冰片对川芎嗪经皮给药大鼠体内药物动力学的影响  

Effect of Borneol on Pharmacokinetics of Transdermal TMP Delivery in Rats

作　　者：王志东[1] 王晖[1] 赵继会[1] 冯年平[1] 

机构地区：[1]上海中医药大学药剂教研室,上海201203

出　　处：《上海中医药大学学报》2014年第3期90-93,共4页Academic Journal of Shanghai University of Traditional Chinese Medicine

基　　金：上海市教委重点学科建设项目(J50302)

摘　　要：目的:考察冰片对川芎嗪经皮给药在大鼠体内药物动力学的影响。方法:制备基于微乳(microemulsion,ME)的川芎嗪-冰片复方经皮给药系统(TMP-Borneol-ME-TDDS)和川芎嗪单方经皮给药系统(TMP-ME-TDDS);将10只SD大鼠随机分为川芎嗪-冰片复方组和川芎嗪单方组,于不同时间采集血样,HPLC法测定川芎嗪的血药浓度;采用SPSS 18.0统计软件和DAS 2.0药动学处理软件对药物动力学结果进行分析。结果:TMP-Borneol-ME-TDDS组川芎嗪的血浆药物浓度-时间曲线下面积(AUC)大于TMP-METDDS组,TMP-Borneol-ME-TDDS组中川芎嗪的表观分布容积(V)小于TMP-ME-TDDS组,差异均具有统计学意义(P<0.05);TMP-Borneol-ME-TDDS的相对生物利用度为131.94%。结论:冰片可提高川芎嗪经皮给药的相对生物利用度,并有可能对其组织分布行为产生影响。Objective： To investigate the possible influence of borneol on the pharmacokinetic of transdermal tetramethylpyrazine （TMP） delivery in rats. Methods： The microenmlsion-based transdermal drug delivery system incorporating TMP and borneol （TMP-Borneol-ME-TDDS） and TMP-loaded transdermal drug delivery system （TMP-ME- TDDS） were prepared. Ten SD rats were randomly divided into TMP-Borneol group and TMP group. The plasma was obtained at different time points and the concentration of TMP was determined by HPLC method. Results： AUC（O-36h） of TMP in TMP-Borneol group was higher than that of the TMP group ; the apparent volume of distribution in TMP-Borneol group was less than that of the TMP group, with significant difference between the two groups （ P 〈 0.05 ）. The relative bioavailability of TMP-Borneol-ME-TDDS was 131.94 %. Conclusion： The transdermal bioavailability of TMP was enhanced with the addition of borneol. The biodistribution of TMP might be influenced by borneol.

关 键 词：川芎嗪 冰片 微乳 经皮给药 药物动力学 大鼠 

分 类 号：R285.5[医药卫生—中药学]