Pharmacokinetics of methyl protodioscin in rats

Methyl protodioscin (MPD), a natural furostanol saponin, showed distinct antitumor activity and is distributed in many traditional Chinese medicines. The pharmacokinetics, distribution and excretion of MPD were first investigated after i.v. injection to rats in this study. The dose-dependent pharmacokinetics of MPD were characterized after i.v. injection (20, 40 and 120 mg/kg of MPD) to rats. A good linearity (r = 0.9989, P < 0.05) was found in the regression analysis of the AUC0-t-dose. The plasma concentrations of MPD declined rapidly with an elimination half-life (t1/2) from 25.56 to 29.32 min. The MPD kinetics was in line with one-compartment model after i.v. injection. 23.43% and 32.86% of MPD was recovered in urine and bile, respectively. The concentrations of MPD in plasma and most examined tissues 5 h after injection were close to or below the Low Limit of Quantification (LLOQ). This indicated that MPD was distributed and eliminated rapidly in rats.