrylate monomer containing a tertiary amino group in an alkyl radical; (b) 0.5 to 10% by weight based on (a) of a dicarboxylic acid having 3 to 10 carbon atoms; and (c) 5 to 20% by weight based on (a) of a fatty monocarboxylic acid having 8 to 18 carbon atoms, where the composition contains at least by 30% by weight of (a), (b), and (c).
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7.发明授权Process for converting a solid (meth)acrylate copolymer into a dispersed form by means of a dispersing agent 有权通过分散剂将固体（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
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
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8.发明申请COMPOSITION COMPRISING AN ANIONIC POLYMERIC MATERIAL AND THE SALT OF A SATURATED MONOCARBOXYLIC ACID HAVING 6 TO 22 CARBON ATOMS 审中-公开包含阴离子聚合材料的组合物和具有6至22个碳原子的饱和单羧酸的盐公开(公告)号：US20120093904A1
公开(公告)日：2012-04-19
申请号：US13378112
申请日：2009-07-30
CPC分类号： A61K9/2846 , A61K9/282 , A61K9/5015 , A61K9/5026 , C08J3/205 , C08J2333/02 , C08J2333/06
摘要： The invention relates to a coating composition for the coating or binding of pharmaceutically, nutraceutically or cosmetically active ingredients, comprising (a) an anionic polymeric material, and (b) one or more salts of saturated monocarboxylic acids having 6 to 22 carbon atoms, characterized in that the amount of the salts of the monocarboxylic acids in the composition corresponds to 3 to 50 mol percent of the amount of anionic groups in the polymeric material. The invention also relates to a process for preparing a dispersion out of the composition, as well as the use of said composition in enteric-coated solid dosage forms.
摘要翻译： 本发明涉及用于涂覆或结合药学，营养或美容活性成分的涂料组合物，其包含（a）阴离子聚合物材料和（b）一种或多种具有6至22个碳原子的饱和一元羧酸盐，其特征在于 因为组合物中单羧酸的盐的量相当于聚合物材料中阴离子基团量的3至50mol％。 本发明还涉及制备组合物中的分散体的方法，以及所述组合物在肠溶包衣固体剂型中的用途。
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9.发明申请POWDERY OR GRANULATED COMPOSITION COMPRISING A COPOLYMER, A SALT OF A FATTY MONOCARBOXYLIC ACID AND A FATTY MONOCARBOXYLIC ACID AND/OR A FATTY ALCOHOL 审中-公开包含共聚物，脂肪酸单羧酸盐和脂肪单羧酸和/或脂肪醇的粉末或成粒组合物公开(公告)号：US20120093903A1
公开(公告)日：2012-04-19
申请号：US13376529
申请日：2010-03-17
CPC分类号： A61K9/2846 , C08J3/12 , C08J3/126 , C08J2333/14 , C08K5/05 , C08K5/09 , C08K5/098 , C08L33/14
摘要： The invention relates to a powdery or granulated composition comprising at least by 30% by weight of a mixture of (a) a copolymer composed of polymerized units of C1- to C4-alkyl esters of acrylic or methacrylic acid and of alkyl(meth)acrylate monomers with a tertiary amino group in the alkyl radical and (b) 5 to 28% by weight based on (a) of a salt of a fatty monocarboxylic acid having 10 to 18 carbon atoms, and (c) 10 to 30% by weight based on (a) of fatty monocarboxylic acid having 8 to 18 carbon atoms and/or a fatty alcohol having 8 to 18 carbon atoms.
摘要翻译： 本发明涉及粉末或颗粒状组合物，其包含至少30重量％的（a）由丙烯酸或甲基丙烯酸的C 1 -C 4烷基酯的聚合单元和（甲基）丙烯酸烷基酯 在烷基中具有叔氨基的单体和（b）基于（a）具有10至18个碳原子的脂肪一元羧酸盐的5-28重量％，和（c）10-30重量％ 基于（a）具有8至18个碳原子的脂肪族单羧酸和/或具有8至18个碳原子的脂肪醇。
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10.发明申请PROCESS FOR CONVERTING A SOLID (METH)ACRYLATE COPOLYMER INTO A DISPERSED FORM BY MEANS OF A DISPERSING AGENT 有权通过分散剂将固体（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
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
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