采用多元定时释药技术制备雷公藤胃漂浮缓释胶囊的研究  

Preparation of gastric floating sustained-release capsules of Tripterygium wilfordii by using multiparticulate time-controlled release technology

作　　者：张伟[1,2] 宋洪涛[1] 张倩[3] 

机构地区：[1]南京军区福州总医院药学科,福建福州350025 [2]福建中医学院药学系,福建福州350003 [3]福建医科大学药学院,福建福州350004

出　　处：《中国中药杂志》2009年第22期2867-2871,共5页China Journal of Chinese Materia Medica

基　　金：福建省自然科学基金项目(2006J0116)

摘　　要：目的:采用多元定时释药技术制备雷公藤胃漂浮缓释制剂。方法:采用挤出滚圆法,以90%十八醇为助漂剂制得空白胃漂浮微丸。使用流化床包衣设备,制备载药胃漂浮微丸。再以低取代羟丙基纤维素作为内溶胀层材料,以乙基纤维素水分散体作为外控释层材料进行包衣制备胃漂浮定时释药包衣微丸。等量称取控释层包衣增重分别为0%,8%,12%,15%,22%的包衣微丸,混均装入硬胶囊中,即得雷公藤胃漂浮缓释胶囊。结果:当溶胀层处方及用量固定后,通过控制控释层的厚度,可使包衣微丸在预期的不同时间定时释药。将几种控释层增重不同的包衣微丸混合后制成雷公藤胃漂浮缓释胶囊,在溶出介质中,均立即起漂,包衣微丸8 h漂浮率大于80%,并于不同时间依次释药,从而在整体上呈现出一种缓释特征。结论:采用多元定时释药技术制备而成的雷公藤胃漂浮缓释胶囊具有良好的漂浮性能和缓释特性。Objective： To prepare gastric floating sustained-release formulation of Tripterygium wilfordii by using multiparticulate time-controlled release technology. Method： The intra-gastric floating blank-pellets were made by extrusion-spheronization method with 10% MCC as diluent and 90% cetylalcohol as floating assistant. The drug-loaded pellets were prepared in a fluid-bed coater with 1%HPMC, 0. 5%SDS and extraction of T. wilfordii as coating solution. The gastric floating time-controlled release pellets were prepared with 3% L-HPC, 1% HPMC and 1% SDS as the inner swelling layer and ethylcellulose aqueous dispersion as the outer controlled layer. Finally, gastric floating sustained-release capsules of T. wilfordii were developed by encapsulating the five kinds of coated pellets whose coating load were 0%, 8%, 12%, 15% and 22% at equivalent ratio in hard gelatin capsules. Result： After formulation and coating load of swelling layer was fixed, the coated pellets would release active compositions in the different time expectably through regulating coating level of controlled layer. Several kinds of coated pellets whose controlled layer had different coating load were mixed and encapsulated into gastric floating sustained-release capsules of T. wilfordii. The capsules could float immediately in the dissolution medium and the floating rate of pellets was more than 80% in 8 h. The various kinds of coated pellets could release active compositions in accordance with time and show a characteristic of sustained-releasing as a whole. Conclusion ： The gastric floating sustained-release capsules of T. wilfordii prepared by using muhiparticulate time-controlled release technology have effective floating behavior and sustained release characteristics.

关 键 词：雷公藤 微丸 胃漂浮 缓释胶囊 多元定时释药技术 

分 类 号：R283[医药卫生—中药学]