双氯芬酸钠在不同凝胶基质中透皮扩散特征的研究

Study on the dermal penetration of diclofenac sodium from several gel systems

目的：研究双氯芬酸钠在凝胶贮库中的扩散特征及其对双氯芬酸钠透皮扩散速率的影响。方法：以改良的 Ｆｒａｎｚ 扩散池为实验装置，回归分析双氯芬酸钠在二种凝胶基质、共十二种条件下经微孔滤膜或透过离体小鼠皮的累积透过量。结果：在亲水的高分子凝胶基质中，离子形式的双氯芬酸钠扩散速率大于分子形成的扩散速率。经皮扩散时，分子形式的双氯芬酸钠在海藻酸凝胶中的扩散速率大于离子形式的扩散速率；在卡波普凝胶中结果则相反。双氯芬酸钠从含有月桂氮苷卓酮的凝胶中透皮扩散的速率比从相应没有月桂氮苷卓酮的凝胶中透皮扩散的速率有所增加，但增加的程度不明显。特别是当卡波凝胶中是离子形式的双氯芬酸钠时，其有无促透剂的２４ ｈ 累积透过量之比值只为１ ．１７ 。

OBJECTIVE:To study the diffusive properties of diclofenac sodium in gel systems and the effect on diffusive rate of diclofenac sodium through the skin of mice.METHODS:Regression method was used to analyze cumulative amounts of diclofenac sodium penetrated from carbopol and calcium alginate gel in acidic and basic conditions.RESULTS:The diffusive rate of diclofenac sodium from the two kinds of hydrophilic polymer gel was higher than that of diclofenac acid.The penetrative rate of diclofenac acid was greater than that of diclofenac sodium in calcium alginate gel.The penetrative rate of diclofenac acid was smaller than that of diclofenac sodium in carbopol.The penetrative rate of diclofenac through the skin of mice was enhanced inconsiderably by azone in the vehicle.Especially for that of diclofenac sodium as ion pair form in carbopol gel,the enhancement ratio was only 1.17 .