绞股蓝总皂苷自微乳化给药系统的制备

Preparation of gypenoside self- microemulsifying drug delivery system

目的绞股蓝总皂苷自微乳化给药系统的制备及评价。方法通过溶解度试验、伪三元相图及星点设计-效应面法,以粒径、Zeta电位、自微乳化时间为指标,筛选最佳处方,并对绞股蓝总皂苷自微乳化给药系统体外释药进行测定。结果绞股蓝总皂苷自微乳的最优处方为:吐温-80 52%,甘油30%,油酸乙酯26%;其平均粒径为51.21 nm,Zeta电位为-13.7 m V,乳化时间为31.54 s,在45 min的体外溶出度是原料药的5倍。结论绞股蓝总皂苷自微乳化给药系统制备工艺可行,能显著提高绞股蓝总皂苷的溶出度。

Objective To prepare gypenoside self- microemulsifying drug delivery system( SMEDDS) and evaluate its quality. Methods The optimized formulation of gypenoside SMEDDS was screened by solubility,ternary phase diagrams and central composite design- response surface method with the particle size,the Zeta potential and the time of self- emulsification as parameters. The physic- chemical property and dissolution characters of gypenoside SMEDDS were also determined. Results The optimized formulation was composed of tween- 80( 52%),glycerol( 30%),ethyl oleate( 26%). The average particle size after the emulsification was 51. 21 nm,the Zeta potential- 13. 7 m V,the time of self- emulsification was 30. 54 s. The percent of accumulated dissolution of gypenoside in SMEDDS in vitro was 5 times of crude material at 45 min. Conclusion The preparation method of gypenoside SMEDDS was feasible,which can significantly increase the dissolution of gypenoside.