AIM: To assess the bioequivalence of oral dexamethasone acetate tablets between the test and reference formulations in healthy adult Chinese subjects on an empty stomach and after meals. METHODS: A randomized, open, single-dose, two-cycle double crossover bioequivalence study was followed. Twenty-four healthy subjects were included in the fasting group, and 32 healthy subjects were included in the postprandial group, taking 2 tablets (0.75 mg/tablet) of the test formulation (T) or 3 tablets (0.50 mg/tablet) of the reference formulation (R) per cycle for two cycles. The concentrations of dexamethasone acetate in human plasma were determined using liquid chromatography-mass spectrometry, and the pharmacokinetic parameters were calculated according to the non-atrial model using WinNonlin 8.0 software.The bioequivalence of both the test formulation and the reference formulation was evaluated. RESULTS: The pharmacokinetic parameters after oral administration of dexamethasone acetate tablets in a fasted state in subjects with the reference formulation are as follows: Tmax 1.13 (0.50, 4.00) and 1.00 (0.50,5.00) h, AUC0-t (72.25±21.55) and (69.23±17.76) ng·mL-1·h, Cmax (14.53±4.51) and (14.52±3.68) ng/mL, AUC0-∞ (74.63±23.01) and (71.32±19.12) ng·mL-1·h. The pharmacokinetic parameters after oral administration of dexamethasone acetate tablets in the postprandial state in subjects were as follows: Tmax 2.00 (1.00,4.50) and 1.50 (1.00, 4.50)h, AUC0-t (81.57±21.28) and (76.06±13.63) ng·mL-1·h, Cmax (12.14±3.21) and (11.93±2.78) ng/mL, and AUC0-∞ (85.12±23.92) and (78.95±14.99) ng·mL-1·h. The 90% confidence intervals for the geometric mean ratios of the main pharmacokinetic parameters of the test formulation of dexamethasone acetate to the reference formulation ranged from 80.00% to 125.00% under both fasting and postprandial conditions. CONCLUSION: Under fasting and postprandial conditions, the test formulation of dexamethasone acetate tablets was bioequivalent to the reference formulation of dexamethasone acetate tablets.