Title:
EPLERENONE CRYSTALLINE FORM EXHIBITING ENHANCED DISSOLUTION RATE
Document Type and Number:
WIPO Patent Application WO2001042272
Kind Code:
A9
Abstract:
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.
Inventors:
BARTON KATHLEEN (US)
BORCHARDT THOMAS B (US)
CARLOS MARLON V (US)
DESAI SUBHASH (US)
FERRO LEONARD J (US)
GAUD HENRY T (US)
GANSER SCOTT (US)
LITTLE CLAY R (US)
MUDIPALLI PARTHA S (US)
PIETZ MARK A (US)
PILIPAUSKAS DANIEL R (US)
SING YUEN-LUNG L (US)
STAHL GLENN L (US)
WIECZOREK JOSEPH J (US)
YAN CHRIS Y (US)
BORCHARDT THOMAS B (US)
CARLOS MARLON V (US)
DESAI SUBHASH (US)
FERRO LEONARD J (US)
GAUD HENRY T (US)
GANSER SCOTT (US)
LITTLE CLAY R (US)
MUDIPALLI PARTHA S (US)
PIETZ MARK A (US)
PILIPAUSKAS DANIEL R (US)
SING YUEN-LUNG L (US)
STAHL GLENN L (US)
WIECZOREK JOSEPH J (US)
YAN CHRIS Y (US)
Application Number:
PCT/US2000/032416
Publication Date:
December 12, 2002
Filing Date:
December 04, 2000
Export Citation:
Assignee:
PHARMACIA CORP (US)
BARTON KATHLEEN (US)
BORCHARDT THOMAS B (US)
CARLOS MARLON V (US)
DESAI SUBHASH (US)
FERRO LEONARD J (US)
GAUD HENRY T (US)
GANSER SCOTT (US)
LITTLE CLAY R (US)
MUDIPALLI PARTHA S (US)
PIETZ MARK A (US)
PILIPAUSKAS DANIEL R (US)
SING YUEN-LUNG L (US)
STAHL GLENN L (US)
WIECZOREK JOSEPH J (US)
YAN CHRIS Y (US)
BARTON KATHLEEN (US)
BORCHARDT THOMAS B (US)
CARLOS MARLON V (US)
DESAI SUBHASH (US)
FERRO LEONARD J (US)
GAUD HENRY T (US)
GANSER SCOTT (US)
LITTLE CLAY R (US)
MUDIPALLI PARTHA S (US)
PIETZ MARK A (US)
PILIPAUSKAS DANIEL R (US)
SING YUEN-LUNG L (US)
STAHL GLENN L (US)
WIECZOREK JOSEPH J (US)
YAN CHRIS Y (US)
International Classes:
A61P1/16; A61P9/04; A61K31/58; A61P9/12; A61P43/00; C07J71/00; C07J75/00; (IPC1-7): C07J1/00; A61K31/58
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