葛根素自微乳给药系统的制备及其质量评价

Preparation and evaluation of puerarin self-microemulsifying drug delivery system

目的研究葛根素自微乳给药系统的处方工艺。方法通过溶解度试验、油和表面活性剂配伍试验,以及伪三元相图的绘制,筛选葛根素自微乳的处方组成;通过粒径、载药量和自微乳化时间优化了葛根素自微乳处方;并对葛根素自微乳的理化性质和稳定性进行了考察。结果葛根素自微乳处方中油相为中链甘油三酯(19.0%)、油酸(19.0%),表面活性剂为聚山梨酯80(19.0%)、聚氧乙烯蓖麻油(19.0%),助表面活性剂为1,2-丙二醇(19.0%),葛根素(5.0%)。自微乳化后粒径为(17.28±0.24)nm,自微乳化时间小于120 s;室温留样6个月,该自微乳性状、质量分数、粒径和自微乳化时间均无明显变化。结论所制备的葛根素自微乳粒径小、稳定性好,符合良好自微乳制剂的要求。

Objective To study the formulation ofpuerarin （PUE） self-microemulsifying drug delivery system （SMEDDS）. Methods The optimum formulation ofPUE SMEDDS was screened by test of solubility, compatibility of oil and surfactant, and pseudo-ternary phase diagram, and the prescription of PUE SMEDDS was optimized by particle size, self-microemulsifying time, and drug loading; The physicochemical characteristics and stability were also determined. Results The optimum SMEDDS composed of Miglyol 812N （19.0%）, oleic acid （19.0%）, polysorbate 80 （19.0%）, EL-35 （19.0%）, 1, 2-propanediol （19.0%）, and puerarin （5.0%）. The particle size was （17.28± 0.24） nm, and self-microemulsifying time was less than 120 s; The appearance, content of PUE, particle size, and sell： microemulsifying time had no obvious changes under room temperature storage for six months. Conclusion The acquired PUE SMEDDS is stable with small particle size, which meets the needs of good SMEDDS formulation.