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目的合成水杨酸天然冰片酯并研究其透皮吸收。方法酸性条件下,酯化反应制备水杨酸天然冰片酯;以2%氮酮为促透剂,采用Franz扩散池进行离体小鼠皮肤的体外渗透性实验,紫外分光光度法检测累积透过量。结果水杨酸天然冰片酯结构通过UV、IR、1H-NMR等图谱的综合解释加以确证;其透皮吸收符合Higuchi方程,累积透过量(Q)与t成线性关系。12h平均累积透过量为2.611 2 mg;12 h平均透皮速率常数为0.253 9 mg.cm-2.h-1。结论水杨酸天然冰片酯合成方法操作简便;2%氮酮对水杨酸天然冰片酯有良好的促透作用。
Objective To synthesize natural salicylic acid ester and study its transdermal absorption. Methods The natural borneol ester of salicylic acid was prepared by esterification reaction under acid condition. In vitro permeation experiment of ex vivo mouse skin was performed by using Franz diffusion cell with 2% Azone as penetration enhancer, and the cumulative permeation rate was measured by ultraviolet spectrophotometry . Results The structure of the natural borneol ester of salicylic acid was confirmed by the comprehensive interpretation of UV, IR and 1H-NMR spectra. The transdermal absorption conformed to the Higuchi equation and the cumulative permeation (Q) was linear with t. 12h average cumulative penetration of 2.611 2 mg; 12 h average transdermal rate constant of 0.253 9 mg.cm-2.h-1. Conclusions The method of synthesizing natural borneol ester of salicylic acid is simple and easy to operate. 2% Azone has a good permeation enhancing effect on natural borneol ester of salicylic acid.