| 摘要 |
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 ACCOMPINED BY ONE OR MORE OTHER SOLID STATE OF EPLERENONE, IN A TOTAL UNIT DOSAGE AMOUNT OF EPLERERIONE OF ABOUT 10 TO 100 MG, AND FURTHER COMPRISING ONE OR MORE PHARMACEUTICALLY ACCEPTABLE EXCIPIENTS.PROCESS ARE PROVIDED FOR PREPARING FORM H EPLERENONE AND FOR PREPARING COMPRISING FORM H EPLERENONE. A METHOD FOR PROPHYLAXIS AND/OR TREATMENT OF AN ALDOSTERONE-MEDIATED CONDITION OR DISORDER IS ALSO PROVIDE COMPRISING ADMINISTERING TO A SUBJECT A THERAPEUTICALLY EFFECTIVE AMOUNT OF EPLERENONE WHEREIN AT LEAST A FRACTION OF THE EPLERENONE PRESENT IS FORM H ELPERENONE.
|
