微针对光甘草定搽剂体外透皮吸收的影响

摘要

Objective To study the effect of transdermal absorption of glabridin liniment with the pig skin pretreated by different microneedles in vitro.Methods The experiment was performed by using HPLC and vertical Franz diffusion cell method with abdominal pig skin as transdermal barrier;all the groups of in vitro accumulative permeation dose,transdermal speedand pig skin residue of glabraidin liniment were measured respectively via sampling at 0.5,1.0,2.0,4.0,8.0 and 12.0 h,which would be analyzed by comparing the hollow microneedle group and the solid microneedle group with the control group.Results The calibration curve of glabraidin was y =21.43 x + 3.557 8,r=0.999 9,with a linear range in 1.0-100.0 μg/ml.The pig skin drug retention of the hollow microneedle group and the solid microneedle group increased by 64.42％ and 39.81％ as compared with that of the control group at 0.5 h,respectively.The drug cumulative transmission of the hollow microneedle group and the solid microneedle group were 664.62％ and 159.46％ higher than that of the control group at 2.0 h.The transdermal rates of the hollow microneedle group and the solid microneedle group produced 131.00％ and 66.61％ higher than that of the control group.All of the linear equation of accumulative permeation dose were cohere with the zero-order model.Conclusion Both microneedles are conducive to the transdermal absorption of glabraidin liniment,reducing the hysteresis time of transdermal absorption and providing the basis for its application in percutaneous administration.%目的 研究不同微针作用于猪皮对光甘草定搽剂体外透皮吸收的影响.方法 采用HPLC和改良Franz扩撒池法,分别以实心微针和空心微针作用于离体的腹部猪皮为试验屏障,给药组与对照给药组于0.5、1.0、2.0、4.0、8.0、12.0 h时分别取样测定,计算药物累积透过量、猪皮药物滞留量和透皮速率.结果 光甘草定标准曲线y =21.43x+ 3.557 8,r=0.9999,线性范围1.0～100.0 μg/ml.在0.5 h时空心微针组、实心微针组的猪皮药物滞留量比对照组分别提高了64.42％、39.81％,2.0 h时其药物累积透过量比对照组分别提高了664.62％、159.46％.3组药物累积透过量线性方程均符合零级模型,空心微针组、实心微针组透皮速率比对照组分别提高了131.00％、66.61％.结论 两种微针作用于猪皮均有利于光甘草定搽剂的透皮吸收,减小透皮迟滞时间,为其在皮肤给药方面的应用提供依据.