| 引用本文: | 张雅雯,尹丽娜,梁泽华,吴斌丽,朱亮,黄夏樱,王胜浩.积雪草酸大鼠体内药动学考察[J].中国现代应用药学,2015,32(3):314-317. |
| ZHANG Yawen,YIN Lina,LIANG Zehua,WU Binli,ZHU Liang,HUANG Xiaying,WANG Shenghao.Study on Pharmacokinetics of Asiatic Acid in Rats[J].Chin J Mod Appl Pharm(中国现代应用药学),2015,32(3):314-317. |
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| 摘要: |
| 目的 建立大鼠血浆中积雪草酸(asiatic acid，AA)的柱前衍生化HPLC，探讨AA在大鼠体内的药动学。方法 SD大鼠，♂，尾静脉注射AA(10 mg?kg-1)，于给药后不同时间采取血浆，经DIKMA Proelut PLS柱固相萃取，柱前衍生化HPLC测定血浆中AA浓度(以甘草次酸为内标)，药物统计软件(PKS 1.0)拟合统计药动学参数。结果 血药浓度在0.1~20 μg?mL-1内线性良好(r=0.999 6)，平均提取回收率为71.1~79.9%，日内、日间精密度RSD均<13%，样品在?20 ℃放置，经2次冻融循环后基本稳定。AA在大鼠体内药-时曲线符合一室开放模型，主要药动学参数为：tmax=2.0 min，Cmax=14.7 μg?mL-1，t1/2=35.1 min，AUC0-t=217.0 μg?min?mL-1，AUC0-∞=234.3 μg?min?mL-1。结论 AA在大鼠体内消除迅速，所建立的提取及柱前衍生化HPLC适用于体内AA的测定。 |
| 关键词: 积雪草酸 血药浓度 固相萃取 一室模型 |
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| 基金项目:浙江省科技厅项目(2011F10048)；浙江省新世纪151人才工程(第二层次)；浙江省卫生高层次创新人才培养工程项目(2008)；浙江省医学重点学科群建设资助项目(XKQ-010-001) |
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| Study on Pharmacokinetics of Asiatic Acid in Rats |
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ZHANG Yawen1, YIN Lina1, LIANG Zehua2, WU Binli1,2, ZHU Liang1,2, HUANG Xiaying1, WANG Shenghao1
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1.Zhejiang Academy of Medical Sciences, Hangzhou 310013, China;2.Department of Pharmacy, Zhejiang University of Traditional Chinese Medicine, Hangzhou 310053, China
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| Abstract: |
| OBJECTIVE To establish a sensitive precolumn derivatization HPLC method for determination of plasma concentration of asiatic acid(AA) and evaluate its pharmacokinetics characteristics in rats. METHODS The male SD rats were intravenously administrated AA by 10 mg?kg-1. The plasma samples were taken at different times, concentrated by SPE method and determined by precolumn derivatization RP-HPLC method, the glycyrrhetinic acid was used as an internal standard. The pharmaeokinetie parameters were accessed by PKS 1.0. RESULTS Excellent liner relationship was obtained in the range of 0.1 to 20 μg?mL-1(r=0.999 6). The averang extraction recovery was 71.1%?79.9%. The intra- and inter-day RSDs were less than 13%. The samples were stabled at -20 ℃, and remained stable after twice freeze-thaw cycles. AA was fitted to a one compartment open model in rats, mainly pharmacokinetic parameters as follow: tmax=2.0 min, Cmax=14.7 μg?mL-1, t1/2=35.1 min, AUC0-t=217.0 μg?min?mL-1, AUC0-∞=234.3 μg?min?mL-1. CONCLUSION AA is disposed extensively and rapidly in rats. The method can be used to determine the concentration and to investigate the pharmacokinetics of AA in rats. |
| Key words: asiatic acid plasma concentration solid phase extraction one compartment model |
