ウイテプゾール, エチレン-酢酸ビニル共重合体混合系新規基剤を用いたプロゲステロン坐剤

概要

論文の詳細を見る
A sustained release suppository containing progesterone (mixed suppository) was prepared to treat the luteal phase defect. A mixture of ethylene-vinyl acetate copolymer (EVA) and Witepsol-W35 was used as the suppository base. Characteristics of the mixed suppositories using various types of EVA were compared with those of Witepsol-W35 alone (control suppository). Determined as physical characteristics were hardness, DSC peak temperature, heat of fusion and release profiles of progesterone. Furthermore, the plasma concentration profiles of progesterone observed from suppositories were measured in rabbits. The sustained release of progesterone from the mixed suppository was observed in the beads cylindrical filter method. When the mixed suppositories were administered to the vagina of rabbits, some part of the suppository remained after 3 hours though nothing remained the control suppository. The Pharmacokinetic parameters obtained from the plasma concentration profiles suggested the sustained release property of progesterone in the biophase when the mixed suppository was administered. With this mixed suppository, the concentrations of progesterone in the vagina, cervical canal and uterus at 3 hours after the administration were higher than those of the control suppository. These results suggest that the mixed suppository could be useful as a dosage form for replacement therapy of progesterone.
日本医療薬学会の論文
1994-12-20