和厚朴酚自微乳化给药系统的研究

Development of self-microemulsifying drug delivery system for honokiol

目的筛选并优化了和厚朴酚自微乳化给药系统(honokiol-SMEDDS)的处方。方法利用溶解度,辅料配伍实验及伪三元相图筛选空白处方,以粒径和体外释放评价为指标选取最佳处方。结果优化后的honokiol-SMEDDS处方油相为辛癸酸甘油酯(MCT),表面活性剂为聚氧乙烯氢化蓖麻油(Cremophor RH40),助表面活性剂为二乙二醇单乙基醚(Transcutol P),油相比例20%,表面活性剂与助表面活性剂的比值K m为2,载药量为10%,平均粒径为28 nm。结论成功制备了honokiol-SMEDDS,显著提高了和厚朴酚的溶解度。

Objective To screen and optimize the formulation of self-microemulsifying drug delivery system （SMEDDS） for honokiol. Methods The formulation of honokiol-SMEDDS was screened by solubility experiment, compatibility test for excipients and pseudo-ternary phase diagrams. And the best formulation was determined by the particle size and in vitro release evaluation. Results In the best formulation of honokiol- SMEDDS, octyl and decyl glycerate （MCT）, polyoxyethylene hydrogenated castor oil （Cremophor RH40） and diethylene glycol monoethyl ether （Transcutol P） were used as oil phase, surfactant and co-surfactant, respec- tively. The percentage of oil phase was 20%, Km of surfactant to cosurfactant was 2, the drug loading was 10%, and the average particle size was 28 nm. Conclusion The honokiol-SMEDDS is prepared successfully, and the solubility of honokiol is improved significantly.