Abstract: A simple HPLC-UV method was established to determine concentrations of ketoprofen (KP) in rabbit plasma following oral administration. Twelve rabbits were selected and divided into three groups. KP β-CD inclusion complex suspension, KP entity suspension (in 0.5% CMC-Na) and 0.5% CMC-Na suspension (as a placebo group) were administered orally to the three groups of rabbits, respectively. Differences in the pharmacokineticspharmacodynamics (PK-PD) parameters between KP β-CD inclusion complex and KP entity were examined. The results indicate that the established HPLCUV method could be used to assay the concentrations of KP in rabbit plasma with good precision. The distribution phase T_1/2α of the complexated KP was 0.4 h, while that of the KP entity was 0.56 h, KP in β-CD inclusion complex could be absorbed more rapidly. The early effect values of the KP inclusion complex were higher than those of the KP entity. The maximal antipyretic effect occurred after the peak of plasma concentration. This phenomenon indicates that the effect compartment of ketoprofen is in the peripheral compartment.