UPLCPDA法研究Liguzinediol在大鼠体内的排泄

Study on the Excretion of Liguzinediol in Rats by UPLCPDA Method

    摘要
  • 摘要: 目的 采用UPLCPDA法对Liguzinediol及其代谢产物在大鼠体内的排泄进行研究。方法 SD大鼠雌雄各6只，尾静脉注射给药10mg/kg，按照时间点分别收集尿液、胆汁、粪便，样品经甲醇处理后，取上清液N2吹干，流动相复溶。采用UPLCPDA法对大鼠尿液、胆汁、粪便中Liguzinediol及其代谢产物进行测定，通过代谢产物与原型药物的吸收系数之比及分子量折算确定代谢产物的换算因子，计算Liguzinediol在大鼠体内的累计排泄量占剂量的百分比（Dose%）。结果 雌雄大鼠尿液、胆汁及粪便排泄过程略有差异，Liguzinediol及其主要代谢产物在雌性大鼠的尿液、胆汁及粪便的Dose%分别为47.94%、16.67%、0.648%，体内累计Dose%为65.26%;Liguzinediol及其主要代谢产物在雄性大鼠的尿液、胆汁及粪便的Dose%分别为35.00%、20.37%、1.156%，体内累计Dose%为56.53%。结论 采用加换算因子的UPLCPDA法可以简便、快速地对Liguzinediol 在大鼠体内的物质平衡进行探索性研究，为开展药物临床研究提供实验依据。

     

    Abstract: OBJECTIVE To study the excretion of Liguzinediol and its metabolites in rats by UPLCPDA method. METHODS Six SD rats were administered intravenously at a dose of 10mg/kg. Its urine， bile and feces were collected according to certain time points. The samples were treated by methanol and the supernatant was dried by N2， then dissolved by mobile phase. Liguzinediol and its metabolites in urine， bile and feces were determinated by UPLCPDA. Conversion factor was confirmed through the determination of UV absorption coefficient and molecular weight of prototype drug together with its metabolites. Then the cumulative excretion of Liguzinediol in rats(Dose%) was calculated. RESULTS There were slight differences in the excretion process between female and male rats. The Dose% of Liguzinediol and its main metabolites in female rats urine， bile and feces respectively were 47.94%， 16.67% and 0.648%， and the total Dose% was 65.26%. The Dose% of Liguzinediol and its main metabolites in male rats urine， bile and feces respectively were 35.00%， 20.37% and 1.156%， and the total Dose% was 56.53%. CONCLUSION The UPLCPDA method with the addition of conversion factor can be used to explore the material balance of Liguzinediol in rats， and provide experimental evidence for clinical research.

     

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