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    Active ingredient patch for low-melting and/or volatile active ingredients
    1.
    发明授权
    Active ingredient patch for low-melting and/or volatile active ingredients 失效
    用于低熔点和/或挥发性活性成分的活性成分贴剂

    公开(公告)号：US5527536A

    公开(公告)日：1996-06-18

    申请号：US367262

    申请日：1995-02-27

    申请人： Hans P. Merkle ,  Klaus Nagels ,  Dietrich Schacht ,  Hans-Michael Wolff

    发明人： Hans P. Merkle ,  Klaus Nagels ,  Dietrich Schacht ,  Hans-Michael Wolff

    IPC分类号： A61K9/70 ,  A61L15/58 ,  A61F13/00

    CPC分类号： A61K9/7053 ,  A61K9/7076 ,  A61L15/58

    摘要： The invention concerns a patch for the controlled release of readily available volatile active substances to the skin, the patch comprising a back layer and, bonded to it, a water-insoluble adhesive film consisting of a pressure-sensitive fusion adhesive, plus a detachable film covering the adhesive film. The patch is characterized in that the pressure-sensitive fusion adhesive contains a triple-block copolymer of polystyrene block copoly(ethylene/butylene) block polystyrene (SEBS) at a concentration of 10 to 80% by wt., and an active substance which, at the temperature at which the adhesive bonds, is a readily volatile liquid, and which is present at a concentration of 2.5 to 25% by wt.

    摘要翻译： PCT No.PCT / DE93 / 00638 Sec。 371日期：1995年2月27日 102（e）日期1995年2月27日PCT提交1993年7月17日PCT公布。 公开号WO94 / 02123 日期1994年2月3日。本发明涉及一种用于将容易获得的挥发性活性物质控制释放到皮肤上的贴剂，该贴剂包含背层并与其结合，由不溶于水的粘合剂组成的水不溶性粘合剂膜 熔融粘合剂，以及覆盖粘合剂膜的可拆卸膜。 该贴剂的特征在于，压敏熔融粘合剂含有浓度为10〜80重量％的聚苯乙烯嵌段共聚（乙烯/丁烯）嵌段聚苯乙烯（SEBS）的三嵌段共聚物和活性物质， 在粘合剂粘合的温度下，是易挥发的液体，其浓度为2.5至25重量％。

    Active ingredient patch for low-melting and/or volatile active ingredients
    2.
    发明授权
    Active ingredient patch for low-melting and/or volatile active ingredients 失效
    用于低熔点和/或挥发性活性成分的活性成分贴剂

    公开(公告)号：US5603948A

    公开(公告)日：1997-02-18

    申请号：US483312

    申请日：1995-06-07

    申请人： Hans P. Merkle ,  Klaus Nagels ,  Dietrich Schacht ,  Hans-Michael Wolff

    发明人： Hans P. Merkle ,  Klaus Nagels ,  Dietrich Schacht ,  Hans-Michael Wolff

    IPC分类号： A61K9/70 ,  A61L15/58 ,  A61F13/02

    CPC分类号： A61K9/7053 ,  A61K9/7076 ,  A61L15/58

    摘要： A method of preparing a patch for the controlled release of readily available volatile active substances to the skin is disclosed. The patch comprises a back layer, and, bonded to the back layer, a water-insoluble adhesive film consisting of a pressure-sensitive fusion adhesive, plus a detachable film covering the adhesive film. The pressure-sensitive fusion adhesive contains a triple-block copolymer of polystyrene block copoly(ethylene/butylene) block polystyrene at a concentration of 10 to 80% by wt., and an active substance at a concentration of 2.5 to 25% by weight, which is a readily volatile liquid at the temperature at which the adhesive bonds.

    摘要翻译： 公开了一种制备用于将容易获得的挥发性活性物质控制释放到皮肤上的贴剂的方法。 贴片包括背层，并且与背层结合由压敏熔融粘合剂组成的水不溶性粘合剂膜，以及覆盖粘合剂膜的可拆卸膜。 压敏熔融粘合剂含有浓度为10〜80重量％的聚苯乙烯嵌段共聚（乙烯/丁烯）嵌段聚苯乙烯和浓度为2.5〜25重量％的活性物质的三嵌段共聚物， 其在粘合剂粘合的温度下是易挥发的液体。

    Transdermal delivery system for the administration of rotigotine
    3.
    发明申请
    Transdermal delivery system for the administration of rotigotine 有权
    用于给予罗替戈汀的透皮递送系统

    公开(公告)号：US20050079206A1

    公开(公告)日：2005-04-14

    申请号：US10623864

    申请日：2003-07-22

    申请人： Dietrich Schacht ,  Mike Hannay ,  Hans-Michael Wolff

    发明人： Dietrich Schacht ,  Mike Hannay ,  Hans-Michael Wolff

    IPC分类号： A61K9/70 ,  A61K31/38

    CPC分类号： A61K9/7061 ,  A61K9/7069 ,  A61K9/7076 ,  A61K31/38

    摘要： An improved Transdermal Delivery System (TDS) comprising a backing layer inert to the components of the matrix, a self-adhesive matrix containing rotigotine and a protective foil or sheet to be removed prior to use, characterized in that the self-adhesive matrix consists of a solid or semi-solid semi-permeable polymer (1) wherein rotigotine in its free base form has been incorporated, (2) which is saturated with rotigotine and contains said rotigotine as a multitude of microreservoirs within the matrix, (3) which is highly permeable for the free base of rotigotine, (4) which is impermeable for the protonated form of rotigotine, (5) wherein the maximum diameter of the microreservoirs is less than the thickness of the matrix. is provided. Said TDS provides for enhanced flux of rotigotine across the TDS/skin interface.

    摘要翻译： 一种改进的透皮递送系统（TDS），其包括对基质的组分是惰性的背衬层，含有罗替戈汀的自粘性基质和在使用前被去除的保护性箔或片，其特征在于，所述自粘性基质由 已经掺入其游离碱形式的罗替戈汀的固体或半固体半透性聚合物（1），（2）其被罗替戈汀饱和并且含有所述罗替戈汀作为基质内的多个微储层，（3） 高度可渗透的罗替戈汀的游离碱，（4）其对于质子化形式的罗替戈汀是不可渗透的，（5）其中微储层的最大直径小于基质的厚度。 被提供。 所述TDS提供通过TDS /皮肤界面的增强的罗替戈汀的通量。

    Device for transdermal administration for the treatment of urinary tract disorders
    4.
    发明申请
    Device for transdermal administration for the treatment of urinary tract disorders 审中-公开
    透皮给药装置用于治疗尿路疾病

    公开(公告)号：US20050226919A1

    公开(公告)日：2005-10-13

    申请号：US10497199

    申请日：2002-09-12

    申请人： Frank Dressen ,  Dietrich Schacht ,  Hans-Michael Wolff

    发明人： Frank Dressen ,  Dietrich Schacht ,  Hans-Michael Wolff

    IPC分类号： A61K9/70 ,  A61K31/403 ,  A61K31/405 ,  A61K31/4439

    CPC分类号： A61K9/7061 ,  A61K31/403

    摘要： This invention provides a device containing a compound of formula (I), wherein R represents a saturated or unsaturated C2-7 aliphatic acyl group optionally substituted by one or more halogen atoms, a hydroxy group, a C1-6 alkoxy group, a carboxyl group, a C2-7 alkoxycarbonyl group, a 5 to 7-membered cycloalkyl group, a phenyl or naphthyl group; a C2-6 hydroxyalkyl group; an aliphatic acyloxyalkyl group having a C2-7 acyl group and a C1-6 alkyl group; a C1-6 alkyl group substituted by a C1-6 alkoxy group, a carboxyl group, a C2-7 alkoxycarbonyl group, a C2-7 alkoxycarbonyl group substituted by a phenyl or naphthyl group, a carbamoyl group, a mono- or di-(C1-6 alkyl)-substituted carbamoyl group or a cyano group; a benzoyl or naphthoyl group optionally substituted by one or more halogen atoms; a furoyl group or a pyridylcarbonyl group; and R1 represents a C1-6 alkyl group optionally substituted by one or more halogen atoms, a phenyl or a naphthyl group; the carbon atom marked “*” represents a carbon atom in (R)-configuration, (S)-configuration or a mixture thereof. The TTS is efficient in the treatment of urinary tract disorders, such as benign prostatic hypertrophy.

    摘要翻译： 本发明提供含有式（I）化合物的装置，其中R表示任选被一个或多个卤素原子取代的饱和或不饱和的C 2-7脂族酰基，羟基，C 羧基，C 2-7烷氧基羰基，5至7元环烷基，苯基或萘基; C 2-6羟基烷基; 具有C 2〜7酰基和C 1-6烷基的脂肪族酰氧基烷基; 被C 1-6烷氧基取代的C 1-6烷基，羧基，C 2-7烷氧基羰基， 被苯基或萘基取代的C 2〜2-7烷氧基羰基，氨基甲酰基，一或二 - （C 1-6烷基）取代的氨基甲酰基 或氰基; 任选被一个或多个卤素原子取代的苯甲酰基或萘甲酰基; 糠酰基或吡啶基羰基; R 1表示任选被一个或多个卤素原子，苯基或萘基取代的C 1-6烷基; 标有“*”的碳原子表示（R） - 构型，（S） - 构型或其混合物中的碳原子。 TTS有效治疗尿路疾病，如良性前列腺肥大。

    POLYVINYLPYRROLIDONE FOR THE STABILIZATION OF A SOLID DISPERSION OF THE NON-CRYSTALLINE FORM OF ROTIGOTINE
    6.
    发明申请
    POLYVINYLPYRROLIDONE FOR THE STABILIZATION OF A SOLID DISPERSION OF THE NON-CRYSTALLINE FORM OF ROTIGOTINE 有权
    用于稳定非结晶形式的固体分散体的聚丙烯吡咯烷酮

    公开(公告)号：US20120322845A1

    公开(公告)日：2012-12-20

    申请号：US13515067

    申请日：2010-12-22

    申请人： Hans-Michael Wolff ,  Christoph Arth ,  Luc Quere ,  Walter Müller

    发明人： Hans-Michael Wolff ,  Christoph Arth ,  Luc Quere ,  Walter Müller

    IPC分类号： C07D333/20 ,  A61P25/00 ,  A61P25/24 ,  A61K31/381 ,  A61P25/16

    CPC分类号： A61K9/7069 ,  A61K9/7053 ,  A61K31/381

    摘要： The present invention relates to a method for stabilizing rotigotine, the method comprising providing a solid dispersion comprising polyvinylpyrrolidone and a non-crystalline form of rotigotine, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6. The present invention also relates to a solid dispersion comprising a dispersing agent and a dispersed phase, said dispersed phase comprising rotigotine and polyvinylpyrrolidone, wherein the weight ratio of rotigotine to polyvinylpyrrolidone is in a range from about 9:3.5 to about 9:6, a pharmaceutical composition comprising such a solid dispersion, in particular a transdermal therapeutic system, as well as a method for the preparation thereof.

    摘要翻译： 本发明涉及一种稳定罗替戈汀的方法，该方法包括提供包含聚乙烯吡咯烷酮和非晶形罗替戈汀的固体分散体，其中罗替戈汀与聚乙烯吡咯烷酮的重量比在约9:3.5至约9:1的范围内， 6。 本发明还涉及包含分散剂和分散相的固体分散体，所述分散相包含罗替戈汀和聚乙烯吡咯烷酮，其中罗替戈汀与聚乙烯吡咯烷酮的重量比在约9:3.5至约9:6的范围内， 包含这种固体分散体，特别是透皮治疗系统的药物组合物以及其制备方法。

    NOVEL POLYMORPHIC FORM OF ROTIGOTINE AND PROCESS FOR PRODUCTION
    7.
    发明申请
    NOVEL POLYMORPHIC FORM OF ROTIGOTINE AND PROCESS FOR PRODUCTION 有权
    新型多元醇多元醇和生产工艺

    公开(公告)号：US20100311806A1

    公开(公告)日：2010-12-09

    申请号：US12744989

    申请日：2008-11-25

    申请人： Hans-Michael Wolff ,  Luc Quere ,  Jens Riedner

    发明人： Hans-Michael Wolff ,  Luc Quere ,  Jens Riedner

    IPC分类号： A61K31/381 ,  C07D333/20 ,  A61P25/16 ,  A61P25/24 ,  A61P25/00

    CPC分类号： C07D333/20

    摘要： The present invention relates to a novel polymorphic form of Rotigotine characterized by at least one of the following X-ray powder diffraction peaks: 12.04, 13.68, 17.72 and 19.01±0.2 (°2θ), measured with a Cu—Kαirradiation (1.54060), and a process for production thereof, which is useful for the manufacture of a stable medicament for treating or alleviating symptoms of Parkinson's Disease and other dopamine-related disorders.

    摘要翻译： 本发明涉及罗替戈汀的新型多晶型物，其特征在于以Cu-Kα辐射（1.54060）测量的以下X射线粉末衍射峰中的至少一个：12.04,13.68,17.72和19.01±0.2（°2） 及其制备方法，其可用于制备用于治疗或缓解帕金森病和其他多巴胺相关病症症状的稳定药物。

    NOVEL POLYMORPHIC FORM OF ROTIGOTINE AND PROCESS FOR PRODUCTION
    9.
    发明申请
    NOVEL POLYMORPHIC FORM OF ROTIGOTINE AND PROCESS FOR PRODUCTION 有权
    新型多元醇多元醇和生产工艺

    公开(公告)号：US20090143460A1

    公开(公告)日：2009-06-04

    申请号：US12324166

    申请日：2008-11-26

    申请人： Hans-Michael Wolff ,  Luc Quere ,  Jens Riedner

    发明人： Hans-Michael Wolff ,  Luc Quere ,  Jens Riedner

    IPC分类号： A61K31/381 ,  C07D333/20

    CPC分类号： C07D333/20

    摘要： The present invention relates to a novel polymorphic form of rotigotine characterized by at least one of the following powder X-ray diffraction peaks: 12.04, 13.68, 17.72 and 19.01±0.2 (° 2θ), measured with a Cu—Kα irradiation (1.54060 Å), and a process for production thereof, which is useful for the manufacture of a stable medicament for treating or alleviating symptoms of Parkinson's disease and other dopamine-related disorders.

    摘要翻译： 本发明涉及一种新型的罗替戈汀的多晶型物，其特征在于以Cu-Kalpha照射（1.54060埃）测量的以下粉末X射线衍射峰中的至少一种：12.04,13.68,17.72和19.01±0.2（°2θ） ）及其生产方法，其可用于制备用于治疗或缓解帕金森病和其他多巴胺相关疾病症状的稳定药物。