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1.发明申请Pharmaceutical Compositions Containing Mixtures of Polymers and Active Agents Poorly Soluble in Water 审中-公开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
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。
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2.发明申请PELLETS HAVING AN ACTIVE COMPOUND MATRIX AND A POLYMER COATING, AND A PROCESS FOR THE PRODUCTION OF THE PELLETS 审中-公开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
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。
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3.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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4.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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公开(公告)号：US08343542B2
公开(公告)日：2013-01-01
申请号：US10542283
申请日：2003-11-21
CPC分类号： A61J3/10 , A61K9/0056 , A61K9/146 , A61K9/1647 , A61K9/2054 , A61K31/192
摘要： The invention relates to a method for producing an oral form of administration which decomposes immediately and releases active ingredients in the mouth. According to said method, (a) an anionic pharmaceutical active ingredient is intensively mixed with (b) a copolymer consisting of radically polymerized C1-C4 esters of the acrylic acid or methacrylic acid and other (meth)acrylate monomers containing functional tertiary amino groups, and (c) between 5 and 50 wt. %, in relation to (b), of a C12-C22 carboxylic acid in the melted mass; the mixture is solidified and ground to form a powder containing active ingredients having an average particle size of 200 μm or less; and the powder is encapsulated in a water-soluble matrix consisting of pharmaceutically standard adjuvants, on the condition that no more than 3 wt. %, in relation to the copolymer, of emulsifiers with an HLB value of at least 14 must be contained therein. The invention also relates to the powder containing active ingredients and the uses of the same.
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6.发明授权公开(公告)号：US07175857B2
公开(公告)日：2007-02-13
申请号：US10489856
申请日：2003-07-08
CPC分类号： A61K9/1694 , A61K9/1635 , A61K9/1682 , A61K9/2846 , A61K9/5026
摘要： The invention relates to a process for the production of granules or powders, suitable as coating agents and binders for oral or dermal pharmaceutical forms, for cosmetics or food supplements, consisting essentially of (a) a copolymer, consisting of free radical-polymerized C1- to C4-esters of acrylic or methacrylic acid and further (meth)acrylate monomers which contain functional tertiary amino groups, (b) 3 to 25% by weight, based on (a), of an emulsifier having an HLB of at least 14, (c) 5 to 50% by weight, based on (a), of a C12- to C18-monocarboxylic acid or of a C12- to C18-hydroxyl compound, where the components (a), (b) and (c) are simultaneously or successively blended or mixed with one another, optionally with addition of a pharmaceutical active compound and/or further customary additives, fused in a heatable mixer, mixed, the melt is cooled and comminuted to give granules or powders.
摘要翻译： 本发明涉及一种用于生产用于化妆品或食品补充剂的适合作为口服或皮肤药物形式的包衣剂和粘合剂的颗粒或粉末的方法，其基本上由（a）共聚物组成，所述共聚物由游离基聚合的C1- 丙烯酸或甲基丙烯酸的C 4 - 酯和另外（甲基）丙烯酸酯单体，其中含有官能叔氨基，（b）3-25重量％，基于（a）的HLB为至少14的乳化剂， （c）5至50重量％，基于（a），C 12 - 12 - C 18 - 单羧酸或C 12 - 其中组分（a），（b）和（c）同时或相继地彼此混合或混合，任选地加入药物活性物质 化合物和/或其它常规添加剂，在可加热混合器中熔融混合，将熔体冷却并粉碎以产生颗粒或粉末。
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7.发明申请公开(公告)号：US20050197434A9
公开(公告)日：2005-09-08
申请号：US10489856
申请日：2003-07-08
IPC分类号： A61K9/16 , A61K9/28 , A61K9/50 , A61K47/10 , A61K47/12 , A61K47/32 , B29C39/14 , C08J3/00 , C08J5/00 , C08K5/04
CPC分类号： A61K9/1694 , A61K9/1635 , A61K9/1682 , A61K9/2846 , A61K9/5026
摘要： The invention relates to a process for the production of granules or powders, suitable as coating agents and binders for oral or dermal pharmaceutical forms, for cosmetics or food supplements, consisting essentially of (a) a copolymer, consisting of free radical- polymerized C1- to C4-esters of acrylic or methacrylic acid and further (meth)acrylate monomers which contain functional tertiary amino groups, (b) 3 to 25% by weight, based on (a), of an emulsifier having an HLB of at least 14, (c) 5 to 50% by weight, based on (a), of a C12- to C18-monocarboxylic acid or of a C12- to C18- hydroxyl compound, where the components (a), (b) and (c) are simultaneously or successively blended or mixed with one another, optionally with addition of a pharmaceutical active compound and/or further customary additives, fused in a heatable mixer, mixed, the melt is cooled and comminuted to give granules or powders.
摘要翻译： 本发明涉及一种用于生产用于化妆品或食品补充剂的适合作为口服或皮肤药物形式的包衣剂和粘合剂的颗粒或粉末的方法，其基本上由（a）共聚物组成，所述共聚物由游离基聚合的C1- 丙烯酸或甲基丙烯酸的C 4 - 酯和另外（甲基）丙烯酸酯单体，其中含有官能叔氨基，（b）3-25重量％，基于（a）的HLB为至少14的乳化剂， （c）5至50重量％，基于（a），C 12 - 12 - C 18 - 单羧酸或C 12 - 其中组分（a），（b）和（c）同时或相继地彼此混合或混合，任选地加入药物活性物质 化合物和/或其它常规添加剂，在可加热混合器中熔融混合，将熔体冷却并粉碎以产生颗粒或粉末。
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公开(公告)号：US08642089B2
公开(公告)日：2014-02-04
申请号：US10498829
申请日：2003-01-30
CPC分类号： A61K9/2027 , A61K9/1694
摘要： The invention relates to a method for producing active ingredient-containing granules or powders involving the following steps: a) melting a mixture consisting of a pharmaceutical active ingredient and of a (meth)acrylate copolymer, which is comprised of 40 to 75 wt. % of radically polymerized C1 to C4 alkyl esters of acrylic acid or of methacrylic acid and can be comprised of 25 to 60 wt. % (meth)acrylate monomers having an anionic group in the alkyl radial; b) extruding the mixture, and; c) comminuting the extrudate to form a granule or powder. The inventive method is characterized in that the active ingredient is the salt of an alkaline substance, and in that the pH value, which can be measured on the obtained powder or granule, is equal to or less than pH 7.0. The invention also relates to pharmaceutical dosage forms or precursors thereof, which can be produced using the inventive method.
摘要翻译： 本发明涉及生产含有活性成分的颗粒或粉末的方法，其包括以下步骤：a）熔化由药物活性成分和（甲基）丙烯酸酯共聚物组成的混合物，其由40至75重量％ ％的丙烯酸或甲基丙烯酸的自由基聚合的C1至C4烷基酯，并且可以包含25至60重量％ 具有阴离子基团的（甲基）丙烯酸酯单体在烷基的径向上; b）挤出混合物， c）粉碎挤出物以形成颗粒或粉末。 本发明的方法的特征在于活性成分是碱性物质的盐，并且可以在所得粉末或颗粒上测量的pH值等于或小于pH7.0。 本发明还涉及可以使用本发明方法制备的药物剂型或其前体。
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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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10.发明授权Coating and binding agent for pharmaceutical formulations with improved storage stability 有权具有改善储存稳定性的药物制剂的涂层和粘合剂公开(公告)号：US07160558B2
公开(公告)日：2007-01-09
申请号：US10239634
申请日：2001-02-27
申请人： Hans-Ulrich Petereit , Christian Meier , Erna Roth
发明人： Hans-Ulrich Petereit , Christian Meier , Erna Roth
摘要： The invention relates to a process for the preparation of a coating and binding agent for oral or dermal pharmaceutical forms, essentially consisting of (a) a copolymer consisting of free-radical-polymerized C1 to C4 esters of acrylic or methacrylic acid and further (meth)acrylate monomers which contain functional tertiary ammonium groups, the coplymer being present in powdered form having an average particle size of 1–40 μm, (b) 3 to 15% by weight, based on (a), of an emulsifier having an HLB of at least 14 and (c) 5 to 50% by weight, based on (a), of a C12—to C18-monocarboxylic acid or a C12—to C18-hydroxyl compound, the components (a), (b) and (c) being blended or mixed with one another with or without addition of water and if appropriate with addition of a pharmaceutical active compound and further customary additives and the coating and binding agent being produced from the mixture by melting, casting, spreading or spraying. The invention further relates to the coating and binding agent itself.
摘要翻译： 本发明涉及一种制备用于口服或皮肤药物形式的包衣和粘合剂的方法，其基本上由（a）由丙烯酸或甲基丙烯酸的自由基聚合的C1至C4酯和（甲基）丙烯酸酯组成的共聚物 ）丙烯酸酯单体，所述共聚物以平均粒径为1-40μm的粉末形式存在，（b）基于（a）的3至15重量％的具有HLB的乳化剂 至少14和（c）5至50重量％，基于（a）的C 12 - C 18 C 18 - 单羧酸或C < 将组分（a），（b）和（c）在或不加入水中彼此混合或混合，如果 适当地添加药物活性化合物和进一步的常规添加剂，并且通过熔融，浇铸，铺展或喷涂由混合物制备涂层和粘合剂。 本发明还涉及涂层和粘合剂本身。
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