大鼠口服二苯乙烯苷及其β-环糊精包合物的排泄研究

Study on excretion of stilbene glycoside (THSG) and its β-cyclodextrin inclusion

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。

The excretion characteristics of stilbene glycoside （THSG） and its β-cyclodextrin inclusion in bile, urine and feces after oral administration to rats were studied. Bile for 24 h, urine and feces for 72 h were collected. The content of THSG was determined by HPLC-UV. The established HPLC-UV method was available for the analysis of THSG in excreta and corresponded to the requirement of biological sample analysis. After given THSG and its β-cyclodextrin inclusion, the amount of prototype THSG in feces were 3.27% and 0.61%, meanwhile THSG in bile were 0.20% and 0.18%, respectively. Only a little THSG was found in urine. The result showed that β-cyclodextrin inclusion reduced the fecal excretion of THSG. However, the characteristic of urinary and biliary excretion wasn′t changed.