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    Eplerenone crystalline form exhibiting enhanced dissolution rate
    2.
    发明申请
    Eplerenone crystalline form exhibiting enhanced dissolution rate 审中-公开
    依普利酮结晶形式具有增强的溶解速率

    公开(公告)号：US20050267302A1

    公开(公告)日：2005-12-01

    申请号：US10727681

    申请日：2003-12-04

    申请人： Kathleen Barton ,  Thomas Borchardt ,  Marlon Carlos ,  Subhash Desai ,  Leonard Ferro ,  Henry Gaud ,  Scott Ganser ,  Clay Little ,  Partha Mudipalli ,  Mark Pietz ,  Daniel Pilipauskas ,  Yuen-Lung Sing ,  Glenn Stahl ,  Joseph Wieczorek ,  Chris Yan

    发明人： Kathleen Barton ,  Thomas Borchardt ,  Marlon Carlos ,  Subhash Desai ,  Leonard Ferro ,  Henry Gaud ,  Scott Ganser ,  Clay Little ,  Partha Mudipalli ,  Mark Pietz ,  Daniel Pilipauskas ,  Yuen-Lung Sing ,  Glenn Stahl ,  Joseph Wieczorek ,  Chris Yan

    IPC分类号： C07J21/00

    CPC分类号： C07J21/00

    摘要： A novel crystalline form (Form H) of the aldosterone receptor antagonist drug eplerenone is provided having a relatively rapid dissolution rate in aqueous media. Also provided are novel solvated crystalline forms of eplerenone that, when desolvated, can yield Form H eplerenone. Also provided is amorphous eplerenone. Pharmaceutical compositions are provided comprising Form H eplerenone, optionally accompanied by one or more other solid state forms of eplerenone, in a total unit dosage amount of eplerenone of about 10 to about 1000 mg, and further comprising one or more pharmaceutically acceptable excipients. Processes are provided for preparing Form H eplerenone and for preparing compositions comprising Form H eplerenone. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder is also provided, comprising administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form H eplerenone.

    摘要翻译： 提供醛固酮受体拮抗剂药物依普利酮的新型结晶形式（形式H），其在水性介质中具有相对快速的溶解速率。 还提供了eplerenone的新型溶剂化结晶形式，当脱溶时，可以产生H形式。 还提供了非依依普利酮。 提供了药物组合物，其包含H形式H eplerenone，任选地伴随有一种或多种其他固体形式的依普利酮，总单位剂量为约10至约1000mg的依普利酮，并且还包含一种或多种药学上可接受的赋形剂。 提供了制备H形式H eplerenone和制备包含H型肝素的组合物的方法。 还提供了用于预防和/或治疗醛固酮介导的病症或病症的方法，其包括向受试者施用治疗有效量的依普利酮，其中至少一部分所述的依普利酮是H型肾上腺素。