水杨酸天然冰片酯的合成及透皮作用的研究

Synthesis and Transdermal Absorption in Vitro of Bornyl Salicylate

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 bornyl salicylate and study its transdermal absorption in vitro. METHODS Bornyl salicylate was prepared by esterification reaction of （ ＋ ） -borneol and salicylic acid. The penetration of bornyl salicylate through mouse skinin vitro was measured using Franz diffusing cell with 2% azone as the penetration enhancer. The content of bornyl salicylate was determined by ultraviolet spectrophotometry. RESULTS The structure of the target compound was identified by UV, IR and J H-NMR.The transdermal absorption of bornyl salicylate was in accordance with Higuchi equation, in which cumulative dose of skin permeation （Q） has a linear relationship with the time. The average cumulative dose of skin permeation of bornyl salicylate for 12 h was 2. 611 2mg, and the rate constant was 0. 253 9 mg · cm^-2 . h-I CONCLUSION The synthesis method of bomyl salicylate is simple. Bornyl salieylate can penetrate the skin of mice well with 2% azone as the penetration enhancer.