OBJECTIVE This study was conducted to evaluate the pharmacokinetic properties and bioequivalence of two oral formulations of canagliflozin: a newly developed generic formulation (test) and a branded formulation (reference). METHODS A randomized, open-label, two-way crossover study was conducted in 55 healthy Chinese subjects. They were randomized to receive a single oral dose of 100 mg of test or reference canagliflozin tablets according to an open crossover design under fasting and fed states. Plasma canagliflozin concentrations were determined by liquid chromatography-tandem mass spectrometry, and the pharmacokinetic parameters maximum concentration (Cmax) and area under the concentration-time curve (AUC0-t and AUC0-∞) were used to evaluate bioequivalence. RESULTS The geometric mean ratio 90% confidence intervals for fasting Cmax, AUC0-t, and AUC0-∞ were 85.14 - 114.40%, 102.14 - 106.51%, and 102.21 - 106.85%, respectively, and fed Cmax, AUC0-t, and AUC0-∞ were 90.15 - 107.17%, 97.38 - 102.19%, and 96.78 - 101.92%, respectively. The mean values of tmax were prolonged in the test compared with the reference formulations. In addition, the mean values of tmax and Cmax for both formulations were significantly different under fed compared with fasting conditions, while there was no significant difference in AUC0-t or AUC0-∞. CONCLUSIONS The two types of canagliflozin tablets were bioequivalent under both fasting and fed states, and both were generally well tolerated.