烯诺孕酮制剂研究进展  

Research progress of nestorone preparations

作　　者：黄婷[1] 曾佳[1] 相琳[2] 邵会石 李娜 王乾 

机构地区：[1]上海市计划生育科学研究所,国家人口和计划生育委员会计划生育药具重点实验室,上海生殖健康药具工程技术研究中心,上海200032 [2]大连大学,大连116622 [3]辽宁绿丹药业有限公司,丹东118009

出　　处：《中国新药杂志》2015年第4期409-414,共6页Chinese Journal of New Drugs

基　　金：国家“十二五”科技支撑计划课题(2012BAI31B02)

摘　　要：第4代孕激素烯诺孕酮(ST-1435,nestorone,NES)孕激素活性显著、无雄激素和雌激素活性、且不与性激素结合球蛋白结合,是长效避孕和哺乳期避孕的首选药物。NES口服无效,其制剂研究主要集中在皮下埋植剂、阴道环、透皮给药系统和微球注射剂等非口服给药形式,但目前无上市制剂。本文就NES制剂的国内外研究进展进行综述,为其进一步研究开发提供借鉴。Nestorone（ ST-1435 ;NES） , the fourth generation progestogen, which has high progestational potency with no androgenic or estrogenic activity and does not bind to sex hormone binding-globulin,is a candidate drug for the long-term and lactation contraception. Since NES is not active orally, researches of its preparations are mainly focusing on non-oral dosage forms such as subdermal implants, vaginal rings, transdermal drug delivery system, and microsphere injections. But till now there is no approved product of NES on the market. This paper re- views the research progress of NES preparations so as to provide reference for its further research and development.

关 键 词：烯诺孕酮 皮下埋植剂 阴道环 透皮给药系统 微球注射剂 

分 类 号：R979.2[医药卫生—药品]