Abstract: OBJECTIVE To explore the pharmacokinetics and bioequivalence of trimebutine maleate sustained-release tablets with multiple dose administration in healthy Chinese volunteers. METHODS A multiple oral dose (300 mg of test or reference preparation twice a day for 6 days) were given to 26 male healthy volunteers in a randomized crossover study. The concentration of trimebutine and N-demethyl trimebutine in plasma were determined by HPLC-MS/MS. The pharmacokinetic parameters were calculated and the bioequivalence of 2 formulations were evaluated by DAS program. RESULTS After multiple dose, the pharmacokinetic parameters of the test and reference trimebutine were as follows: C_max were (35.668±22.196), (33.022±16.077)ng·mL^-1, t_max were (3.154±1.875), (0.365±9.946)h, t_1/2 were (20.793±13.305)h and (16.989±4.707)h, AUC_ss were (252.075±150.358), (224.106±95.405)ng·h·mL^-1, respectively. Meanwhile, the pharmacokinetic parameters of N-demethyl trimebutine were as follows: C_max were (1 571.809±823.169), (1 623.535±536.813)ng·mL^-1, t_max were (-0.250±11.259), (2.481±1.237)h, t_1/2 were (9.796±2.450), (9.220±2.009)h, AUC_ss were (11 254.863±5 746.620), (10 911.059±4 111.751)ng·h·mL^-1, respectively. CONCLUSION The test and reference preparation of trimebutine are bioequivalent.