星点设计－效应面法优化葛根素自微乳化给药系统.docVIP

PAGE PAGE 1 编号 20111 编号 201111192 刊用形式 论著 江兴龙1，贾运涛2，张良珂1*，田 睿3，滕永真3 （1. 重庆医科大学 药学院，重庆 400016；2. 重庆医科大学附属儿童医院 药剂科，重庆 400010；3. 重庆医科大学 生命科学院，重庆 400016） ［摘要］ 目的 葛根素自微乳化释药系统的制备优化及评价。方法 通过测定葛根素在各辅料中的溶解度，处方配伍实验，绘制伪三元相图筛选自微乳化释药系统组分；以葛根素在不同自微乳处方中的平衡溶解度和粒径为指标，采用星点设计－效应面优化法，确定较优处方；并用透析袋扩散法对葛根素自微乳的体外释药性质进行考察研究。结果 葛根素自微乳较优处方组成为：ODO-Cremophor RH40-Transcutol P，比例为17.5∶55.0∶27.5，葛根素在最优处方中的溶解度为51.27 mg.g-1，是其蒸馏水中溶解度的9.22倍，用蒸馏水稀释后平均粒径为21.51 nm。结论 成功制备了葛根素自微乳，可显著提高葛根素的溶解度；应用星点设计－效应面优化法能够快速方便的得到葛根素自微乳化给药系统的较优处方。 ［关键词］ 葛根素；自微乳化给药系统；星点设计-效应面法 ［中图法分类号］ ［文献标识码］ A Optimization of the self-microemulsifying drug delivery system of puerarin by the central composite design-response surface methodology Jiang Xinglong1,2, Jia Yuntao2, Zhang Liangke1*, Tian Rui3, Teng Yongzhen3, (1. School of Pharmacy, Chongqing Medical University, Chongqing 400016, China; 2. Department of Pharmacy, Children’s Hospital of Chongqing Medical University, Chongqing 400010, China; 3. Institute of Life Sciences, Chongqing Medical University, Chongqing 400016, China) ［Abstract］ Objective To prepare the self-microemulsifying drug delivery system (SMEDDS) of puerarin and study its release characteristics in vitro. Methods Formulation of puerarin SMEDDS was screened by solubility experiment, compatibility test and pseudo-ternary phase diagrams. According to the equilibrium solubility of puerarin in blank SMEDDS, the optimized formulation was determined by the central composite design-response surface methodology. The release of puerarin SMEDDS in different release medium were measured. Results The optimum formulation of puerarin SMEDDS was composed of ODO/Cremophor RH40/Transcutol P with weight ratio of 17.5∶55.0∶27.5.The solubility of puerarin in the optimum formulation is 51.27 mg.g-1, which is 9.22 times of that in the distilled water. The average particle size was 21.51 nm. Conclusion Puerarin SMEDDS were prepared successfully and could increase the solubility of