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

作　　者：王涛[1] 周园[1] 薛薇[1] 刘永谦[2] 王宁生[3] 宓穗卿[3] 

机构地区：[1]广州中医药大学中药学院,广州510006 [2]广东省妇幼保健院,广州510010 [3]广州中医药大学临床药理研究所,广州510405

出　　处：《中国药学杂志》2013年第10期823-826,共4页Chinese Pharmaceutical Journal

基　　金：国家自然科学基金资助项目(30701100)

摘　　要：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.

关 键 词：水杨酸天然冰片酯 合成 透皮吸收 氮酮 

分 类 号：R914.4[医药卫生—药物化学]