杠柳毒苷在大鼠体内排泄的初步研究*

目的]研究杠柳毒苷在大鼠体内的排泄情况.方法]建立了液-液萃取后用高效液相色谱测定大鼠尿液、粪便和胆汁中杠柳毒苷含量的方法,并对大鼠静注及灌胃杠柳毒苷后的排泄情况进行分析.结果]大鼠按12mg/kg剂量灌胃给予杠柳毒苷后,72 h尿中杠柳毒苷和其代谢物的累积排泄量占给药剂量的0.44%,粪中杠柳毒苷和其水解代谢物的累积排泄量占给药剂量的12.39%;按0.74 mg/kg剂量尾静脉注射给予杠柳毒苷后,72 h尿中杠柳毒苷及其代谢物的累积排泄量占给药剂量的6.24%,粪中杠柳毒苷及其水解代谢物的累积排泄量占给药剂量的7.33%;按0.74 mg/kg剂量尾静脉注射给予杠柳毒苷后,21 h内累积经胆汁排泄的杠柳毒苷占给药总量的76.13%.结论]杠柳毒苷原形药物主要经胆汁排泄,但从尿液和粪便排泄则很少,尿液中可能存在结合代谢物,粪便中主要以肠菌代谢物(杠柳次苷)的形式排泄.

Study on excretion of periplocin in rats

Objective] To study on excretion of periplocin in rats.Methods] A liquid-liquid extraction followed by high performance liquid chromatography (HPLC) method was used to detect the content of periplocin in feces,urine and bile of rats.Then the study of excretion after oral and intravenous administration was carried out.Results] After oral administration Periplocin at a dose of 12mg/kg,the cumulative excretions of Periplocin and its conjugated metabolite in urine within 72h was 0.44%,and in feces the values of Periplocin and its hydrolytic metabolite was 12.39%.When administered intravenously at a dose of 0.74mg/kg,the cumulative excretions of Periplocin and its conjugated metabolite in urine within 72h was 6.24%,and in feces the values of Periplocin and its hydrolytic metabolite was 7.33%,and the cumulative excretions of Periplocin in bile within 21h was 76.13%.Conclusion] Periplocin was mainly eliminated via bile,but hardly via feces and urine.And Periplocin was eliminated via feces and urine in the forms of its metabolites by intestinal bacteria (deduced as Periplocymarin),conjugated metabolites,respectively.