目的优化柚皮素自微乳给药系统处方。方法通过测定柚皮素在各辅料中的溶解度,利用伪三元相图初步筛选柚皮素自微乳给药系统组分;以柚皮素在不同自微乳处方中的载药量和粒径为指标,采用Box-Behnken设计-效应面法优化,确定最佳处方。结果柚皮素自微乳最佳处方选择油酸乙酯为油相,聚山梨酯80为乳化剂,PEG 400为助乳化剂,比例为14.02∶44.36∶30,最佳处方中载药量为347.167 mg/g,粒径为38.21 nm。结论应用Box-Behnken效应面法优化柚皮素自微乳给药系统是有效可行的。
Objective To optimize the formula of self-microemulsifying drug delivery system(SMEDDS) for naringenin. Methods The solubility test of naringenin in different secondary solvents and pseudotemary phase diagam was utilized to select components of naringenin SMEDDS. According to the drug loading and particle size of naringenin in different self-microemulsifying drug prescriptions, the optimal prescription was determined using the Box-Behnken design and response surface method. Results The optimal prescription of naringenin SMEDDS was composed of Ethyloleate(oil), Polysorbate 80(surfactant), and PEG 400(co-surfactant), with a weight ratio of 14.02∶44.36∶30. The drug loading of naringenin was 347.167 mg/g, and particle size was 38.21 nm in the optimal prescription. Conclusion It is effective and practical to use Box-Behnken design and response method for optimizing the naringenin SMEDDS.