Tetramethylpyrazine, isolated from Ligusticum wallichii Franch., is widely used for the treatment of cerebrovascular and cardiovascular diseases in China. To assess and compare the pharmacokinetic characteristics and bioequivalence of two tetramethylpyrazine phosphate (TMPP) tablets in healthy Chinese male subjects. 20 healthy male subjects were randomly divided into two groups according to a two-period crossover design test. A single oral dose of 200 mg test or reference tablets was given with a 7-day washout period under fasting conditions. Blood samples were taken at scheduled time points, and the concentration of TMPP was measured by LC-MS. Drug And Statistical Software-Version 2.0 was used to calculate the pharmacokinetic parameters and assess bioequivalence of the two formulations. 20 subjects were enrolled in the study, and none dropped out. The main pharmacokinetic parameters of test and reference formulations were as follows: T1/2 was (1.79±0.82) hours and (1.64±0.52) hours, tmax was (0.76±0.37) hours and (0.94±0.44) hours, Cmax was (961.14±309.64) ng/mL and (1,059.09±350.69) ng/mL, AUC0-12h was (1,744.69±643.49) ng×h/mL and (1,726.32±494.11) ng×h/mL, AUC0-∞ was (1,756.95 ± 643.63) ng×h/mL and (1,740.16±504.89) ng×h/mL, respectively. The relative bioavailability of TMPP tablets was 102.4±26.0%, and no serious adverse events were reported. This single-dose study in healthy Chinese male fasted subjects showed that the TMPP test and reference tablets were bioequivalent. .