Abstract: OBJECTIVE To establish a sensitive precolumn derivatization HPLC method for determination of plasma concentration of asiatic acid(AA) and evaluate its pharmacokinetics characteristics in rats. METHODS The male SD rats were intravenously administrated AA by 10 mg?kg^-1. The plasma samples were taken at different times, concentrated by SPE method and determined by precolumn derivatization RP-HPLC method, the glycyrrhetinic acid was used as an internal standard. The pharmaeokinetie parameters were accessed by PKS 1.0. RESULTS Excellent liner relationship was obtained in the range of 0.1 to 20 μg?mL^-1(r=0.999 6). The averang extraction recovery was 71.1%?79.9%. The intra- and inter-day RSDs were less than 13%. The samples were stabled at -20 ℃, and remained stable after twice freeze-thaw cycles. AA was fitted to a one compartment open model in rats, mainly pharmacokinetic parameters as follow: t_max=2.0 min, C_max=14.7 μg?mL^-1, t_1/2=35.1 min, AUC_0-t=217.0 μg?min?mL^-1, AUC_0-∞=234.3 μg?min?mL^-1. CONCLUSION AA is disposed extensively and rapidly in rats. The method can be used to determine the concentration and to investigate the pharmacokinetics of AA in rats.