温通膏方微针贴剂的体外释放与透皮性能研究

Research on the in vitro Release and Transdermal Properties of Wentong Gao Microneedle Patch

目的考察温通膏方微针贴剂的体外释放和透皮特性。方法采用高效液相色谱法测定温通膏方中补骨脂素和异补骨脂素的含量。(1)体外释放试验:采用药物透皮扩散池,配制不同浓度(10%、20%、30%、40%)的乙醇-生理盐水溶液作为接收液,分别在1、2、4、8、12、24 h等6个时间点取样分析;绘制累积释放率(Q/%)-时间(t/h)曲线,根据释放规律选择Higuchi方程模型和一级动力学模型进行拟合分析。(2)体外透皮实验:制备离体大鼠皮肤,以20%乙醇-生理盐水作为接收液,分别在1、2、4、8、12、24 h等6个时间点取样分析;绘制累积透过率(Q/%)-时间(t/h)曲线,选择零级动力学模型、一级动力学模型和Higuchi方程模型对曲线进行拟合分析。结果选择20%乙醇-生理盐水为最佳接收介质,温通膏方微针贴剂中补骨脂素、异补骨脂素的24 h累积释放率分别为34.980%、30.623%;温通膏方微针贴剂中补骨脂素、异补骨脂素的24 h累积透过率均优于温通膏凝胶剂,分别为8.546%、6.949%。结论将温通膏方开发成微针贴剂,能有效降低皮肤屏障作用,增强药物吸收,有助于提高临床疗效。

Objective The in vitro release and transdermal properties of Wentong Gao microneedle patch were investigated.MethodsThe contents of psoralen and isopsoralen were determined by HPLC.(1)In vitro release test:,(,20%,30%,40%)were prepared as the receiving solution and respectively sampled at 6 time points including 1,2,4,8,12,and 24 h;the cumulative release rate(%)-time(h)curve was drawn,and Higuchi equation modeland first-order dynamic model were selected for fitting according to the release rule.(2) In vitro transdermalexperiment: in vitro rat skin was prepared, and 20% ethanol-physiological saline solution was selected as thereceiving solution and sampled at 6 time points including 1,2,4,8,12 and 24 h. The cumulative transmittance(%)-time(h) curve was drawn, and the zero-order dynamic model, first-order dynamic model and Higuchiequation model were selected for fitting analysis of the curve.Results20% ethanol saline was chosen as the bestreceiving medium. The 24 h cumulative release rates of psoralen and isopsoralen in Wentong Gao microneedle patchrespectively were 34.980% and 30.623%. The 24 h cumulative transmission rates of psoralen and isopsoralen inWentong Gao microneedle patch were better than those in Wentong Gao normal gel, which were 8.546% and 6.949%,respectively.ConclusionThe development of the Wentong Gao microneedle patch can effectively reducethe skin barrier effect,increase drug absorption,and improve clinical efficacy.