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    IMPLANT HAVING A CORE AND A TUBE ENCASING THE CORE
    1.
    发明申请
    IMPLANT HAVING A CORE AND A TUBE ENCASING THE CORE 审中-公开
    具有核心和管子的植入物加入核心

    公开(公告)号：US20130297040A1

    公开(公告)日：2013-11-07

    申请号：US13979642

    申请日：2012-01-16

    申请人： Jacques Donnez ,  Anne Van Langendonkt ,  Sylvie Defrère ,  Jean-Michel Foidart ,  Christine Jérome ,  Brigitte Evrard ,  Raphaël Riva ,  Fabrice Krier ,  Mélanie Mestdagt

    发明人： Jacques Donnez ,  Anne Van Langendonkt ,  Sylvie Defrère ,  Jean-Michel Foidart ,  Christine Jérome ,  Brigitte Evrard ,  Raphaël Riva ,  Fabrice Krier ,  Mélanie Mestdagt

    IPC分类号： A61K9/00

    CPC分类号： A61K9/00 ,  A61K9/0024 ,  A61K31/138 ,  A61K31/192 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/565 ,  A61K31/566 ,  A61K31/567 ,  A61K31/57 ,  A61K31/635 ,  A61K38/09

    摘要： The present invention relates to an implant comprising: —a core material comprising polydimethylsiloxane or at least one hydrogel polymer; —a tube encasing said core material comprising an ethylene vinyl acetate polymer or at least one hydrogel polymer; —a sealant for closure of the open ends of said tube comprising polydimethylsiloxane or a mono-, di-, or triacetoxy derivative thereof, or at least one hydrogel polymer; and —at least one active ingredient; wherein said at least one active ingredient is selected from the group comprising celecoxib, sulindac, tamoxifen, oestrogen, oestradiol, ethinyl oestradiol, mestranol, dienogest, norgestrel, levonorgestrel, desogestrel, norgestimate, ethynodiol diacetate, leuprorelin, buserelin, gonrelin, triptorelin, nafarelin, deslorelin, histrelin, and supprelin; and with the proviso that when the sealant is said at least one hydrogelpolymer, the core material comprises polydimethylsiloxane. Furthermore, the invention relates to an implant for use as a medicament. In particular, the invention relates to an implant for use in the treatment of endometriosis.

    摘要翻译： 本发明涉及一种植入物，其包含： - 包含聚二甲基硅氧烷或至少一种水凝胶聚合物的核心材料; - 包围所述芯材料的管，其包含乙烯乙酸乙烯酯聚合物或至少一种水凝胶聚合物; - 用于封闭所述管的开口端的密封剂，其包含聚二甲基硅氧烷或其单 - ，二 - 或三乙酰氧基衍生物或至少一种水凝胶聚合物; 和至少一种活性成分; 其中所述至少一种活性成分选自塞来昔布，舒林酸，他莫昔芬，雌激素，雌二醇，炔雌醇，雌孕酮，依诺孕，炔诺孕酮，左炔诺孕酮，去氧孕烯，诺孕酯，炔雌醇二乙酸酯，亮丙瑞林，布舍瑞林，天冬氨素，曲普瑞林， ，deslorelin，histrelin和supprelin; 并且条件是当密封剂被称为至少一种水凝胶聚合物时，芯材料包括聚二甲基硅氧烷。 此外，本发明涉及用作药物的植入物。 特别地，本发明涉及用于治疗子宫内膜异位症的植入物。

    Pharmaceutical compositions of pyrimidine-2,4,6-triones
    2.
    发明申请
    Pharmaceutical compositions of pyrimidine-2,4,6-triones 审中-公开
    嘧啶-2,4,6-三硝基苯胺的药物组合物

    公开(公告)号：US20070191404A1

    公开(公告)日：2007-08-16

    申请号：US10594162

    申请日：2005-03-31

    申请人： Pierre Bartsch ,  Didier Cataldo ,  Richard Endele ,  Brigitte Evrard ,  Jean-Michel Foidart ,  Hans-Willi Krell ,  Gerd Zimmermann

    发明人： Pierre Bartsch ,  Didier Cataldo ,  Richard Endele ,  Brigitte Evrard ,  Jean-Michel Foidart ,  Hans-Willi Krell ,  Gerd Zimmermann

    IPC分类号： A61K31/515

    CPC分类号： A61K9/0075 ,  A61K9/0078 ,  A61K31/198 ,  A61K31/515 ,  A61K47/183 ,  A61K47/6951 ,  B82Y5/00 ,  A61K2300/00

    摘要： It was surprisingly found that a-trioxopyrimidine-cyclodextrin-complex formed of a trioxopyrimidine derivative represented by the below-described formula (I) and a water-soluble cyclodextrin (further abbreviated as CD) exhibits enhanced water solubility, excellent stability, and low topical stimulation and is useful as a therapeutic agent. Accordingly, the present invention provides a trioxopyrimidine-cyclodextrin complex formed of a trioxopyrimidine derivative or a salt thereof and a cyclodextrin, preferably α-, β- or γ-cyclodextrin or a water-soluble cyclodextrin derivative (water-soluble being defined as a solubility of at least 0.5 gr/100 ml water at 25° C.), wherein the trioxopyrimidine derivative is represented by formula (I). It was furthermore found that such a trioxopyrimidine complex with cyclodextrin and an adjuvant such as L-lysine or L-arginine show improved water solubility and bioavailability, excellent stability, and low topical stimulation and is useful as a therapeutic agent.

    摘要翻译： 令人惊奇地发现由下式（I）表示的三氧嘧啶衍生物和水溶性环糊精（进一步缩写为CD）形成的α-三氧嘧啶 - 环糊精复合物显示出增强的水溶性，优异的稳定性和低的局部 刺激并且可用作治疗剂。 因此，本发明提供由三氧嘧啶衍生物或其盐与环糊精形成的三氟嘧啶 - 环糊精复合物，优选α-，β-或γ-环糊精或水溶性环糊精衍生物（水溶性定义为溶解度 在25℃下为至少0.5gr / 100ml水），其中三氧嘧啶衍生物由式（I）表示。 此外，发现这种与环糊精和L-赖氨酸或L-精氨酸等佐剂的三氧嘧啶配合物显示改善的水溶性和生物利用度，优异的稳定性和低的局部刺激，并且可用作治疗剂。