Pharmacokinetic profile of 2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside in mice after oral administration of Polygonum multiflorum extract.

CONTEXT

Stilbene glycoside (2,3,5,4'-tetrahydroxystilbene-2-O-β-D-glucoside) is a main bioactive component of Polygonum multiflorum, a traditional Chinese medicine (TCM) commonly used in clinic for anti-aging treatment. Its medicinal activities, such as anti-oxidation, anti-inflammation and endothelial protection, have been extensively studied, but its pharmacokinetic property is still unclear.

OBJECTIVE

A pharmacokinetic study was undertaken to quantitatively determine P. multiflorum stilbene glycoside (PM-SG) in mouse plasma after oral administration of 100 mg/kg P. multiflorum extract.

MATERIALS AND METHODS

A sensitive reversed-phase high-performance liquid chromatography (RP-HPLC) coupled with liquid-liquid phase extraction method was employed for this study. Pharmacokinetic parameters of PM-SG were determined in mice applying both compartmental and non-compartmental analyses.

RESULTS AND DISCUSSION

The calibration curve for PM-SG in the plasma was linear (r(2) > 0.99) over the range of 0.66 to 56.40 μg/ml, and the concentration-time curve was plotted with the maximum concentration (C(max)) and time to reach maximum concentration (T(max)) of 29.62 μg/ml and 60 min, respectively. The intra- and inter-day variations were less than 3% for relative standard deviation (RSD) and relative error (RE), with a good recovery of more than 97% (RSD <3%). All pharmacokinetic parameters estimated by compartmental and non-compartmental models reached a same conclusion that PM-SG was rapidly absorbed and widely distributed throughout the body with a great efficiency of utility, followed by quick elimination and clearance.

CONCLUSIONS

This was the first report on determination of the pharmacokinetic profile of PM-SG in mice after oral administration. The result may provide a meaningful basis for evaluating the clinical applications of such a bioactive compound from herbal medicines.