环孢素缓释栓剂的研制

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其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.

Study on Ciclosporine Sustained-release Suppository

To prepare ciclosporin (CsA) sustained-release suppositories. Method; 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. Result: 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 t1/2 of microencapsulated suppository was extended significantly (P < 0.05) and AUC had a tendency to increase, compared to the oral solution. Conclusion: CsA microencapsulated suppository has the effect of detained delivery.