OBJECTIVE: To develop a method for the determination of ropinirole in human plasma and pharmacokinetic study. METHODS: After precipitated with acetonitrile, using atenolol as internal standard, plasma sample was determined by UPLC-MS/MS. The separation was performed on Waters ACQUITY UPLC BEH Amide column with mobile phase consisted of water (containing 10 mmol/L ammonium acetate and 0.1% formic acid)-acetonitrile (85 ∶ 15,V/V) at flow rate of 0.3 mL/min. The column temperature was set at 40 ℃, and sample size was 5 μL. The analyses were carried out by ESI under MRM model in positive mode. The mass transition ion-pairs were as follows: m/z 261.2→114.1 (ropinirole) and m/z 267.2→145.0 (internal standard). 8 healthy volunteers were selected with a gender ratio of half to half, and were given Ropinirole hydrochloride tablets 1.0 mg. Plasma concentrations of ropinirole were determined before and after medication. The pharmacokinetic parameters were calculated by WinNonlin 6.3 software. RESULTS: The linear range of ropinirole were 0.02-2 ng/mL (r=0.997 3) with RSDs of inter-batch and intra-batch<10%; accuracy ranged 95.2%-99.7%, and extraction recoveries ranged 68.5%-79.9%. Both matrix effects and dilution effects didn’t influence the determination of plasma concentration. The main pharmacokinetic parameters of ropinirole in 8 healthy volunteers after oral administration of Ropinirole hyolrocholride tablets 1.0 mg were as follows: cmax was (2.1±0.5) ng/mL,tmax was (1.0±0.5) h, t1/2 was (4.7±1.5) h, AUC0-36 h was (14.7±6.0)ng·h/mL, AUC0-∞ was (15.1±6.1)ng·h/mL. There was no statistical significance in main pharmacokinetic parameters between different gender (P>0.05). CONCLUSIONS: The method is simple, sensitive and less time-consuming. It is suitable for the plasma concentration determination and pharmacokinetic study of ropinirole in human.