| abstract |
A process for preparing amorphous eplerenone is disclosed, wherein the process comprises: (a) a step of forming a dispersion of eplerenone in water; (b) a step of flash freezing the dispersion; and (c) a step of freeze drying the frozen dispersion to form amorphous eplerenone. Amorphous eplerenone is useful as an intermediate in the preparation of crystalline Form H and crystalline Form L of eplerenone. In addition, it is believed that amorphous eplerenone possesses a different dissolution rate compared to its crystalline Forms and, where amorphous eplerenone is present in a pharmaceutical composition and where dissolution of eplerenone in the gastrointestinal tract is the rate-controlling step for delivery of the eplerenone to the target cells, such amorphous eplerenone can provide different bioavailability relative to Form H and Form L. |