环孢素缓释栓剂的制备及体外释放度研究

Preparation and Dissolution of Cyclosporin Sustained-Release Suppositories

目的 制备环孢素缓释栓剂 ,并对其体外释放进行研究。方法 先用复凝聚法将环孢素制成微囊 ,进而制成微囊栓剂 ,并与普通环孢素栓剂作对照 ,进行体外释放度研究。结果 环孢素微囊及其微囊栓剂的T50、Td、T80 比其普通栓剂明显延长 ,存在极显著差异 (P <0 0 1) ,且环孢素微囊栓剂的T50、Td、T80 也比其微囊明显延长 ,存在极显著差异 (P <0 0 1)。结论 环孢素微囊及其微囊栓剂均具有一定的缓释作用 ,且环孢素微囊栓剂的缓释作用时间更长。

Objective To study the preparation and dissolution of cyclosporin sustained release suppositories. Methods Cyclosporin microcapsules were prepared using complex coacervation. Then the sustained release suppositories were prepared using microencapsulated cyclospoin. The dissolution rate of cyclosporin from microcapsules and from microencapsulated suppositories were observed and compared with ordinary suppositories. Results The T 50 , Td, T 80 of cyclosporin from microcapsules and from microencapsulated suppositories was much longer than that from the ordinary suppositories ( P <0 01). The T 50 , Td, T80 of cyclosporin microencapsulated suppositories were longer than those of other microcapsules ( P <0 01). Conclusion Cyclosporin microcapsules and the microencapsulated suppositories demonstrated sustained release effects to some degrees. Especially, the sustained release effects of the cyclosporin microencapsulated suppositories were more satisfactory.