雷公藤胃漂浮缓释片的制备和质量评价

目的 研制雷公藤胃漂浮缓释片,考察其漂浮和释药性能.方法 采用粉末直接压片法制备雷公藤胃漂浮缓释片,以漂浮性能、雷公藤总二萜内酯的释放度为考察指标,进行处方筛选,并采用正交设计实验对处方进行优化.结果 以羟丙基甲基纤维素(HPMC_(K4M))为骨架材料,十六醇为助漂剂,碳酸氢钠为产气剂,聚维酮为致孔剂,制备了一天给药两次的胃内漂浮型缓释片.该制剂在人工胃液中立即起漂,2h释放约30%,6 h释放约60%,12 h释放90%以上,满足12 h释放要求,体外释药规律符合Higuchi方程,说明本缓释片属于药物扩散和骨架溶蚀混合控释机制.结论 研制的雷公藤胃漂浮缓释片具有良好的漂浮性能和释药特性.

Preparation of gastric floating sustained-release tablets of Triperygium wilfordii and its quality evaluation

Objective To prepare gastric floating sustained-release tablets of Triperygium wilfordii and study its behavior of floating and release characteristics. Methods The sustained-release tablets were prepared by direct powder compared to tablets technique. The floating and release of total diterpene-lactones were used as indicators to evaluate and optimize the formulation. Then the formulation was optimized by influential factors and orthogonal design test. Results The gastric floating sustained-release tablets which was taken orally twice one day, were prepared with HPMC_(K4M) as matrix, cetyI alcohol as floating assistant, sodium bicarbonate as gas-producer, PVP as poremaking. The tablets released 30% in 2 h, 60% in 6 h, exceeding 90% in 12 h, the release behavior of the tablets was fitted to Higuchi equation,and it was properly characterized by the drug diffusion and bulk erosion mechanism. Conclusion Gastric floating sustained-release tablets of T. wilfordii prepared has good behavior of floating and release characteristics.