五妙水仙膏凝胶剂基质处方优选及体外透皮性能考察

Formulation Optimization of Matrix and Investigation of in Vitro Transdermal Properties of Wumiao Shuixian Cream Gel

目的:优选五妙水仙膏凝胶剂的基质处方并研究其体外透皮性能。方法:以凝胶剂基质在室温下的黏度和屈服值、在体表温度下的黏度和屈服值、触变性的综合评分为指标,通过正交试验优化处方中丙二醇、卡波姆、三乙醇胺和甘油的用量。采用改良的Franz扩散池,运用HPLC测定处方中没食子酸、盐酸小檗碱和β,β-二甲基丙烯酰阿卡宁的含量,以有效成分的24 h内单位面积累积透过量为指标,考察促渗剂冰片、薄荷脑、氮酮对该凝胶体外透皮性能的影响。结果:五妙水仙膏凝胶剂基质处方最佳配比为丙二醇15 g,卡波姆-940 4 g,三乙醇胺3 g,甘油20 g和薄荷脑6 g。结论:按优选处方制备的五妙水仙膏凝胶剂外观均匀细腻、黏度适中、涂展性好,呈现出良好的体外透皮性能。

Objective： To optimize the matrix formulation of Wumiao Shuixian cream gel and investigate its in vitro transdermal properties. Method： Taking composite score of viscosity and yield value at room temperature,viscosity and yield value at average temperature of skin and thixlotropy of gel matrix as index,orthogonal test was employed to optimize the formulation with amounts of propylene glycol, carbopol,triethanolamine and glycerol as factors. Modified Franz diffusion cell was adopted, HPLC was employed to simultaneous determine contents of gallic acid,berberine hydrochloride and β,β-dimethylacry lalkannin,effects of penetration enhancers on in vitro transdermal properties were investigated with the cumulative permeation amount of three active ingredients in 24 h as index. Result： Optimum formulation of gel matrix was made from 15 g of propylene glycol,4 g of carbopol-940,3 g of triethanolamine,20 g of glycerol and 6 g of menthol. Conclusion：The prepared Wumiao Shuixian cream gel has uniform and fine appearance, moderate viscosity and good spreadability with a favorable in vitro transdermal properties.