发明名称 |
Eplerenone crystalline form exhibiting enhanced dissolution rate |
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.
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申请公布号 |
US2002038021(A1) |
申请公布日期 |
2002.03.28 |
申请号 |
US20000732208 |
申请日期 |
2000.12.07 |
申请人 |
BARTON KATHLEEN P.;BORCHARDT THOMAS B.;CARLOS MARLON V.;DESAI SUBHASH;FERRO LEONARD J.;GAUD HENRY T.;GANSER SCOTT S.;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. |
发明人 |
BARTON KATHLEEN P.;BORCHARDT THOMAS B.;CARLOS MARLON V.;DESAI SUBHASH;FERRO LEONARD J.;GAUD HENRY T.;GANSER SCOTT S.;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. |
分类号 |
C07D301/12;C07J1/00;C07J21/00;C07J31/00;C07J41/00;C07J53/00;C07J71/00;C12P33/00;C12P33/10;C12Q1/02;(IPC1-7):C07J17/00 |
主分类号 |
C07D301/12 |
代理机构 |
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