促透剂对积雪草苷体外经皮渗透的影响

Effects of penetration enhancers upon percutaneous permeability of asiaticoside solution in vitro

目的：研究促透剂对积雪草苷经皮渗透的影响。方法用离体鼠皮研究积雪草苷溶液以及含5%氮酮、薄荷脑、冰片等3种促透剂的积雪草总苷溶液的体外经皮渗透性，计算累积渗透量和渗透速率，采用HPLC法测定接收液中积雪草苷浓度。结果积雪草苷在20μg/ml^100μg/ml范围内标准曲线为：A=3479.7C＋571.93，r=0.9996，表明线性关系良好。日内精密度RSD为1.4％，1.5%，1.0%，日间精密度RSD为1.6％，1.3%，1.1%，稳定性实验的平均RSD为1.4%，低、中、高3个浓度的加样回收率分别为94.8%，101.1%，99.6%。随着积雪草苷溶液浓度增加，其透过量逐渐增加，几种促透剂对积雪草苷均有促透作用。结论HPLC可以准确地检测体外透皮接收液中积雪草苷的浓度，方法简便、快速；3种促透剂能促进积雪草苷的经皮透过量，5%薄荷脑和冰片促透效果好。

Objective To explore the effects of penetration enhancers upon the percutaneous permeability of asiaticoside solution. Methods Asiaticoside solution ,added with different pentration enhancer（5%azong, menthol,and borneol）,were added to a piece of rat skin.High Performance Liquid Chromatography（HPLC） was used, and the following chromatographic conditions were set：BDS HYPERSIL C18 column （250 mm ＆#215; 4.6 mm, 5μm）; mobile phase： acetonitrile- water （25：75）; column temperature： 35; flow rate： 1mL＆#183;min-1; detection wavelength： 207nm; injection volume： 10μl. The asiaticoside in the solution of receiver was determined. The percentage drug percutaneous release at different time intervals and the permeate rate was calculated. Results The standard curve of asiaticoside was linear within the range from 20μg/ml to 100μg/ml, r=0.9996. The RSD of intra-day precision were 1.4%, 1.5%and 1.0%;and the RSD of inter-day precision were 1.6%, 1.3%and 1.1%. The RSD of asiaticoside stability was 1.4%. The average recoveries were 94.8%, 101.1%and 99.6%respectively. The quantity of penetration across skin reflected higher with the concentration increasing of asiaticoside. There was a large difference found when using different penetration enhancers. Conclusion HPLC method carrys the features of being simple, fast, and accurate in detecting the asiaticoside in the solution of receiver. 5%menthol and 5%borneol demonstrate the stronger effects to the percutaneous permeation rate of asiaticoside.