[Purpose]: To assess the pharmacokinetics of single-dose terbinafine (CAS 78628-80-5) 250 mg tablets in Chinese healthy volunteers.[Methods] :Plasma samples were obtained at 0 (pre-drug), 0.5; 1.0; 1.33; 1.67; 2.0; 2.33; 2.67; 3.0;4.0; 6.0; 9.0; 12.0; 24.0; 36.0; 48.0; 60.0; 72.0 and 84.0 h post-administration.Terbinafine levels were determined by HPLC-MS/MS and the plasma samples were validated at the calibration range from 2 to 2000 ng/mL.[Results]: The results showed that AUClast is 3550 +1065 (ngxhr/ml), AUCinf is 3985±1171 (ngxhr/ml), Cmax is 576+171 (ng/ml), MRT is 28.7±+8.4 (hr), Tmax is 1.57±0.75 (hr) and T1/2 is 45.9±12.0 (hr).[COnclusion]: More studies about multiple-dose pharmacokinetics of terbinafine and its effect to the drugs tnetabolized by CYP 2D6 with a narrow therapeutic index need to be done in Chinese.