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木犀草素在大鼠体内的药动学研究

Study on pharmacokinetics of luteolin in rats

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【作者】 陈秀杰刘磊朱文良刘永胜黄邦清屈东香毕开顺

【Author】 CHEN Xiu-jie1,2,LIU Lei2,ZHU Wen-liang2,LIU Yong-sheng2,HUANG Bang-qing2,QU Dong-xiang2,BI Kai -shun1 (1.Shenyang Pharmaceutical University,Shenyang 110016,China;2.Laboratory of Pharmacokinetic and Pharmacogenomics,Harbin Medical University,Harbin 150081,China)

【机构】 沈阳药科大学药学院哈尔滨医科大学药代动力学与药物基因组信息学教研室

【摘要】 目的:建立木犀草素血药浓度的高效液相色谱测定方法,并探讨其在大鼠体内的药动学行为。方法:采用Agilent TC-C18(4.6mm×150mm,5μm)色谱柱,以乙腈-0.5mol·L-1磷酸二氢钾溶液(40∶60)为流动相,流速1.0mL.min-1,检测波长280nm。大鼠灌胃木犀草素30mg·kg-1后,于不同时间点断尾采血,用HPLC法测定其血药浓度,经3P97药动学计算程序处理,得到药动学参数。结果:大鼠血浆中,木犀草素的线性范围为20~1200ng·mL-1(r=0.9967),方法回收率大于96%,最低检测限为15ng·mL-1。大鼠灌胃木犀草素后,木犀草素的血药浓度-时间变化曲线符合二室模型,Tmax为(0.732±0.13)h,Cmax为(0.691±0.14)mg·mL-1,AUC为(0.435±0.12)mg·h·mL-1。结论:本试验建立的大鼠血浆中木犀草素含量的HPLC测定方法,专属性强,灵敏度高,可用于该药在大鼠体内的药代动力学研究。

【Abstract】 Objective:To establish an HPLC method for the determination of luteolin in rat plasma and to study the pharmacokinetics of luteolin in rats.Methods:An Agilent TC-C 18(4.6 mm×150 mm,5 μm) column was adopted,the mobile phase was a mixture of acetonitrile and 0.5 mol·L-1 potassium dihydrogen phosphate solution(40∶60) at the flow rate of 1.0 mL·min-1 and the UV detector was operated at 280 nm.After oral administration of luteolin(30 mg·kg-1),the luteolin concentration in rat plasma was detected by HPLC.The pharmacokinetic parameters were calculated by 3P97 program.Results:In rat plasma,a good linearity between peak area ratio of diosmetin to the internal standard and the concentration was found in the range of 20-1200 ng·mL-1(r=0.9967);the method recoveries were over 96%.The limit of test was 15 ng·mL-1.The plasma luteolin concentration-time curve could be evaluated by the two compartment model. T max,C max and AUC were (0.732±0.13) h,(0.691±0.14) mg·mL-1 and (0.435±0.12) mg·h·mL-1,respectively.Conclusion:The developed HPLC method for the pharmacokinetic study of luteolin in rat after oral administration is precise and specific.

【关键词】 木犀草素药动学高效液相色谱
【Key words】 luteolinpharmacokineticsHPLC
【基金】 黑龙江省科技厅攻关课题(GC07C337)
  • 【文献出处】 药物分析杂志 ,Chinese Journal of Pharmaceutical Analysis , 编辑部邮箱 ,2009年09期
  • 【分类号】R285
  • 【被引频次】7
  • 【下载频次】621
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