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熊果酸在大鼠体内的药代动力学研究
引用本文:温金华,;徐良全,;盛向远,;左荣,;魏筱华,;裘雅玲,;李艳明.熊果酸在大鼠体内的药代动力学研究[J].矿产勘查,2014(12):13-15.
作者姓名:温金华  ;徐良全  ;盛向远  ;左荣  ;魏筱华  ;裘雅玲  ;李艳明
作者单位:[1]南昌大学第一附属医院药学部,南昌330006; [2]南昌大学基础医学部,南昌330006; [3]南昌大学第一附属医院GCP中心,南昌330006
基金项目:国家自然科学基金(青年)资助项目(81202583)
摘    要:目的探讨熊果酸分别口服、静脉注射及合用环孢素后,其药代动力学变化。方法将15只SD雄性大鼠按随机数字表法分为3组,每组5只。口服给药组予80 mg·kg^-1的熊果酸灌胃;合用环孢素组先予10 mg·kg^-1环孢素灌胃,15 min后再灌服80 mg·kg^-1的熊果酸;尾静脉给药组予熊果酸原料药(80 mg·kg^-1,先用少量的DMSO溶一下,再用生理盐水稀释)尾部静脉注射。采用HPLC方法测定血药浓度,DAS软件分析药代动力学参数。结果与口服给药组相比较,合用环孢素组及静脉给药组其各药代动力学参数AUC(0-t)、AUC(0-∞)及Cmax均显著增大(P〈0.05)。结论口服给药后熊果酸在大鼠体内的生物利用度较低;环孢素可增加熊果酸的口服生物利用度。

关 键 词:熊果酸  药代动力学  生物利用度  大鼠  动物  实验

Pharmacokinetics of Ursolic Acid in Rats
Affiliation:WEN Jin-hua, XU Liang-quan , SHENG Xiang-yuan , ZUO Rong, WEI Xiao-hua,QIU Ya-ling ,LI Yan-ming (a. Department of Pharmacy, the First Affiliated Hospital ; b. Deparment of Basic Medicine ; c. GCP Center, the First Affiliated Hospital, Nanchang University, Nanchang 330006, China)
Abstract:Objective To explore the changes in pharmacokinetics of ursolic acid after oral administration,intravenous injection or combined treatment with cyclosporine. Methods Fifteen male SD rats were randomly divided into three groups,with 5 rats in each group. The oral administration group was intragastrically given ursolic acid 80 mg·kg^-1. The intravenous administration group was injected with ursolic acid 80 mg·kg^-1via tail vein( ursolic acid was dissolved in DMSO and then diluted in normal saline). The combined treatment group was intragastrically given ursolic acid 80 mg·kg^-115 minutes after treatment with cyclosporine 10 mg · kg^-1. Blood concentrations of ursolic acid were determined by HPLC,and pharmacokinetic parameters were analyzed using DAS software. Results Compared with oral administration group,pharmacokinetics parameters AUC( 0- t),AUC( 0- ∞)and Cmaxincreased significantly in both intravenous administration group and combined treatment group. Conclusion The bioavailability of ursolic acid is low after oral administration in rats. Cyclosporine can increase the oral bioavailability of ursolic acid.
Keywords:ursolic acid  pharmacokinetics  bioavailability  animals  laboratory  rats
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