Dioscin (diosgenyl 2,4-di-O-alpha-l-rhamnopyranosyl-beta-d-glucopyranoside) is an important constituent of some traditional Chinese medicines with several bioactivities. We have investigated the pharmacokinetics of dioscin in rat after intravenous and oral administrations. Compartmental methods were used to perform pharmacokinetic data analysis. The dose-dependent pharmacokinetics of dioscin was characterized after intravenous administrations (0.064, 0.16, 0.4 and 1.0mg/kg) to rats. There was significant decrease in clearance with increasing dose (4.67+/-0.09 ml/min/kg (0.064 mg/kg) versus 3.49+/-0.23 ml/min/kg (1.0 mg/kg), P<0.05), and the plot of reciprocal clearance values versus the doses was linear (r=0.909, P<0.05). After an I.V. dose of 1mg/kg, simultaneous oral gavage of activated charcoal did not change the pharmacokinetic parameters indicating enterohepatic recycling of dioscin is not important in rat. The absolute oral bioavailability was very low (0.2%). In tissue distribution and bile excretion studies after I.V. and oral administrations, dioscin was shown to undergo a prolonged absorption from the intestinal tract and slow elimination from organs, and only a small amount of drug was recovered in bile. The cumulative amounts of dioscin in feces and urine indicated that the parent drug is mainly excreted in the feces.

中文翻译：

---

薯di皂素在大鼠体内的药代动力学特征。

薯os皂素（2，4-二-O-α-鼠李糖吡喃糖基-β-d-吡喃葡萄糖苷）是一些具有多种生物活性的中药的重要成分。我们已经研究了静脉和口服给药后洋地黄素在大鼠体内的药代动力学。隔室方法用于进行药代动力学数据分析。在大鼠静脉内给药（0.064、0.16、0.4和1.0mg / kg）后，对薯os的剂量依赖性药代动力学进行了表征。清除率随剂量增加而显着降低（4.67 +/- 0.09 ml / min / kg（0.064 mg / kg），而3.49 +/- 0.23 ml / min / kg（1.0 mg / kg），P <0.05）和相对清除率值与剂量的关系图呈线性关系（r = 0.909，P <0.05）。静脉注射1mg / kg后，口服活性炭同时进行管饲并没有改变药代动力学参数，这表明薯os的肠肝循环在大鼠中并不重要。绝对的口服生物利用度非常低（0.2％）。在静脉和口服给药后的组织分布和胆汁排泄研究中，薯os皂素显示出从肠道的吸收延长和从器官的缓慢清除，并且胆汁中仅回收了少量药物。粪便和尿液中薯os素的累积量表明母体药物主要从粪便中排泄。已显示出薯os皂素在肠道中的吸收时间延长，在器官中的清除速度缓慢，并且胆汁中仅回收了少量药物。粪便和尿液中薯os素的累积量表明母体药物主要从粪便中排泄。已显示出薯os皂素在肠道中的吸收时间延长，在器官中的清除速度缓慢，并且胆汁中仅回收了少量药物。粪便和尿液中薯os素的累积量表明母体药物主要从粪便中排泄。