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91. 发明申请

US20060281887A1 PH-sensitive polymer 有权
标题翻译： PH敏感聚合物
公开(公告)号：US20060281887A1
公开(公告)日：2006-12-14
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。

92. 发明申请

US20060204576A1 Multilayer dosage forms, which contain active substances and which comprise a neutral core, and an inner and outer coating consisting of methacrylate copolymers and methacrylate monomers 审中-公开
标题翻译：包含活性物质并且包含中性核心的多层剂型，以及由甲基丙烯酸酯共聚物和甲基丙烯酸酯单体组成的内外涂层
公开(公告)号：US20060204576A1
公开(公告)日：2006-09-14
申请号：US10532831
申请日：2003-09-04
申请人： Hans-Ulrich Petereit , Markus Rudolph , Jennifer Dressman , Thomas Beckert
发明人： Hans-Ulrich Petereit , Markus Rudolph , Jennifer Dressman , Thomas Beckert
IPC分类号： A61K9/24
CPC分类号： A61K31/58 , A61K9/1635 , A61K9/209 , A61K9/2846 , A61K9/5026 , A61K9/5078
摘要： The invention relates to a multilayer dosage form comprised of: a) a neutral core; b) an inner coating consisting of a methacrylate copolymer; c) an outer coating consisting of a copolymer of which 40 to 95% by weight is composed of radically polymerized C1 to C4 alkyl esters of acrylic acid or of methacrylic acid and of which 5 to 60% by weight is composed of (meth)acrylate monomers having an anionic group in the alkyl radical. The invention is characterized in that the inner coating is essentially comprised of a methacrylate copolymer, of which at least up to 90% by weight consists of (meth)acrylate monomers with neutral radicals, which, in accordance with DIN 53 787, has a minimum film formation temperature of no higher than 30° C., and which contains the pharmaceutical active substance in bound form.
摘要翻译：本发明涉及一种多层剂型，其包括：a）中性核; b）由甲基丙烯酸酯共聚物组成的内涂层; c）由共聚物组成的外涂层，其中40至95重量％由丙烯酸或甲基丙烯酸的C 4-14烷基酯的自由基聚合的C 1〜并且其中5至60重量％由在烷基中具有阴离子基团的（甲基）丙烯酸酯单体组成。本发明的特征在于，内涂层基本上由甲基丙烯酸酯共聚物组成，其中至少高达90重量％由具有中性自由基的（甲基）丙烯酸酯单体组成，其根据DIN 53787具有最小值成膜温度不高于30℃，含有结合形式的药物活性物质。

93. 发明授权

US06998140B2 Dispersion comprising a non-ionic emulsifier 有权
标题翻译：包含非离子乳化剂的分散体
公开(公告)号：US06998140B2
公开(公告)日：2006-02-14
申请号：US09926484
申请日：2001-02-02
申请人： Christian Meier , Johanna Eisele , Michael Schnabel , Klaus Schultes , Stefan Grimm , Hans-Ulrich Petereit , Thomas Suefke
发明人： Christian Meier , Johanna Eisele , Michael Schnabel , Klaus Schultes , Stefan Grimm , Hans-Ulrich Petereit , Thomas Suefke
IPC分类号： A61K9/16 , A61K9/14
CPC分类号： A61K9/2027 , A61K9/5026 , C08F2/30 , C08F220/18 , C08F2220/1816 , C08F220/14 , C08F220/06
摘要： The invention relates to a dispersion suitable for use as coating agent and binder for pharmaceutical forms, having a solids content of 10–70% by weight consisting of a) from 90 to 99% by weight of a methacrylate copolymer consisting of at least 90% by weight of (meth)acrylate monomers containing neutral radicals and having a glass transition temperature Tg of from −20° C. to +20° C. as determined by the DSC method, and b) 1–10% by weight of a nonionic emulsifier having an HLB of from 15.2 to 17.3.
摘要翻译：本发明涉及适合用作药物形式的包衣剂和粘合剂的分散体，其固含量为10-70重量％

94. 发明申请

US20050281871A1 Methods for coating substrates for pharmaceutical uses with a mixture of two film-forming coating agents 审中-公开
标题翻译：用两种成膜包衣剂的混合物涂覆药物用基质的方法
公开(公告)号：US20050281871A1
公开(公告)日：2005-12-22
申请号：US10529636
申请日：2003-10-18
申请人： Hans-Ulrich Petereit , Christian Meier , Erna Roth
发明人： Hans-Ulrich Petereit , Christian Meier , Erna Roth
IPC分类号： A23L1/308 , A61K9/28 , A61K9/48 , A61K9/50 , A61K9/24
CPC分类号： A61K9/2893 , A23L33/25 , A61K9/284 , A61K9/2846 , A61K9/2866 , A61K9/4891 , A61K9/5026 , A61K9/5047 , A61K9/5089
摘要： The invention relates to methods for producing pharmaceuticals or parts of pharmaceuticals or food supplements or parts thereof, by coating substrates with a mixture of two film-forming coating agents that can contain other pharmaceutically standard additives, especially softeners and/or a pharmaceutical active ingredient.
摘要翻译：本发明涉及通过用可以含有其它药学标准添加剂，特别是软化剂和/或药物活性成分的两种成膜包衣剂的混合物涂覆基质来制备药物或药物的一部分或其食品补充剂或其部分的方法。

95. 发明申请

US20050154165A1 Ph-sensitive polymer 有权
标题翻译：敏感聚合物
公开(公告)号：US20050154165A1
公开(公告)日：2005-07-14
申请号：US10510371
申请日：2002-10-22
申请人： Hans-Ulrich Petereit , Christian Meier , Klaus Schultes , Marie Yessine , Jean-Christophe Leroux
发明人： Hans-Ulrich Petereit , Christian Meier , Klaus Schultes , Marie Yessine , Jean-Christophe Leroux
IPC分类号： A61K9/107 , A61K9/00 , A61K9/127 , A61K9/14 , A61K31/7105 , A61K31/711 , A61K38/00 , A61K39/395 , A61K45/00 , A61K47/32 , A61K47/48 , A61K48/00 , A61P1/04 , A61P1/16 , A61P1/18 , A61P3/06 , A61P3/10 , A61P9/10 , A61P17/00 , A61P17/06 , A61P19/02 , A61P19/06 , A61P21/04 , A61P25/00 , A61P25/16 , A61P25/28 , A61P27/02 , A61P29/00 , A61P31/04 , A61P31/14 , A61P31/18 , A61P31/20 , A61P31/22 , A61P35/00 , A61P37/02 , A61P37/06 , A61P37/08 , C08F220/06 , C08F220/18 , 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，它是一种（甲基）丙烯酸酯共聚物，它由20至65％（重量）的丙烯酸和/或甲基丙烯酸单元和80-35％（重量）的C 1 - 至（C 18） - （甲基）丙烯酸的烷基酯，其特征在于其分子量为1 000至50 000g / mol，并且导致至少60％的溶血在pH5.5下，在pH7.4下溶血小于5％，浓度为150mug / ml，在人红细胞的细胞毒性试验中。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。

96. 发明申请

US20050152977A1 Dosage form and method for producing the same 有权
标题翻译：用途及其制备方法
公开(公告)号：US20050152977A1
公开(公告)日：2005-07-14
申请号：US10512860
申请日：2004-03-02
申请人： Hans-Ulrich Petereit , Christian Meier , Klaus Schultes
发明人： Hans-Ulrich Petereit , Christian Meier , Klaus Schultes
IPC分类号： A61K9/28 , A61K9/32 , A61K9/24
CPC分类号： A61K9/2846 , Y02A50/473
摘要： The invention relates to a process for producing a coated drug form or a drug form in the form of an active ingredient matrix, by processing a copolymer, an active pharmaceutical ingredient, a core if present and/or pharmaceutically customary excipients in a conventional manner by melting, injection molding, extrusion, wet granulation, casting, dipping, spreading, spraying or compression to form a coated drug form and/or to form an active ingredient matrix, characterized in that a copolymer is used which is composed of 20 to 33% by weight methacrylic acid, 5 to 30% by weight methyl acrylate, 20 to 40% by weight ethyl acrylate and more than 10 to 30% by weight butyl methacrylate and, if desired, 0 to 10% by weight further vinylically copolymerizable monomers, with the proviso that the glass transition temperature of the copolymer in accordance with ISO 11357-2, section 3.3.3, is 55 to 70° C. The invention further relates to the drug form produced in accordance with the invention, to the copolymer, and to the use thereof.
摘要翻译：本发明涉及通过以常规方式加工共聚物，活性药物成分，核心（如果存在）和/或药学上常规的赋形剂来生产呈活性成分基质形式的包被药物形式或药物形式的方法熔融，注射成型，挤出，湿法制粒，浇铸，浸涂，铺展，喷雾或压缩以形成涂覆的药物形式和/或形成活性成分基质，其特征在于使用共聚物，其由20-33％的甲基丙烯酸，5至30重量％的丙烯酸甲酯，20至40重量％的丙烯酸乙酯和大于10至30重量％的甲基丙烯酸丁酯，以及如果需要，0至10重量％的进一步的乙烯基共聚单体，条件是根据ISO 11357-2，第3.3.3节的共聚物的玻璃化转变温度为55至70℃。本发明还涉及根据本发明生产的药物形式至th e共聚物，以及其用途。

97. 发明授权

US06420473B1 Acrylic enteric coating compositions 有权
标题翻译：丙烯酸肠溶组合物
公开(公告)号：US06420473B1
公开(公告)日：2002-07-16
申请号：US09501866
申请日：2000-02-10
申请人： Ramireddy Chittamuru , George Reyes , Thomas P. Farrell , Charles F. Vesey , Dev K. Mehra , Hans-Ulrich Petereit , Klaus Lehmann
发明人： Ramireddy Chittamuru , George Reyes , Thomas P. Farrell , Charles F. Vesey , Dev K. Mehra , Hans-Ulrich Petereit , Klaus Lehmann
IPC分类号： C08J312
CPC分类号： A61K9/2893 , A61K9/2813 , A61K9/2846 , A61K47/02
摘要： A non-toxic, edible, enteric film coating, dry powder composition for use in making an aqueous enteric suspension which may be used in coating pharmaceutical tablets comprises a) an acrylic resin, said resin comprising i) from 20 to 85 percent by weight of at least one alkyl acrylate or alkyl methacrylate moiety, ii) from 80 to 15 percent by weight of at least one vinyl or vinylidene moiety having a carboxylic acid group capable of salt formation, and iii) from 0 to 30 percent by weight of at least one other vinyl or vinylidene moiety copolymerizable with i) and ii), b) an alkalizing agent capable of reacting with the acrylic resin such that, after reaction, 0.1 to 10 mole percent of the acidic groups in 1a-ii) are present in the salt form, and c) a detackifier.
摘要翻译：可用于制备可用于包衣药物片剂的水性肠溶悬浮液的无毒，可食用的肠溶薄膜包衣干粉组合物包括a）丙烯酸树脂，所述树脂包含i）20至85重量％至少一种丙烯酸烷基酯或甲基丙烯酸烷基酯部分，ii）80至15重量％的至少一个具有能够形成盐的羧酸基团的乙烯基或亚乙烯基部分，和iii）至少0至30重量％可与i）和ii）共聚的另一个乙烯基或亚乙烯基部分，b）能够与丙烯酸类树脂反应的碱化剂，使得反应后，1a-ii）中的0.1〜10摩尔％的酸性基团存在于盐形式，和c）防粘剂。

98. 发明授权

US6063399A Adhesive binders for dermal or transdermal therapy systems 失效
标题翻译：用于皮肤或透皮治疗系统的粘合剂粘合剂
公开(公告)号：US6063399A
公开(公告)日：2000-05-16
申请号：US995986
申请日：1997-12-22
申请人： Manfred Assmus , Thomas Beckert , Guenter Bergmann , Stephanie Kaehler , Hans-Ulrich Petereit
发明人： Manfred Assmus , Thomas Beckert , Guenter Bergmann , Stephanie Kaehler , Hans-Ulrich Petereit
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％。

99. 发明授权

US5342646A Method for making carrier systems for biologically active materials 失效
标题翻译：制备生物活性物质载体体系的方法
公开(公告)号：US5342646A
公开(公告)日：1994-08-30
申请号：US979425
申请日：1992-11-19
申请人： Wolfgang Kleese , Dieter Kraemer , Hans-Ulrich Petereit , Klaus Lehmann , Werner Siol
发明人： Wolfgang Kleese , Dieter Kraemer , Hans-Ulrich Petereit , Klaus Lehmann , Werner Siol
IPC分类号： C07K17/08 , C12N11/08 , G01N33/545 , B05D7/00 , A61K9/16 , B05D1/12
CPC分类号： G01N33/545 , C07K17/08 , C12N11/08
摘要： What is disclosed is a method for preparing carrier systems, adaptable to the covalent bonding thereto of biologically active materials, consisting of a known solid support material having a surface coated with a polymer containing functional groups suitable for covalent bonding, by coating the support material with a film-forming polymer dispersion and a non-film-forming polymer dispersion, suitably in admixture, at least one of the two polymer dispersions containing a polymer having functional groups suitable for covalent bonding with a biologically active material.
摘要翻译：公开的是一种制备载体系统的方法，其适用于生物活性材料的共价键合，其由已知的固体支持材料组成，所述固体支持材料具有涂覆有包含适于共价键合的官能团的聚合物的表面，通过用一种成膜聚合物分散体和一种非成膜聚合物分散体，适当地混合两种聚合物分散体中的至少一种，其含有具有适于与生物活性材料共价键合的官能团的聚合物。

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