1 0 0 0 難水溶性薬物のエマルションからの消化管吸収機構に関する研究
1 0 0 0 OA 酢酸リュープロレリン徐放性注射剤
- 著者
- 戸口 始 小川 泰亮 岡田 弘晃 山本 眞樹
- 出版者
- 公益社団法人 日本薬学会
- 雑誌
- YAKUGAKU ZASSHI (ISSN:00316903)
- 巻号頁・発行日
- vol.111, no.8, pp.397-409, 1991-08-25 (Released:2008-05-30)
- 参考文献数
- 61
- 被引用文献数
- 10 14
Leuprorelin (leuprolide, D-Leu6-(des-Gly10-NH2)-LH-RH ethylamide) acetate is a superactive agonist of luteinizing hormone-releasing hormone (LH-RH). We developed once-a-month injectable microcapsules of this agonist by our novel in-water drying method. This depot formulation can release the drug at an apparent zero-order rate over one month with bioerosion of copoly (lactic/glycolic acid) utilized as a wall material of the polycore microcapsules. A dramatic prolonged depression of pituitary-gonadal axis, chemical castration, was achieved by the once-a-month injection in experimental animals ; it expects a reliable effcacy for treating hormone-dependent prostatic, breast cancers and endometriosis. Studies on the dosage design of this new delivery system of leuprorelin are summarized.