OBJECTIVE： To establish the method for pharmacokinetic study of luteolin and cynaroside in rats and to determine pharmacokinetic parameters. METHODS： 16 SD rats were randomly divided into luteolin group （sublingual iv， 1.34 mg/kg） and cynaroside group （sublingual iv， 0.64 mg/kg）. 0.5 ml blood were collected before administration and 0，15，30 min and 1，2，3，4，6， 8，12， 24， 48 h after administration respectively to prepare plasma. UPLC-TQ-MS was adopted to determine plasma concentration， and pharmacokinetic parameters were calculated. A CORTECSTM UPLC® C18 （100 mm×2.1 mm， 1.6 μm） column was used with mobile phase consisted of acetonitrile-water （containing 0.1％ formic acid） at a flow rate of 0.4 ml/min， the column temperature was set at 40 ℃， and quercetin was used as internal standard. RESULTS： The linear range of luteolin and cynaroside were 2.5-500 ng/ml （r＝0.998 2） and 10-2 500 ng/ml （r＝0.993 5）. The lowest quantitation limits were 1 and 2.5 ng/ml， and extraction were 70.75％-87.72％ and 75.40％-91.18％ （n＝6）； RSD of inter-day and intra-day were all lower than 10％ （n＝3）. Pharmacokinetic parameters as t1/2 were （1.88±0.32） and （1.57±0.08） h； CL were （0.77±0.18） and （0.06±0.01） L/（h·kg）； AUC0-6 h were （189.60±40.04） and （1 093.14±187.36） ng·h/ml；AUC0-∞ were （195.18±38.37） and （1 097.11±188.07） ng·h/ml. CONCLUSIONS： The method can be used for pharmacokinetic study of luteolin and cynaroside in rats， and the pharmacokinetics of them in rats are in line with two-compartment model.