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    SOLID-STATE FORM OF CELECOXIB HAVING ENHANCED BIOAVAILABILITY
    1.
    发明公开
    SOLID-STATE FORM OF CELECOXIB HAVING ENHANCED BIOAVAILABILITY 无效
    美国芝加哥大学芝加哥大学

    公开(公告)号：EP1150959A1

    公开(公告)日：2001-11-07

    申请号：EP00982255.2

    申请日：2000-12-06

    申请人： Pharmacia Corporation

    发明人： HAGEMAN, Michael, J. ,  HE, Xiaorong ,  KARARLI, Tugrul, T. ,  MACKIN, Lesley, A. ,  MIYAKE, Patricia, J. ,  ROHRS, Brian, R. ,  STEFANSKI, Kevin, J.

    IPC分类号： C07D231/12 ,  A61K31/415 ,  A61P29/00

    CPC分类号： C07D231/12 ,  A61K9/0007 ,  A61K9/14 ,  A61K9/145 ,  A61K9/146 ,  A61K9/1635 ,  A61K9/1652 ,  A61K9/2018 ,  A61K9/2027 ,  A61K9/2054 ,  A61K9/2059 ,  A61K9/209 ,  A61K9/5084 ,  A61K9/5161 ,  A61K31/415 ,  A61K31/635 ,  A61K47/34 ,  C07D213/61 ,  C07D261/08 ,  C07D307/58 ,  C07D311/58

    摘要： The selective cyclooxygenase-2 inhibitory drug celecoxib is provided in amorphous form. Also provided is a celecoxib drug substance wherein the celecoxib is present, in at least a detectable amount, as amorphous celecoxib. Also provided is a celecoxib-crystallization inhibitor composite comprising particles of amorphous celecoxib or a celecoxib drug substance of the invention in intimate association with one or more crystallization inhibitors, for example polymers. Also provided is a pharmaceutical composition comprising such a celecoxib-crystallization inhibitor composite and one or more excipients. Also provided are processes for preparing amorphous celecoxib, a celecoxib drug substance of the invention, a celecoxib-crystallization inhibitor composite of the invention, and a pharmaceutical composition of the invention. Also provided is a method of treating a medical condition or disorder in a subject where treatment with a cyclooxygenase-2 inhibitor is indicated, comprising administering, for example orally, a composition of the invention in a therapeutically effective amount.

    摘要翻译： 选择性环加氧酶-2抑制药塞来昔布以非晶形式提供。 还提供塞来考昔药物，其中塞来昔布以至少可检测量存在，作为无定形塞来昔布。 还提供了塞来昔布结晶抑制剂复合物，其包含与一种或多种结晶抑制剂例如聚合物紧密结合的本发明的无定形塞来昔布或塞来昔布药物物质的颗粒。 还提供了包含这种塞来昔布结晶抑制剂复合物和一种或多种赋形剂的药物组合物。 还提供了制备本发明的塞来昔布药物，本发明的塞来昔布结晶抑制剂复合物和本发明的药物组合物的无定形塞来昔布的制备方法。 还提供了一种治疗受试者的医疗状况或病症的方法，其中所述方法是用环氧合酶-2抑制剂进行治疗，包括以治疗有效量施用例如口服本发明组合物。