| abstract |
A novel crystalline form of the aldosterone receptor antagonist drug eplerenone (Form H) is disclosed which dissolves relatively rapidly in an aqueous medium. The present invention also relates to novel solvated crystalline forms of azeplerenone which, upon desolvation, may yield eplerenone H-form. The subject also covers amorphous eplerenone. The present invention also relates to a pharmaceutical composition comprising an eplerenone Form H, optionally together with one or more other solid forms of eplerenone, in a total amount of ca. 10 - approx. 1000 mg eplerenone in unit dosage form, further comprising one or more pharmaceutically acceptable excipients. The invention also relates to a process for the preparation of azeplerenone H-form and to the preparation of eplerenone H-formulated compositions. The invention also relates to the prevention and / or treatment of a process aldosterone-mediated condition or disorder; the method of administration comprising administering to the subject a therapeutically effective amount of eplererenone containing at least in part eplerenone H-form sulfur eplerenone. SHE |