公开(公告)号：EP1505072A3

公开(公告)日：2006-06-21

申请号：EP04020121.2

申请日：2000-12-04

申请人： Pharmacia Corporation

发明人： Barton, Kathleen ,  Borchardt, Thomas B. ,  Carlos, Marlon, V. ,  Desai, Subhash ,  Ferro, Leonard, J. ,  Gaud, Henry, T. ,  Ganser, Scott ,  Little, Clay, R. ,  Mudipalli, Partha S. ,  Pietz, Mark, A. ,  Pilipauskas, Daniel R. ,  Sing, Yuen-Lung, L. ,  Stahl, Glenn, L. ,  Wieczorek, Joseph, J. ,  Yan, Chris Y.

IPC分类号： C07J71/00 ,  A61K31/58 ,  A61P5/42

CPC分类号： C07J71/0015

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.