鸢尾苷元胃内漂浮型缓释片的制备及体外释放的研究

Preparation and release mechanism of tectorigenin intragastric floating sustained-release tablets

研究鸢尾苷元胃内漂浮型缓释片的制备工艺及释放机制。采用羟丙基甲基纤维素(HPMC_(K15M))、交联聚乙烯吡咯烷酮(PVPP)、十八醇、碳酸氢钠为辅料,湿法制粒压片,以体外漂浮性能和体外释放性能为考察指标,采用正交实验设计对处方进行筛选与优化。优化的处方为鸢尾苷元33.3%、HPMCK15 M16.7%、PVPP 20.0%、十八醇13.3%、碳酸氢钠5%、预胶化淀粉10.7%。制得的片剂在人工胃液中10 s内起漂,体外持续漂浮时间>12 h;10 h累积释放度在70%以上。Ritger-Peppas方程拟合分析表明,该缓释片有药物扩散和骨架溶蚀双重作用。鸢尾苷元胃内漂浮型缓释片外观与可压性良好,且具有良好的漂浮性能和释药特征。

To investigate the preparation technology and release mechanism of tectorigenin intragastric floating sustained-release tablets. The tablet was produced by wet granulation compression method,with hydroxypropyl methyl cellulose（ HPMCK15 M）,cross-linked polyvinyl pyrrolidone（ PVPP）,octadecanol and sodium bicarbonate as excipient. The prescriptions were screened and optimized by orthogonal experimental design with in vitro floating capacity and drug release characteristics as the evaluation indexes. The optimization results were as follows： tectorigenin 33. 3 %,HPMCK15 M16. 7 %,PVPP 20. 0 %,octadecanol 13. 3 %,sodium bicarbonate 5 %,and starch gel 10. 7 %. The prepared tablet can be floated within 10 s in the artificial gastric juice,lasting for 12 h in vitro,with a cumulative release rate of 70 % in 10 h. The analysis of Rritger-Peppas equation showed that the sustained-release tablet had two advantages of both drug diffusion and skeleton dissolution. The tablet had good appearance and compressibility,as well as favorable floating capacity and drug release characteristics.