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41.发明申请Multiparticle Pharmaceutical Dosage Form for a Low-Soluble Active Substances and Method for Producing Said Pharmaceutical Dosage Form 有权用于制备低剂量活性物质的多药物药物剂型及生产所述药物剂型的方法公开(公告)号：US20080166416A1
公开(公告)日：2008-07-10
申请号：US11572720
申请日：2005-07-08
IPC分类号： A61K9/14 , A61K31/513 , A61K31/4439 , A61K31/55
CPC分类号： A61K31/506 , A61K9/1617 , A61K9/1652 , A61K9/5026 , A61K9/5078 , A61K31/427 , A61K31/55
摘要： The invention relates to an oral multiparticle pharmaceutical dosage form in the form of a receptacle reducing the pH values of stomach, containing a plurality of pellets, particles, granules or agglomerates whose mean diameter ranges from 50 to 2500 μn substentially consisting of a) an internal matrix layer containing an active agent which is neither peptide or protein, nor the derivatives or conjugates thereof, a lipophilic matrix whose melting point is greater than 37° C. and a polymer with mucoadhesive effect, b) an external film coating substentially consisting of a polymer or an anionic copolymer which is optionally formulated with conventional pharmaceutical additives, wherein the active agent has a water solubility according to DAB 10, of at least 30 volume parts of water for one part by weight of the active agent and is coated with the lipophilic matrix and said active agent-containing lipophilic matrix is coated with a matrix made of a polymer with mucoadhesive effect. A method for producing the inventive multiparticle pharmaceutical dosage is also disclosed.
摘要翻译： 本发明涉及呈容器形式的口服多颗粒药物剂型，其减少胃的pH值，其含有多个颗粒，颗粒，颗粒或附聚物，其平均直径范围为50至2500个，其特征在于a）内部 含有不是肽或蛋白质的活性剂的基质层，也不是其衍生物或共轭物，其熔点大于37℃的亲脂基质和具有粘膜粘附作用的聚合物，b）由 聚合物或阴离子共聚物，其任选地与常规药物添加剂配制，其中活性剂具有根据DAB 10的水溶性，至少30体积份的水用于1重量份的活性剂，并且用亲脂性 基质和所述含活性剂的亲脂基质涂覆有由具有粘膜粘附作用的聚合物制成的基质。 还公开了用于生产本发明的多颗粒药物剂量的方法。
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公开(公告)号：US07264943B2
公开(公告)日：2007-09-04
申请号：US10501140
申请日：2003-10-16
IPC分类号： C07D501/22 , C12P35/04
CPC分类号： C12P35/04
摘要： The invention relates to a process for the preparation of cephalexin with the aid of a penicillin amidase immobilized on a crosslinked hydrophilic copolymer which has binding activity for ligands having nucleophilic groups and is in bead form.
摘要翻译： 本发明涉及一种借助于固定在交联的亲水共聚物上的青霉素酰胺酶来制备头孢氨苄的方法，所述交联的亲水共聚物对具有亲核基团的配体具有结合活性且呈珠粒形式。
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公开(公告)号：US20050079216A1
公开(公告)日：2005-04-14
申请号：US10502648
申请日：2003-01-30
申请人： Hans-Ulrich Petereit , Thomas Suefke , Christian Meier , Michael Schnabel , Ingrid Blesing , Stefan Grimm
发明人： Hans-Ulrich Petereit , Thomas Suefke , Christian Meier , Michael Schnabel , Ingrid Blesing , Stefan Grimm
IPC分类号： A61J3/06 , A61K9/02 , A61K9/08 , A61K9/20 , A61K9/28 , A61K9/32 , A61K9/48 , A61K9/50 , A61K9/52 , A61K31/49 , A61K47/20 , A61K47/32 , A61P9/06 , A61K9/14
CPC分类号： A61K9/5026 , A61K9/2846 , Y02A50/473
摘要： The invention relates to a method for producing a pharmaceutical dosage form as tablets, pellets and/or in the form of an active ingredient-containing matrix, whereby the tablets, pellets and/or active ingredient-containing matrix contain a pharmaceutical active ingredient and a copolymer serving as a coating agent and/or binding agent, and optionally contain a core and pharmaceutically common additives. According to the invention, the copolymer, the pharmaceutical active ingredient, the optionally present core and/or the pharmaceutically common additives are processed using known techniques by melting, injection molding, extrusion, wet granulation, casting, dipping, spreading out, spraying on, or pressing to form tablets, pellets and/or an active ingredient-containing matrix. The inventive method is characterized in that a copolymer is used that consists of 20 to 34 wt. % methacrylic acid, 20 to 69 wt. % methylacrylate and 0 to 40 wt. % ethylacrylate and, optionally, of 0 to 10 wt. % of additional vinylically copolymerizable monomers with the provision that the glass transition temperature of the copolymer is no higher than 60° C. according to ISO 11357-2, Item 3.3.3. The invention also relates to the pharmaceutical dosage form produced according to this method, said copolymer and the use thereof.
摘要翻译： 本发明涉及用于制备药物剂型作为片剂，丸粒和/或含有活性成分的基质形式的方法，由此所述片剂，丸剂和/或含活性成分的基质含有药物活性成分和 共聚物作为包衣剂和/或粘合剂，并且任选地含有核心和药学上常用的添加剂。 根据本发明，共聚物，药物活性成分，任选存在的核心和/或药学上常用的添加剂使用已知技术通过熔融，注射成型，挤出，湿法制粒，浇铸，浸渍，扩散，喷涂， 或压制以形成片剂，丸剂和/或含活性成分的基质。 本发明的方法的特征在于使用由20〜34重量％ ％甲基丙烯酸，20〜69重量％ ％甲基丙烯酸酯和0至40wt。 ％丙烯酸乙酯和任选地0至10wt。 ％的额外的乙烯基共聚单体，其规定，根据ISO 11357-2，项目3.3.3，共聚物的玻璃化转变温度不高于60℃。 本发明还涉及根据该方法生产的药物剂型，所述共聚物及其用途。
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公开(公告)号：US20050065224A1
公开(公告)日：2005-03-24
申请号：US10498971
申请日：2003-08-25
申请人： Stefan Menzler , Hans-Ulrich Petereit , Christian Meier , Thomas Boller , Thomas Suefke , Klaus Schultes , Roger Recktenwald
发明人： Stefan Menzler , Hans-Ulrich Petereit , Christian Meier , Thomas Boller , Thomas Suefke , Klaus Schultes , Roger Recktenwald
IPC分类号： C08F220/28 , C08F246/00 , C08J9/00 , C08F118/02
CPC分类号： C08F220/28 , C08F246/00 , Y10S530/815
摘要： The invention relates to a macroporous plastics bead material with an average particle diameter from 10 to 1000 μm, containing a copolymer of a) 5-60 wt. % vinylically polymerizable monomers with a water solubility of at least 1% at 20° C., b) 1-40 wt. % vinylically polymerizable monomers with an additional functional group, which can enter into covalent bonds with the nucleophilic groups of the ligands in a polymer-like reaction, c) 10-40 wt. % hydrophilic, crosslinking radical-polymerizable monomers with two or more ethylenically unsaturated polymerizable groups and d) 10-60 wt. % vinylically polymerizable monomers with a water solubility of at most 1% at 20° C. are contained, as a rule with the monomers a) to d) adding up to 100%.
摘要翻译： 本发明涉及平均粒径为10-1000μm的大孔塑料珠粒材料，其含有a）5-60wt。 ％乙烯基聚合性单体，水溶性在20℃下至少为1％，b）1-40wt。 具有另外的官能团的具有可与聚合物样反应中的配体的亲核基团共价键的乙烯基聚合性单体的％，c）10-40wt。 具有两个或更多个烯属不饱和可聚合基团的亲水性交联自由基聚合单体，和d）10-60wt。 在20℃下水溶解度最多为1％的％乙烯基聚合性单体的含量通常与单体a）至d）相加至100％。
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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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公开(公告)号：US09700520B2
公开(公告)日：2017-07-11
申请号：US12678406
申请日：2007-09-25
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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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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48.发明授权PH-dependent controlled release pharmaceutical composition for non-opioids with resistance against the influence of ethanol 有权对依赖乙醇影响的非阿片样物质的PH依赖性控释药物组合物公开(公告)号：US09555006B2
公开(公告)日：2017-01-31
申请号：US12678429
申请日：2007-09-25
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 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。
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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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50.发明申请PHARMACEUTICAL DOSAGE FORM COMPRISING ONE OR MORE ANTIRETROVIRAL ACTIVE INGREDIENTS 审中-公开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。
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