不同促渗剂对香附四物汤外用贴剂中效应成分体内药动学的影响  

Effects of different penetration enhancers on pharmacokinetics of active components in Xiangfu Siwu transdermal patches

作　　者：潘瑛[1,2] 李振皓[1,2] 钱大玮[1,2] 刘培[1,2] 张洋[1,2] 尚尔鑫[1,2] 张丽[1,2] 段金廒[1,2] 

机构地区：[1]南京中医药大学中药资源产业化与方剂创新药物国家地方联合工程研究中心,江苏南京210023 [2]南京中医药大学江苏省方剂高技术研究重点实验室,江苏南京210023

出　　处：《中国中药杂志》2016年第2期294-302,共9页China Journal of Chinese Materia Medica

基　　金：国家自然科学基金项目(81202880);江苏省自然科学基金项目(BK2012456);江苏高校优势学科建设工程项目(ysxk-2014);江苏省高校自然科学重大基础研究项目(12KJA360002)

摘　　要：考察不同种类和不同浓度促渗剂作用下,香附四物汤效应部位(XBW)贴剂中6种有效成分的体内药动学特性并优选适宜促渗剂。采集大鼠不同促渗剂组经皮给药后不同时间点的血浆样本,UPLC-MS/MS测定血浆中6种成分的浓度,DAS软件计算主要药动学参数,应用主成分分析求得各组不同时间点6种成分血药浓度的总因子得分F,以F代替血药浓度对t做曲线,以该曲线的曲线下面积为指标判断不同促渗剂的促渗效果。与对照组相比,其余各组的曲线下面积均明显增加,说明促渗剂效果显著,其中以5%薄荷醇促渗效果最为明显。5%薄荷醇能显著促进XBW中6种主要有效成分在大鼠体内的吸收,为香附四物汤开发为经皮给药制剂的研究提供了一定科学依据和参考。To study the effect of different penetration enhancers on the pharmacokinetic characters of six active components in Xiangfu Siwu transdermal patch（ XBW） and optimize the best penetration enhancers. During the experiment,the patches containing different penetration enhancers were stuck on the rat＇s skin,and then the blood samples were acquired at different time points. Six active components in plasma were determined by UPLC-MS / MS. The main pharmacokinetic parameters were calculated with DAS software package. The total factor scores（ F） of the plasma concentrations of six components at every time point in different groups were calculated using principle component analysis,and the areas under F versus time curves（ AUCF-t） were employed to be the indexes for selecting penetration enhancers. The results demonstrated that compared with the control group,the AUCF-tfrom other groups increased prominently and furthermore,5% menthol manifested the best effect. In this research,5% menthol could remarkably promote the percutaneous penetration effect of the six active compounds in XBW,and it could provide a scientific basis for the preparation research of XBW.

关 键 词：经皮渗透 主成分分析 多组分 促渗剂 香附四物汤效应部位 药动学 UPLC-MS/MS 

分 类 号：R285.5[医药卫生—中药学]