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目的采用UPLC-PDA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10mg/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UPLC-PDA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UPLC-PDA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。
Objective To study the excretion of Liguzinediol and its metabolites in rats by UPLC-PDA. Methods Six male and one female SD rats were injected intravenously with 10mg / kg intravenous injection. Urine, bile and feces were collected respectively at different time points. After the sample was treated with methanol, the supernatant N2 was blown dry and the mobile phase was reconstituted. The UPLC-PDA method was used to determine the Liguzinediol and its metabolites in urine, bile and feces of rats. The conversion factor of metabolites was determined by the ratio of the absorption coefficients of the metabolites to the prototype drugs and the molecular weight. The Liguzinediol Cumulative excretion as a percentage of dose (Dose%). Results The excretion of urine, bile and feces of male and female rats were slightly different. The Dose% of urine, bile and feces of Liguzinediol and its major metabolites were 47.94%, 16.67% and 0.648% in female rats, respectively. % Was 65.26%. The Dose% of urine, bile and feces of Liguzinediol and its major metabolites in male rats were 35.00%, 20.37% and 1.156%, respectively. The cumulative Dose% in vivo was 56.53%. Conclusions The UPLC-PDA method with addition and subtraction factors can explore the substance balance of Liguzinediol in rats easily and quickly, and provide the experimental basis for the clinical research of drugs.