尼群地平胶囊自乳化释药系统处方优化研究

Studies on Optimizing the Formula of Nitrendipine Self-emulsifying Drug Delivery System

目的 :优化尼群地平自乳化释药系统处方。方法 :以尼群地平在不同种类及比例的油相、表面活性剂中的溶解度为考察指标 ,筛选尼群地平自乳化释药系统处方。结果 :尼群地平自乳化释药系统处方为尼群地平、肉豆寇酸异丙酯、Labrasol、Tween 80、十二烷基硫酸钠 ,该处方所形成的微乳平均粒径为 11 1nm ,在溶出介质蒸馏水、0 1mol/LHCl、pH 6 8磷酸盐缓冲液中的溶出度无明显差异 ,4 5min时的溶出度均在 75 %以上。结论 :按优化处方制得的尼群地平自乳化释药系统大大提高了尼群地平在水中的溶出度。

AIM:To optimize the formula of nitrendipine self-emulsifying drug delivery system.METHOD:Screening the formula of nitrendipine self-emulsifying drug delivery system on the basis of the solubility of nitrendipine in various kinds and ratios of surfactants and oil phases.RESULT: The formula of nitrendipine self-emulsifying drug delivery system was composed of Nitrendipine/IPM/Labrasol/Tween-80/SLS.It can create microemulsion droplets with a mean droplet size of 11.1 nm.The dissolution has no significant difference in distilled water,0.1 mol/L hydrochloric acid and phosphorate buffer,which was over 75% at 45 min.CONCLUSION:The dissolution of nitrendipine in water was significantly increased by using optimized formula of nitrendipine self-emulsifying drug delivery system.