Development of Orally Active Dosage Forms for Steroids

摘要

The purpose of the project was the development of slow-release oral formulations of presently-marketed contraceptive preparations, ethynylestradiol (EE) and norethindrone (NET) or mestranol (MEE) and norethindrone acetate (NET acetate), and the evaluation of formulations in vitro and in vivo in order to determine if the dosage form would minimize daily peaks of the drug and reduce body burden while maintaining contraceptive efficacy. Steroid-containing microspheres which indicated good sustained release in vitro were evaluated in vivo in baboons and in clinical studies. The results of the baboon dosing studies indicated generally good sustained release of the orally ingested slow release formulations of norethindrone as compared to commercial tablets.