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目的:研究二苯乙烯苷(THSG)单体及其β-环糊精包合物对大鼠灌胃后经胆汁、粪和尿的排泄特征。方法:大鼠分别灌胃给予THSG单体及其β-环糊精包合物,24h内收集胆汁,72h内收集尿液和粪便,采用HPLC-UV测定生物样品中THSG含量。结果:HPLC-UV测定方法的专属性、标准曲线线性关系、样品回收率和日内、日间精准度均符合生物样品测定要求。THSG单体及其β-环糊精包合物对大鼠灌胃给药后,粪便以原型形式排泄分别占总药量的3.27%,0.61%,胆汁排泄分别为0.20%,0.18%,尿液中仅检出少量THSG。结论:β-环糊精包合物减少了THSG原型经粪便的排泄,但不改变THSG原型的胆汁和尿液排泄特征。
Objective: To investigate the excretion of bile, feces and urine after intragastric administration of stilbene glycoside (THSG) monomer and its β-cyclodextrin inclusion complex. METHODS: Rats were given intragastric administration of THSG monomer and its β-cyclodextrin inclusion complex. Bile was collected within 24 hours. Urine and feces were collected within 72 hours. The content of THSG in biological samples was determined by HPLC-UV. RESULTS: The specificity of the HPLC-UV assay method, the linearity of the standard curve, the sample recovery rate, and the intra- and inter-day precision all met the requirements for the determination of biological samples. After oral administration of THSG monomer and its β-cyclodextrin inclusion complex to rats, fecal excretion in the prototype form accounted for 3.27% and 0.61% of the total dose, and biliary excretion was 0.20% and 0.18%, respectively. Only a small amount of THSG was detected in the liquid. CONCLUSIONS: β-cyclodextrin inclusions reduce fecal excretion of THSG prototypes but do not alter the bile and urine excretion characteristics of the THSG prototype.