OBJECTIVE:To establish a method for the determination of dasatinib concentration in human plasma and study the bioequivalence of 2 kinds of tablets. METHODS:In a randomized two-way crossover study,24 healthy male volunteers were divid-ed into two groups,and were administered respectively with test and reference preparations 100 mg under fasting and fed condi-tions. The plasma concentration of dasatinib was determined by LC-MS/MS. Using imatinib mesylate as internal standard,the deter-mination was performed on Welchrom C18 column with mobile phase consisted of acetonitrile-0.1% formic acid(70∶30,V/V). Posi-tive ion scanning was conducted under MRM mode,ESI,and ion pair for quantitative analysis were m/z 488.5→401.2 (dasatinib) and m/z 494.6→394.2(internal standard). DAS 3.2.8 software was used for data processing and variance analysis was adopted to in-vestigate the bioequivalence of 2 kinds of tablets. RESULTS:The linear rang of dasatinib was 1-300 ng/ml. The pharmacokinetic pa-rameters of test and reference preparations under fasting conditions were as follows:cmax were (165.599 ± 67.592) and (164.533 ± 77.960)ng/ml;tmax were(1.145±0.504)and(1.080±0.467)h;t1/2 were(5.080±2.262)and(3.771±1.596)h;AUC0-36 h were (550.487 ± 256.494) and (585.986 ± 324.885) ng·h/ml. The pharmacokinetic parameters of test and reference preparations under fed conditions were as follows:cmax were(163.058±47.533)and(165.440±53.012)ng/ml;tmax were(1.630±1.066)and(1.576± 0.530)h;t1/2 were(4.720±2.677)and(4.311±2.610)h;AUC0-36 h were(568.036±192.521)and(601.100±216.855)ng·h/ml. Relative bioavailability of AUC0-36 h under fasting and fed conditions were(100.2±7.5)% and(99.2±3.8)%. Analysis of variance showed there were no significant difference in the pharmacokinetic parameters of between 2 preparations and cyde(P>0.05),there was statistical significance among subjects(P<0.05). CONCLUSIONS:LC-MS/MS method can determine the concentration of da-satinib in human plasma rapidly;and the two preparations are bioequivalent.