贺国芳  方淑贤  刘东

（华中科技大学同济医学院附属同济医院药学部，武汉，430030）

摘要：目的:制备环孢素的缓释栓剂。方法：制备了环孢素双层栓剂、阻滞栓剂及含部分环孢素微囊的微囊栓剂，并进行了体内外释药试验。结果：体外释放度试验显示微囊栓剂具有一定的缓释效果，为一级释放。家兔体内试验也表明，微囊栓剂的生物半衰期与口服液相比显著延长（P〈0.05 ），AUC有增加的趋势。结论：环孢微囊栓剂具有一定缓释作用。

关键词：环孢素；缓释栓剂

Study on Ciclosporine Sustained-release Suppository

He Guofang, Fang Shuxian, Liu Dong (Dept of Pharmacy, Tongji Hospital, Huazhong University of Science and Technology, Wuhan, 430030)

ABSTRACT Objective: To prepare ciclosporin (CsA) sustained-release suppositories. Methods: CsA two-storied suppository，retarded suppository and microencapsulated suppositories contented some CsA microcapsules were prepared. The experiment of release had been done in vitro and vivo. Results: In vitro, the microencapsulated suppository demonstrated sustained-release effects. It followed the first-order kinetic equation. At the same time, rabbits’ vivo experiments showed the t_1/2 of microencapsulated suppository was extended significantly(P﹤0.05) and AUC had a tendency to increase, compared to the oral solution. Conclusions: CsA microencapsulated suppository has the effect of detained delivery.

KEY WORDS Ciclosporin; Sustained-release suppository