Abstract: AIMTo establish a method to determine the concentration and phatmacokinetic parameters of stilbene glucoside in plasma of mice and rabbits by using HPLC. METHODSThe analytical column was Diamonsil^TM C₁₈ column (250 mm×4.6 mm, 5 μm). The mobile phase consisted of acetonitrile-methanol-1% formic acid (15∶18∶67). The flow rate was 1.0 mL·min^-1. The UV detection wavelength was set at 320 nm. RESULTSThe standard curve range was 0.41～42.0 μg·mL^-1 (γ=0.9999). The lowest detection concentration was 0.051 μg·mL^-1. The recoveries in three different concentrations (high, middle and low) were 97.98%, 101.7% and 104.5%, respectively, the RSD of within-day were 8.7%, 2.9% and 5.5%, respectively. The mean plasma concentration-time curves of stilbene glucoside after intravenous administration were confirmed to be open two-compartment model in mice and rabbits. The T_1/2α, T_1/2β, K₂₁, K₁₂, K₁₀, V_c, AUC, CL of mice were 1.9 min, 8.3 min, 6.6 h^-1, 3.8 h^-1, 16.0 h^-1, 0.090 L·kg^-1, 6.918 mg·h·L^-1 and 1.445 L·h^-1·kg^-1, respectively. The T_1/2α, T_1/2β, K₂₁, K₁₂, K₁₀, V_c, AUC, CL of rabbits were 2.7 min, 13.5 min, 4.2 h^-1, 3.0 h^-1, 11.2 h^-1, 0.198 L·kg^-1, 4.530 mg·h·L^-1, and 2.208 L·h^-1·kg^-1, respectively. The absorption of stilbene glucoside was irregular after oral administration to mice, the plasma concentration was very low and the pharmacokinetic characteristic did not comply with any compartment model. CONCLUSIONThe method was quick, precise and reproducible. It can be used to determine the concentration of stilbene glucoside in plasma and to obtain the pharamacokinetic parameters.