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    Multilayer dosage form comprising a matrix that influences release of a modulatory substance
    91.
    发明申请
    Multilayer dosage form comprising a matrix that influences release of a modulatory substance 审中-公开
    包含影响调节物质释放的基质的多层剂型

    公开(公告)号：US20070042045A1

    公开(公告)日：2007-02-22

    申请号：US10573019

    申请日：2004-09-15

    申请人： Rosario Lizio ,  Hans-Ulrich Petereit ,  Manfred Assmus ,  Herna Ravishankar

    发明人： Rosario Lizio ,  Hans-Ulrich Petereit ,  Manfred Assmus ,  Herna Ravishankar

    IPC分类号： A61K9/24

    CPC分类号： A61K9/5078 ,  A61K9/5026

    摘要： The invention relates to a multilayer pharmaceutical form for controlled active ingredient release, essentially comprising a) optionally a neutral core (nonpareilles), b) an inner controlling layer comprising a substance having a modulating effect, which is embedded in a matrix which influences the delivery of the modulatory substance and which comprises pharmaceutically usable polymers, waxes, resins and/or proteins, and where appropriate an active ingredient, c) an active ingredient layer comprising an active pharmaceutical ingredient and, where appropriate, a substance having a modulating effect, d) an outer controlling layer comprising at least 60% by weight of one or a mixture of a plurality of (meth)acrylate copolymers composed of 98 to 85 C1 to C4 alkyl esters of (meth)acrylic acid and 2 to 15% by weight of methacrylate monomers with a quaternary ammonium group in the alkyl radical, and, where appropriate, further water-insoluble pharmaceutically usable polymers, where the layers may additionally and in a manner known per se comprise pharmaceutically usual excipients.

    摘要翻译： 本发明涉及用于受控活性成分释放的多层药物形式，其基本上包括a）任选的中性核心（非矫正剂），b）内部控制层，其包含具有调节作用的物质，其嵌入影响递送的基质中 的调节物质，并且其包含药学上可用的聚合物，蜡，树脂和/或蛋白质，并且在适当的情况下为活性成分，c）活性成分层，其包含活性药物成分和适当时具有调节作用的物质，d ）外部控制层，其包含至少60重量％的由98至85℃1至C 4的至少一种或多种（甲基）丙烯酸酯共聚物的混合物， （甲基）丙烯酸的烷基酯和2至15重量％的在烷基中具有季铵基团的甲基丙烯酸酯单体，以及在适当情况下进一步的水不溶性药学上可接受的聚 其中层可以另外地以本身已知的方式包含药学上通常的赋形剂。

    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
    93.
    发明申请
    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
    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。

    Granulate or powder for producing coating or binding agents for medicaments
    96.
    发明申请
    Granulate or powder for producing coating or binding agents for medicaments 有权
    用于生产药物的涂层或粘合剂的颗粒或粉末

    公开(公告)号：US20050197434A9

    公开(公告)日：2005-09-08

    申请号：US10489856

    申请日：2003-07-08

    申请人： Hans-Ulrich Petereit ,  Christian Meier ,  Erna Roth ,  Andreas Gryczke

    发明人： Hans-Ulrich Petereit ,  Christian Meier ,  Erna Roth ,  Andreas Gryczke

    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。

    Dosage form and method for producing the same
    98.
    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。

    Adhesive binders for dermal or transdermal therapy systems
    99.
    发明授权
    Adhesive binders for dermal or transdermal therapy systems 失效
    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％。