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). MATERIALS AND 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 (C) and area under the concentration-time curve (AUC and AUC) were used to evaluate bioequivalence. RESULTS: The geometric mean ratio 90% confidence intervals for fasting C, AUC, and AUC were 85.14 - 114.40%, 102.14 - 106.51%, and 102.21 - 106.85%, respectively, and fed C, AUC, and AUC were 90.15 - 107.17%, 97.38 - 102.19%, and 96.78 - 101.92%, respectively. The mean values of t were prolonged in the test compared with the reference formulations. In addition, the mean values of t and C for both formulations were significantly different under fed compared with fasting conditions, while there was no significant difference in AUC or AUC. CONCLUSION: The two types of canagliflozin tablets were bioequivalent under both fasting and fed states, and both were generally well tolerated.