透皮促进剂对两种锌盐经皮渗透性的影响

以水难溶性锌盐(共轭亚油酸锌)及水溶性锌盐(葡萄糖酸锌)为目标药物,考察氮酮、油酸、二甲亚砜、尿素、谷氨酸钠5种常用透皮促进剂对形成凝胶剂、油溶性膏剂经皮渗透性的影响。制备两种锌盐的凝胶剂和乳膏剂,采用Franz扩散池和离体小鼠皮进行体外透皮吸收试验,测定一定浓度透皮促进剂下,10 h锌盐的单位面积累积透过量(Q)。结果 3%二甲亚砜对共轭亚油酸锌凝胶剂增渗比EF最大,为2.68;2%谷氨酸钠对葡萄糖酸锌凝胶剂EF最大,为2.19;而3%二甲亚砜对形成膏剂的两种锌盐促透效果最好,共轭亚油酸锌膏剂EF为2.65,葡萄糖酸锌膏剂EF为2.87。说明在水润湿的凝胶剂中,二甲亚砜为水难溶性锌盐的最佳促进剂,谷氨酸钠是水溶性锌盐的最佳促进剂;二甲亚砜为膏剂中锌盐经皮渗透性较佳的透皮促进剂。

Effects of Different Penetration Enhancers on Transdermal Permeability of Two Kinds of Zinc Salt

Abstract] Objective: To study the effects of 5 kinds of penetration enhancers-azone, oleic acid, dimethyl sulfoxide (DMSO), urea, and sodium glutamate at different mass fraction on the permeability of two kinds of zinc salts across male mice skin in different preparations. Methods: Gels and w/o creams of two kinds of zinc salt was prepared by penetration enhancers. Using modified Franz diffusion cell and male mice skin as model, the concentration of zinc salt was determined and accumulative permeation quantity were fitted. Results: It was found zinc conjugated linoleates gels with 3% dimethyl sulfoxide showed the optimal permeation with 2.68-fold enhancement, zinc gluconate with 2% sodium glutamate showed the optimal permeation with 2.19-fold enhancement, while w/o creams of two kinds of zinc salts with 3% dimethyl sulfoxide showed the optimal permeation. Conclusion: In wetting gels, the best permeation enhancer for water insoluble zinc salt was DMSO, while the best one for water-soluble zinc salt was sodium glutamate. In the w/o creams, DMSO was the optimal transdermal enhancer for better percutaneous permeability of zinc salt.