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1.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：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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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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4.发明授权Aqueous carbonated medium containing an amino(meth)acrylate polymer or copolymer 有权包含氨基（甲基）丙烯酸酯聚合物或共聚物的含水碳酸酯介质公开(公告)号：US08951558B2
公开(公告)日：2015-02-10
申请号：US13322530
申请日：2009-07-30
IPC分类号： A61K9/48 , A61K9/32 , A61K9/16 , A61K9/50 , A23G3/02 , A23L1/30 , A23L3/015 , A23P1/00 , B29D22/00 , B29D23/00 , B32B1/08 , B32B27/08 , A61K47/32 , C08F8/30 , C08L39/00 , A61K47/08
CPC分类号： A61K47/08 , Y10T428/13 , Y10T428/1352
摘要： The invention relates to an aqueous medium containing an amino(meth)acrylate polymer or copolymer which is not soluble in dematerialised water, characterized in that the medium has a content of an aqueous phase of at least 60% by weight and a content of up to 40% by weight of solids comprising the amino(meth)acrylate polymer or copolymer, whereby the aqueous phase is charged by a sufficient amount of carbon dioxide that effects the amino(meth)acrylate polymer or copolymer to be present in solute form in the medium. The aqueous medium may be used beneficially as a coating or binding solution for the spray coating or binding of pharmaceutical compositions or nutraceutical compositions or cosmetical compositions.
摘要翻译： 本发明涉及含有不溶于非物质化水的氨基（甲基）丙烯酸酯聚合物或共聚物的水性介质，其特征在于该介质的含水量至少为60重量％，含量至多 40重量％的包含氨基（甲基）丙烯酸酯聚合物或共聚物的固体，由此通过足够量的二氧化碳装入水相，使得氨基（甲基）丙烯酸酯聚合物或共聚物以溶质形式存在于介质中 。 有利地，水性介质可用作药物组合物或营养组合物或美容组合物的喷涂或结合的包衣或结合溶液。
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公开(公告)号：US09597293B2
公开(公告)日：2017-03-21
申请号：US12598138
申请日：2007-05-07
申请人： Fang Liu , Abdul W. Basit , Rosario Lizio , Hans-Ulrich Petereit , Christian Meier , Michael Damm
发明人： Fang Liu , Abdul W. Basit , Rosario Lizio , Hans-Ulrich Petereit , Christian Meier , Michael Damm
CPC分类号： A61K9/5073 , A61K9/5026
摘要： The present invention provides a solid dosage form including an inner coating located between a core containing a pharmaceutically active ingredient and an outer enteric coating; wherein the inner coating includes a partially neutralized anionic polymeric material, and at least a carboxylic acid having 2 to 16 carbon atoms the salts thereof or mixtures of the acid and its salt; wherein the outer coating includes an anionic polymeric material which is less or not at all neutralized than the material of the inner coating.
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公开(公告)号：US10537530B2
公开(公告)日：2020-01-21
申请号：US13603984
申请日：2012-09-05
申请人： Fang Liu , Abdul W. Basit , Rosario Lizio , Hans-Ulrich Petereit , Christian Meier , Michael Damm
发明人： Fang Liu , Abdul W. Basit , Rosario Lizio , Hans-Ulrich Petereit , Christian Meier , Michael Damm
IPC分类号： A61K9/50
摘要： The invention provides a gastric resistant, enteric-coated solid dosage form including a core containing a pharmaceutically active ingredient, an inner coating for the core, and an outer enteric coating. The inner coating comprises an anionic polymeric material or a water-soluble neutral polymeric material, and further comprises a water soluble inorganic salt which is not a carbonate or bicarbonates. The outer enteric coating comprises an anionic polymeric material which is less neutralized than the polymeric material comprising the inner coating and disintegrates rapidly at a pH of 5.5 to 7.0 upon entering the small intestine.
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7.发明申请SOLID DOSAGE FORMS COMPRISING AN ENTERIC COATING WITH ACCELERATED DRUG RELEASE 审中-公开固体药剂包含加速药物释放的肠衣公开(公告)号：US20130058986A1
公开(公告)日：2013-03-07
申请号：US13603984
申请日：2012-09-05
申请人： Fang LIU , Abdul W. Basit , Rosario Lizio , Hans-Ulrich Petereit , Christian Meier , Michael Damm
发明人： Fang LIU , Abdul W. Basit , Rosario Lizio , Hans-Ulrich Petereit , Christian Meier , Michael Damm
IPC分类号： A61K9/00
摘要： The present invention provides a solid dosage form including an inner coating located between a core containing a pharmaceutically active ingredient and an outer enteric coating; wherein the inner coating includes a partially neutralized anionic polymeric material and at least a carboxylic acid having 2 to 16 carbon atoms, the salts thereof, or mixtures of the acid and its salt; wherein the outer coating includes an anionic polymeric material which is less neutralized than the material of the inner coating or not at all neutralized.
摘要翻译： 本发明提供了一种固体剂型，其包括位于含有药物活性成分的核心和外部肠溶衣之间的内部涂层; 其中所述内涂层包括部分中和的阴离子聚合物材料和至少一种具有2至16个碳原子的羧酸，其盐，或其酸及其盐的混合物; 其中所述外涂层包括阴离子聚合物材料，所述阴离子聚合物材料比所述内涂层的材料中和程度低，或者完全不被中和。
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8.发明申请AQUEOUS CARBONATED MEDIUM CONTAINING AN AMINO(METH)ACRYLATE POLYMER OR COPOLYMER 有权含氨基（甲基）丙烯酸酯聚合物或共聚物的水性中和体公开(公告)号：US20120087977A1
公开(公告)日：2012-04-12
申请号：US13322530
申请日：2009-07-30
IPC分类号： A61K47/32 , C08J3/205 , A61K9/14 , B32B1/08 , A61K9/48 , A23L1/30 , A23P1/08 , A23P1/02 , C08L33/14 , A61K9/32
CPC分类号： A61K47/08 , Y10T428/13 , Y10T428/1352
摘要： The invention relates to an aqueous medium containing an amino(meth)acrylate polymer or copolymer which is not soluble in demineralised water, characterized in that the medium has a content of an aqueous phase of at least 60% by weight and a content of up to 40% by weight of solids comprising the amino(meth)acrylate polymer or copolymer, whereby the aqueous phase is charged by a sufficient amount of carbon dioxide that effects the amino(meth)acrylate polymer or copolymer to be present in solute form in the medium. The aqueous medium may be used beneficially as a coating or binding solution for the spray coating or binding of pharmaceutical compositions or nutraceutical compositions or cosmetical compositions.
摘要翻译： 本发明涉及含有不溶于去离子水的氨基（甲基）丙烯酸酯聚合物或共聚物的水性介质，其特征在于所述介质的含水量至少为60重量％，含量至多 40重量％的包含氨基（甲基）丙烯酸酯聚合物或共聚物的固体，由此通过足够量的二氧化碳装入水相，使得氨基（甲基）丙烯酸酯聚合物或共聚物以溶质形式存在于介质中 。 有利地，水性介质可用作药物组合物或营养组合物或美容组合物的喷涂或结合的包衣或结合溶液。
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9.发明申请公开(公告)号：US20100129446A1
公开(公告)日：2010-05-27
申请号：US12598138
申请日：2007-05-07
申请人： Fang Liu , Abdul W. Basit , Rosario Lizio , Hans-Ulrich Petereit , Christian Meier , Michael Damm
发明人： Fang Liu , Abdul W. Basit , Rosario Lizio , Hans-Ulrich Petereit , Christian Meier , Michael Damm
IPC分类号： A61K9/32 , B05D3/00 , A61K31/57 , A61K31/522
CPC分类号： A61K9/5073 , A61K9/5026
摘要： The present invention refers to a solid dosage form comprising an inner coating located between a core containing a pharmaceutically active ingredient and an outer enteric coating; wherein said inner coating comprises a partially neutralized anionic polymeric material, and at least a carboxylic acid having 2 to 16 carbon atoms the salts thereof or mixtures of said acid and its salt; wherein said outer coating comprises an anionic polymeric material which is less or not at all neutralized than the material of the inner coating.
摘要翻译： 本发明涉及一种固体剂型，其包含位于包含药物活性成分的核心和外部肠溶衣之间的内部涂层; 其中所述内涂层包含部分中和的阴离子聚合物材料，和至少一种具有2至16个碳原子的羧酸盐或其所述酸及其盐的混合物; 其中所述外涂层包含阴离子聚合物材料，其比内涂层的材料更少或不完全中和。
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10.发明授权公开(公告)号：US08734849B2
公开(公告)日：2014-05-27
申请号：US10564096
申请日：2004-07-15
申请人： Rosario Lízio , Hans-Ulrich Petereit , Erna Roth , Inès Andres , Michael Damm
发明人： Rosario Lízio , Hans-Ulrich Petereit , Erna Roth , Inès Andres , Michael Damm
IPC分类号： A61K9/14
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，其尺寸范围为50-2500μm，其基本上由以下组成：a）含有作为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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