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公开(公告)号：US6063399A
公开(公告)日：2000-05-16
申请号：US995986
申请日：1997-12-22
IPC分类号： A61K9/70 , C09J133/14 , A61F13/02
CPC分类号： A61K9/7061 , C09J133/14
摘要： An adhesive binder for dermal or transdermal therapy systems consists of the following components:(a1) 55-99.9 wt. % of a (meth)acrylate copolymer of a structural (meth)acrylate or a functional (meth)acrylate monomer, wherein the functional monomer has a tertiary or quaternary amino group,(a2) 0.1-45 wt. % of an acid group-containing acrylate or (meth)acrylate polymer or copolymer, and(b) 25-80 wt. % of a plasticizer, based on the sum of (a1) and (a2).
摘要翻译： 用于皮肤或透皮治疗系统的粘合剂粘合剂由以下组分组成：（a1）55-99.9wt。 ％的结构（甲基）丙烯酸酯或官能（甲基）丙烯酸酯单体的（甲基）丙烯酸酯共聚物，其中官能单体具有叔或季氨基，（a2）0.1-45重量％ ％的含酸基的丙烯酸酯或（甲基）丙烯酸酯聚合物或共聚物，和（b）25-80重量％ 基于（a1）和（a2）的总和的增塑剂的％。
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公开(公告)号：US09107451B2
公开(公告)日：2015-08-18
申请号：US12845994
申请日：2010-07-29
CPC分类号： A23P1/04 , A23P10/30 , A61K9/4891 , A61K47/32
摘要： A coating composition for the enteric coating of capsule halves made of water-soluble or water-swellable polymer material in a dipping process is provided. The composition is an aqueous dispersion or solution, containing a polymer mixture of at least one first (meth)acrylate copolymer, which is enteric, and at least one further (meth)acrylate copolymer, which is enteric or water-insoluble, and also auxiliaries which influence the viscosity of the dispersion and the elasticity of the dried polymer film. The solids content of the dispersion or solution is more than 25% by weight and the viscosity is 150 to 1500 mPa·s and a dried film produced from the dispersion or solution has an elongation at break of at least 200%. Also provided is a capsule composed of two capsule halves coated with the dispersion or solution in a dipping process does. The enteric capsule does not dissolve in 0.1 N HCl at pH 1.2 after two hours, but completely dissolves in buffer at pH 6.8 in less than 30 minutes. A method to prepare enteric coated capsule halves is also provided.
摘要翻译： 提供了一种用于在浸渍过程中由水溶性或水溶胀性聚合物材料制成的胶囊半部的肠溶衣涂料组合物。 该组合物是含有至少一种肠溶性的至少一种第一（甲基）丙烯酸酯共聚物和至少一种其它（甲基）丙烯酸酯共聚物的聚合物混合物的水性分散体或溶液，其为肠溶或水不溶性的，以及辅助剂 这影响了分散体的粘度和干燥的聚合物膜的弹性。 分散体或溶液的固体成分大于25重量％，粘度为150〜1500mPa·s，由分散液或溶液产生的干燥膜的断裂伸长率为200％以上。 还提供了由在浸渍过程中涂覆有分散体或溶液的两个胶囊半部组成的胶囊。 肠溶胶囊在pH2.2后2小时内不溶于0.1N HCl，但在不到30分钟内完全溶于pH 6.8的缓冲液中。 还提供了制备肠溶衣胶囊半部的方法。
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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：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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15.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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16.发明申请POWDERY OR GRANULATED COMPOSITION COMPRISING A COPOLYMER, A DICARBOXYLIC ACID AND A FATTY MONOCARBOXYLIC ACID 审中-公开包含共聚物，二羧酸和脂肪单羧酸的粉末或成粒组合物公开(公告)号：US20120071565A1
公开(公告)日：2012-03-22
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).
摘要翻译： 一种粉状或粒状组合物，其含有：（a）以聚合形式含有丙烯酸或甲基丙烯酸的C 1至C 4烷基酯和在烷基中含有叔氨基的（甲基）丙烯酸烷基酯单体的共聚物; （b）相对于（a）碳原子数为3〜10的二羧酸为0.5〜10重量％ 和（c）基于（a）具有8至18个碳原子的脂肪一元羧酸的5至20重量％，其中所述组合物含有至少30重量％的（a），（b）和（c ）。
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公开(公告)号：US07879966B2
公开(公告)日：2011-02-01
申请号：US11476182
申请日：2006-06-28
申请人： Hans-Ulrich Petereit , Christian Meier , Klaus Schultes , Marie-Andree Yessine , Jean-Christophe Leroux
发明人： Hans-Ulrich Petereit , Christian Meier , Klaus Schultes , Marie-Andree Yessine , Jean-Christophe Leroux
IPC分类号： C08F20/06
CPC分类号： A61K9/0019 , A61K9/0014 , A61K47/32
摘要： A pH-sensitive polymer which has cytotoxic or membranolytic properties at pH values below pH 6.5. Carriers for natural or synthetic biomolecules or active pharmaceutical ingredients using such a pH-sensitive polymer.
摘要翻译： pH值敏感的聚合物，其pH值低于pH 6.5时具有细胞毒性或膜分解性能。 使用这种pH敏感聚合物的天然或合成生物分子或活性药物成分的载体。
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18.发明申请公开(公告)号：US20090280183A1
公开(公告)日：2009-11-12
申请号：US11721399
申请日：2005-11-05
IPC分类号： A61K9/10 , A61K31/7088 , A61P1/00 , A61K39/395
CPC分类号： A61K9/5138 , A61K9/1652 , A61K9/1676 , A61K9/1694 , A61K9/5192 , A61K31/7088
摘要： The invention relates to an oral, multiparticulate form of administration, comprising pellets in the size ranging from 50 to 2500 $g(m)m which are substantially constituted of a) an inner matrix layer containing nanoparticles that contain a nucleic acid active ingredient and being embedded in a matrix of a polymer having a mucoadhesive effect, and b) an outer film coating, substantially consisting of an anionic polymer or copolymer that is optionally formulated with pharmaceutically conventional adjuvants, especially emollients.
摘要翻译： 本发明涉及口服，多颗粒形式的施用，其包含尺寸范围为50至2500g（m）m的颗粒，其基本上由以下组成：a）含有含有核酸活性成分的纳米颗粒的内基质层， 嵌入在具有粘膜粘附作用的聚合物的基质中，以及b）外膜包衣，其基本上由阴离子聚合物或共聚物组成，其任选地与药学上常规的佐剂特别是润肤剂配制。
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公开(公告)号：US07553918B2
公开(公告)日：2009-06-30
申请号：US10510371
申请日：2002-10-22
申请人： Hans-Ulrich Petereit , Christian Meier , Klaus Schultes , Marie-Andree Yessine , Jean-Christophe Leroux
发明人： Hans-Ulrich Petereit , Christian Meier , Klaus Schultes , Marie-Andree Yessine , Jean-Christophe Leroux
IPC分类号： C08F20/06
CPC分类号： A61K9/0019 , A61K9/0014 , A61K47/32
摘要： The invention relates to a pH-sensitive polymer which is a (meth)acrylate copolymer composed of 20 to 65% by weight acrylic and/or methacrylic acid units and 80 to 35% by weight units of C1- to C18-alkyl esters of (meth)acrylic acid, characterized in that it has a molecular weight in the range from 1 000 to 50 000 g/mol, and brings about at least 60% haemolysis at pH 5.5, and less than 5% haemolysis at pH 7.4, in a concentration of 150 μg/ml in a cytotoxicity test with human red blood cells. The invention further relates to the use of the pH-sensitive polymer as carrier for pharmaceutically effective biomolecules or active pharmaceutical ingredients and as ingredient of corresponding dosage forms.
摘要翻译： 本发明涉及一种pH敏感性聚合物，它是由20-65％（重量）丙烯酸和/或甲基丙烯酸单元组成的（甲基）丙烯酸酯共聚物和80-35％（重量）单元的C 1 -C 18烷基酯（ 甲基）丙烯酸，其特征在于其分子量在1000至500000克/摩尔的范围内，并且在pH7.5下产生至少60％的溶血，并且在pH7.4时溶血小于5％，在 在人红细胞的细胞毒性试验中浓度为150ug / ml。 本发明还涉及pH敏感性聚合物作为药学上有效的生物分子或活性药物成分的载体和作为相应剂型的成分的用途。
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20.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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