山茶油对非甾体抗炎药经皮渗透的促进作用

目的考察山茶油对5种非甾体抗炎药体外经皮渗透的促进作用及其与药物油水分配系数的关系。方法采用两室扩散池装置,以离体大鼠腹部皮肤为渗透屏障,用预处理皮肤法考察山茶油的促渗透作用;用HPLC法测定非甾体抗炎药不同时间在接受池药物浓度,计算累积渗透量及其他渗透动力学参数;用摇瓶法测定药物正辛醇介质分配系数以拟合其与山茶油促渗活性关系。结果山茶油可有效促进非甾体抗炎药的经皮渗透率(除双氯芬酸钠外),尤其对氟比洛芬,促渗效果最明显(P<0.01),其增渗倍数达到3.51;山茶油的促渗活性与非甾体抗炎药的正辛醇介质分配系数呈类似抛物线关系。结论山茶油作为一种低毒、无刺激性的渗透促进剂,能够有效提高药物的经皮渗透效果,具有良好的开发应用前景。

Effects of camellia oil on permeation of non-steroidal anti-inflammatory drugs

Objective To examine the enhancing effect of camellia oil on the skin permeation of non-steroidal anti-inflammatory drugs.Methods The percutaneous penetration experiment was performed on a 2-chamber diffusion cell in vitro with the application of camellia oil to the skin as a penetration enhancer.The rat abdomen skin was used as barrier.The samples from the receptor solution were assayed by HPLC.The partition coefficients of drugs between n-octanol and vehicle were measured to get the relationship between the enhancing effect of camellia oil and partition coefficients.Results Camellia oil could effectively enhance the permeation of drugs through the excited rat skin especially for flurbiprofen(P<0.01) with the R_e value(3.51.)The relationship between the enhancing effects and the partition coefficients of drugs between n-octanol and vehicle were like parabolic curve.Conclusions Camellia oil may be developed as an effective penetration enhancer with low toxin and without irritation which is worthy of exploitation.