An enantioselective high-performance liquid chromatographic assay for the quantitation of the enantiomers of flurbiprofen in human plasma is described. The procedure involved extraction of flurbiprofen from acidified plasma into hexane-diethyl ether (8:2, v/v). Stereoselective separation was achieved with a prepacked alpha 1-acid glycoprotein column without any derivatization procedure. A second assay using a conventional reversed-phase column to determine racemic flurbiprofen is also described. The detection wavelength was set at 246 nm. The limit of quantification was found to be 50 ng/ml for both assays. The method was demonstrated to be sufficiently sensitive for stereoselective pharmacokinetic studies of flurbiprofen.