Comparative pharmacokinetic profiles of glycyrrhetic acid (GA), glycyrrhizic acid (GL) and Gancao-Fuzi-Tang (KF) after oral administration of GL and KF were studied. Plasma samples taken from rats were acidified with acetic acid and GA was extracted with isopropanol-ethyl ether (1 : 1). Separation of GA was performed on a C(18) column with the detection wavelength set at 254 nm. The mobile phase was methanol-acetonitrile-water-acetic acid (58 : 18 : 24 : 1 v/v). The results showed that the mean residence time and area under the curve of GA in KF-administered rats were 27.6+/-1.5 h and 122.8+/-46.7 microg.h/ml respectively, which were significantly different from those in GL-administered rats (15.0+/-2.0 h and 40.9+/-9.6 microg.h/ml, respectively). The results suggest the increased effect of GA after oral administration of KF in comparison with GL.