Abstract: A sensitive high performance liquid chromatographic analytical methed wasestablished for determining the concentration of matrine in human serum,The recovery of matrine was99.1～102.2%。The RSD(%)in within-day and between-days were no more than 6%, Thecalibration curve was linear in the range from l.25μg·mL^-1 to 40.0μg·mL^-1 with r=0.9997.The serum drug concentratiom- time curve after iv infusion with a dose of 6 mg .kg^-1 in l00 mlglucose solution for 8 heaIthy volunteers was fitted to a 2-compartment open model.The excretion ofunchanged drug in urine was 52. 75%of the dose in 32 h and the ClR was l43. 79 ml· min^-1.