Eplerenone crystalline form exhibiting enhanced dissolution rate

• Main Authors: DESAI SUBHASH, PILIPAUSKAS DANIEL R, BORCHARDT THOMAS B, LITTLE CLAY R, PIETZ MARK A, BARTON KATHLEEN P, CARLOS MARLON V, STAHL GLENN L, WIECZOREK JOSEPH J, GANSER SCOTT S, YAN CHRIS Y, GAUD HENRY T, MUDIPALLI PARTHA S, SING YUEN-LUNG L, FERRO LEONARD J
• Format: Patent
• Language: English
• Published: 01.12.2005
• Edition: 7
• Subjects: CHEMISTRY; METALLURGY; ORGANIC CHEMISTRY; STEROIDS

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.