麝香壮骨膏中不同极性药物的体外释放与透皮对比

Comparative Analysis of in vitro Release and Percutaneous Penetration of Different Polar Drugs in Shexiang Zhuanggu Plasters

目的:考察麝香壮骨膏中盐酸苯海拉明、水杨酸甲酯的体外释放和透皮规律。方法:采用垂直式Franz扩散池进行体外释放和透皮试验,HPLC法测定释放液和透皮接受液中盐酸苯海拉明、水杨酸甲酯含量,计算单位面积累积释放率和累积透过率。结果:麝香壮骨膏中盐酸苯海拉明、水杨酸甲酯24h单位面积累积释放率均值分别为19.75%,73.50%,释放过程均符合Higuchi模型;单位面积累积透过率分别为12.48%,45.62%,透皮过程均符合零级模型;麝香壮骨膏样品中水杨酸甲酯单位面积平均累积释放率、累积透过率显著高于盐酸苯海拉明(P<0.05)。结论:麝香壮骨膏中,脂溶性药物较水溶性药物具有更高的体外释放和经皮渗透性能。

Objective:To study the in vitro release and percutaneous permeation of diphenhydramine hydrochloride and methyl salicylate in Shexiang Zhuanggu plasters.Methods:In vitro release and transdermal permeation were performed by means of vertical Franz diffusion cells.The contents of diphenhydramine hydrochloride and methyl salicylate in release fluid and transdermal receptor fluid were determined by HPLC.The cumulative release rate per unit area and the cumulative percentage of drug penetrating the skin were calculated.Results:The 24-hour average cumulative release percentages of diphenhydramine hydrochloride and methyl salicylate in Shexiang Zhuanggu plasters were 19.75%and 73.50%,and the in vitro release process of the two drugs conformed to Higuchi models;the cumulative transmission rates of the two drugs through the skin per unit area were 12.48%and 45.62%,and the in vitro transdermal process of the two drugs conformed to zero order models.Within 24 h,the average cumulative release rate and cumulative transmittance per unit area of methyl salicylate in Shexiang Zhuanggu plasters were significantly higher than those of diphenhydramine hydrochloride(P<0.05).Conclusion:In Shexiang Zhuanggu plasters,drugs with higher liposolubility have greater in vitro release and percutaneous permeation than water-soluble drugs.