Ferruginol, a diterpene phenol, has recently received attention for its extensive pharmacological properties, including anti-tumor, antibacterial, cardio-protective and gastroprotective effects. In the present study, a high-performance liquid chromatographic (HPLC) method was developed for determination of ferruginol in rat plasma and applied for the pharmacokinetics study. The HPLC assay was performed with a VP ODS-C(18) column. The mobile phaseconsisted of methanol and 1% acetic acid solution (90:10, v/v). The flow rate was 1.0 mL/min, and the wavelength was set at 270 nm. This method was linear over the studied range of 0.1-10.0 microg/mL( )for ferruginol. The correlation coefficient was 0.9998. The intra-day and inter-day precisions were better than 4 and 5%, respectively. The extraction recovery and accuracy were greater than 97 and 96%, respectively. The detection limit was 30 ng/mL. The mean maximum concentration of ferruginol in rat plasma was 3.14 microg/mL at 40 min after oral administration at a dose of 20 mg/kg. Ferruginol was absorbed quickly p.o. with t(1/2)ka = 14.86 min and had a high rate of elimination with t(1/2) = 41.73 min. The pharmacokinetic process of ferruginol in rat was well described with a one-compartment model.