PROCESS FOR PREPARATION OF AN ORAL CONTROLLED RELEASE PHARMACEUTICAL COMPOSITION IN THE FORM OF ORAL OSMOTIC DELIVERY SYSTEM FOR ONCE-A-DAY THERAPY FOR TREATMENT AND PROPHYLAXIS OF CARDIAC AND CICULATORY DISEASES.

摘要

A process for the preparation of an oral controlled relase pharmaceutical composition in the form of oral osmotic system for once-a-day therapy for the treatment and prophylaxis of cardiac and circulatory diseases. The process comprises (a) mixing carvedilol or its pharmaceutically acceptable salt or ester, a polymeric swelling agent, one or more water-soluble compounds for inducing osmosis, and optionally other or more water-soluble compounds for inducing osmosis, and optionally other pharmaceutical excipients; (b) converting the mixture obtained in step (a) into a core by filling the mixture into capsules, or granulating or pelletizing the mixture by conventional means and compressing the granules or pellets so obtained into tablets. The core is surrounded with a semi-permeable membrane, such that the membrane is permeable to surrounding fluids but is impermeable to the contents of the core; and a passageway is provided through the membrane (b) for releasing the contents of the core. The oral osmotic delivery system thus formed releases the carvedilol plasma levels such that the ratio of peak plasma levles to plasma levels at 24 hours after administration, and the mean residence time of carvedilol are within a desirable range for said once-a-day therapy for the treatment and prophylaxis of cardiac and circulatory diseases.