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    pH-sensitive polymer
    2.
    发明授权
    pH-sensitive polymer 有权
    pH敏感聚合物

    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。

    Macroporous material in the form of plastic pearls
    5.
    发明授权
    Macroporous material in the form of plastic pearls 失效
    大孔材料以塑料珠的形式

    公开(公告)号：US07381552B2

    公开(公告)日：2008-06-03

    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： C12N11/08 ,  G01N33/545 ,  C07K17/08

    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％。

    Macroporous material in the form of plastic pearls
    6.
    发明申请
    Macroporous material in the form of plastic pearls 失效
    大孔材料以塑料珍珠的形式

    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％。

    Dosage form and method for producing the same
    7.
    发明授权
    Dosage form and method for producing the same 有权
    用途及其制备方法

    公开(公告)号：US07498044B2

    公开(公告)日：2009-03-03

    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： A61K9/14 ,  A61K9/16 ,  A61K9/20 ,  A61K9/48

    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，浸渍，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至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。

    Dosage form and method for producing the same
    9.
    发明申请
    Dosage form and method for producing the same 有权
    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。