Abstract: Aim To establish RP-HPLC method for determination of plasma scutellarin concentration and study of the pharmacokinetic behavior of scutellarin in rat after ig administration of breviscapine and its β-cyclodextrin complex (breviscapine-β-CD). MethodsMobile phase composed of methanol and acetate buffer. The column was Shim-pack Ｃ₁₈.Twelve rats randomized into 2 groups were separately given breviscapine and breviscapine-β-CD at single dose of 10.8 mg·kg^-1. Drug in plasma was extracted and determined by HPLC. The pharmacokinetic parameters were calculated by 3P97 software. Results Linearity was obtained over the range of 10-400 ng·mL^-1. The recovery was 95.32%-98.81%. C_max and AUC_0-12h of breviscapine were (154±18) ng·mL^-1 and (710±126) ng·h·mL^-1. For breviscapine-β-CD, C_max and AUC_0-12h were (328±31) ng·mL^-1 and (1 093±200) ng·h·mL^-1, respectively. There were significant differences of AUC_0-12h between breviscapine and breviscapine-β-CD (P<001). ConclusionThe assay method was suitable for the determination of scutellarin plasma concentration in rat. Brevescapine-β-CD showed greater absorption compared with that of brevescapine.