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石榴叶鞣质中短叶苏木酚在大鼠体内药代动力学变化

Determination and pharmacokinetic study of brevifolin in rat after ig administration of pomegranate leaf extract

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【作者】 王雪莉邢东明丁怡陈芸芸孟甄杜力军

【Author】 WANG Xue-li,XING Dong-ming,DING Yi,CHEN Yun-yun,MENG Zhen,DU Li-jun (Laboratory of Pharmaceutical Sciences,Dept of Biological Science and Biotechnology,Tsinghua University,Beijing 100084,China)

【机构】 清华大学生物科学与技术系药物药理研究室清华大学生物科学与技术系药物药理研究室 北京100084北京100084北京100084

【摘要】 目的建立测定短叶苏木酚血药浓度的高效液相色谱方法,探讨大鼠ig石榴叶鞣质后体内短叶苏木酚动力学变化。方法色谱条件依利特Hypersil色谱柱;流动相为乙腈-5mmol·L-1磷酸二氢钾溶液(pH25;86∶14,V/V);流速10ml·min-1;紫外检测波长为276nm,以短叶苏木酚峰面积定量。结果短叶苏木酚在176~880μg·L-1内线性良好,回归方程为^Y=393E5X+182E3(n=5),相关系数r2=09994,血浆中最低检测浓度为176μg·L-1。其352,176,880μg·L-13个浓度的回收率>85%,日内日间变异<7%。大鼠ig石榴叶鞣质后短叶苏木酚体内吸收、分布及消除均较快,符合二室开放模型。结论短叶苏木酚可以部分的反映了石榴叶鞣质的药代动力学特征。

【Abstract】 Aim To develop a sensitive, simple and accurate method for quantification of brevifolin, one of the bioactive components of pomegranate leaf extract,in rat plasma following ig administration of extract by reversed phase high performance liquid chromatography.Methods The calibration curve for brevifolin was linear (r2=0.9994) over the concentration range 17.6~880 μg·L~-1 .At this concentration range, the method of overall recoveries (85%~94%) for brevifolin was constructed and the intra-and inter-day assays from rat plasma were less than 7%.Results Following oral administration of pomegranate leaf extract 0.8 g·kg~-1 ,the concentration-time profile was fitted with an open two-compartment system with lag time and the max concentration of brevifolin in plasma of 132 μg·L~-1 at 24.4 min.The pharmacokinetic profile indicates that brevifolin has the similar kinetic characteristics to ellagic acid, including rapid absorption,distribution and elimination.Conclusion This reverse HPLC is suitable for determining brevifolin in plasma.

【关键词】 短叶苏木酚石榴叶HPLC药代动力学
【Key words】 brevifolinpomegranate leaf extractHPLCpharmacokinetics
【基金】 清华大学科技开发项目资助项目(No2002162)
  • 【文献出处】 中国药理学通报 ,Chinese Pharmacological Bulletin , 编辑部邮箱 ,2005年03期
  • 【分类号】R285
  • 【被引频次】18
  • 【下载频次】443
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