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目的:研究雄黄单次给药后,雄黄中的砷及其四种代谢物在大鼠的肾脏、胆汁和肠道(粪便)的排泄动力学。方法:大鼠单次灌胃给药75mg/kg。大鼠尿液、胆汁、粪便进行微波消解后,用原子荧光光度法(AFS)测定其总砷浓度;采用离子交换树脂对大鼠尿液、胆汁、粪便中的四种砷代谢物(iAs(Ⅲ)、iAs(Ⅴ)、MMA、DMA)进行分离后,用AFS法测定各代谢物浓度。应用PK Solutions2.0TM药动学软件计算动力学参数。结果:报道了雄黄中的总砷及其四种砷代谢物在大鼠尿液、胆汁、肠道中的排泄动力学参数。粪便总砷排泄量占服用量的97.7%;肾排泄量仅占服用量的0.0367%;胆汁排泄量占服用量的35.39%,但绝大部分代谢物并未进入血液中,而是经肠道随粪便排出体外。结论:雄黄主要经肠道通过粪便排泄,肾脏排泄不是雄黄中的砷的主要排泄途径。雄黄中的砷在体内存在肝肠循环。
Objective: To study the excretion kinetics of arsenic in realgar and its four metabolites in rat kidney, bile and intestine (feces) after a single administration of realgar. Methods: Rats were administered orally with 75mg / kg orally. Rat urine, bile, and feces were subjected to microwave digestion, and their total arsenic concentrations were determined by atomic fluorescence spectrometry (AFS). Four kinds of arsenic metabolites (iAs Ⅲ), iAs (Ⅴ), MMA, DMA), the concentration of each metabolite was determined by AFS method. PK kinetics software was used to calculate kinetic parameters. Results: The excretion kinetics parameters of total arsenic in realgar and its four arsenic metabolites in urine, bile and intestine of rats were reported. Excretion of total arsenic accounted for 97.7% of the total amount of excretion; renal excretion accounted for only 0.0367% of the dose; biliary excretion accounted for 35.39% of the dose, but the vast majority of metabolites did not enter the bloodstream, but by the intestinal tract Excreted with the excrement. Conclusion: Realgar is mainly excreted through the intestine via excretion, and renal excretion is not the main excretion pathway of arsenic in realgar. Realgar in the presence of arsenic in the body enterohepatic circulation.