【摘要】 目的:研究不同剂量染料木黄酮及其葡萄糖醛酸化代谢产物在大鼠尿中的排泄动力学。方法:将染料木黄酮制成混悬液,按6.25、12.5、50mg.kg-1给大鼠灌胃,于灌胃后不同时间收集尿液,用葡萄糖醛酸酶溶液处理尿液。采用高效液相色谱法测定尿液中染料木黄酮及其葡萄糖醛酸化代谢产物的浓度。结果:6.25、12.5、50 mg.kg-1时,累积以原形经尿液排泄的药物分别为34.79±10.83、187.30±69.96和213.56±30.58μg,累积经尿液排泄的总药物(原形药物+葡萄糖醛酸化药物)分别为217.79±52.06、583.05±106.92和1108.37±88.14μg,累积经尿液排泄的葡萄糖醛酸化代谢产物分别占尿液排泄总量的84.03%、67.88%和80.73%。结论:染料木黄酮在大鼠尿液中主要以葡萄糖醛酸结合形式排泄,原形及其葡萄糖醛酸化代谢产物的排泄呈现明显的非线性剂量依赖性特征。更多还原

【Abstract】 AIM: To study the urinary excretion of genistein at different doses in rats.METHODS: Suspended in（0.5）% CMC-Na solution,genistein was orally administered to rats at the dose of（6.25）,（12.5） and 50(mg·kg^-1),respectively.At various time intervals,the urine was collected.The urine was treated with β-glucuronidase.The genistein in urine was extracted twice by vortexing with（2.0） ml mixture of methyl tert-tubtyl ether and pentane（v/v=82）.The organic phase was removed into the tubes and then evaporated in ventilation cabinet.The residue was dissolved in 50 μl of methanol.The solution of 20 μl was drawn and detected by high-performance liquid chromatography.RESULTS: The accumulative urine excretion of genistein was（34.79）±（10.83）,（187.30）±（69.96） and（213.56）±（30.58） μg at the dose of（6.25）,（12.5） and 50(mg·kg^-1),respectively.The total drug（genistein+glucuronidated genistein） excreted from urine was（217.79）±（52.06）,（583.05）±（106.92） and（1108.37）±（88.14） μg,and the ratio of glucuronidated genistein was（84.03）%,（67.88）% and（80.73）% at the dose of（6.25）,（12.5） and 50(mg·kg^-1),respectively.CONCLUSION: The genistein is excreted mainly in the form of glucuronidated genistein in rat urine.The genistein and glucuronidated genistein are excreted in the manner of non-linear dose-dependent.更多还原