摘要
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。
To study renal, biliary, and intestinal excretion of arsenic and its four metabolites in Realgar in rats after single dose of oral administration. Method： Rats were orally administrated with single dose 75mg/kg. Total arsenic concentrations in urine, bile, and arsenic contents in feces were determined by atomic spectrophotofluorimetry （AFS） after microwave digestion pretreatment. Concentrations of four arsenic metabolites （ iAs（ Ⅲ） ,iAs（Ⅴ） ,MMA,DMA） were tested by AFS after separation by ion exchange resin. PK Solutions 2.0TM soft-ware was used to process experimental data. Results： Parameters of excretion of total arsenic and its four metabolites in rat urine, bile and feces were first reported. Amount of total arsenic excreting in feces was 97.7% of the dose intake. Only 0.0367% excreted by urine. The amount of biliary excretion was 35.39%. However, most of the metabolites in bile excreted with feces instead of entering into the blood circulation. Conclusion： Intestinal excretion is the main excretion pathway of Realgar. Renal excretion does not appear to be the main elimination route for Realgar. There is existence of hepato-enteric circulation of arsenicals in Realgar.
出处
《中药药理与临床》
CAS
CSCD
北大核心
2009年第3期39-42,共4页
Pharmacology and Clinics of Chinese Materia Medica
基金
国家自然科学基金资助项目(30672637)
关键词
雄黄
砷
代谢物
排泄
药物动力学
Realgar, arsenic, metabolite, excretion, pharmacokinetics
