To provide an aldosterone receptor antagonist drug eplerenone having a new crystalline form which exhibits relatively high physical stability at normal temperatures of storage and use.
A process for preparing Form L crystalline eplerenone is provided, and a drug substance selectively comprises 90 to 100% Form L eplerenone together with one or more other solid state forms of eplerenone, for example, Form H eplerenone. A pharmaceutical composition comprises about 10 to about 1,000 mg of a total unit dosage amount of eplerenone and, in addition, one or more excipients. A method for prophylaxis and/or treatment of an aldosterone-mediated condition or disorder comprises administering to a subject a therapeutically effective amount of eplerenone, wherein at least a fraction of the eplerenone present is Form L eplerenone.
GAUD HENRY T
GANSER SCOTT
LITTLE CLAY R
MUDIPALLI PARTH S
BORSCHARDT THOMAS B
CARLOS MARLON V
DESAI SUBHASH
FERRO LEONARD J
PIETZ MARK A
PILIPAUSKAS DANIEL R
SING YUEN-LUNG L
STAHL GLENN L
WIECZOREK JOSEPH J
YAN CHRIS Y
