A simple and sensitive high-performance liquid chromatographic method for determination and identification of rutaecarpine in rat plasma has been developed. Up to 0.1 ml of plasma containing rutaecarpine was deproteinized by acetonitrile, which contained an internal standard (paeonol). The supernatant was injected onto a reversed-phase column using a acetonitrile-water-orthophosphoric acid (85%) (60:40:0.1, v/v/v, pH 2.5-2.8) as the mobile phase and ultraviolet detection at 344 nm. It was applied to the pharmacokinetic study of rutaecarpine in rat after a 2 mg/kg intravenous administration. A biphasic process with a rapid distribution followed by a slower elimination phase was observed from the plasma concentration-time curve. Compartmental analysis yielded a two-compartment model.