Abstract

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_max) and area under the concentration-time curve (AUC_0–t and AUC_0–∞) were used to evaluate bioequivalence.
Results: The geometric mean ratio 90% confidence intervals for fasting C_max, AUC_0–t, and AUC_0–∞ were 85.14 – 114.40%, 102.14 – 106.51%, and 102.21 – 106.85%, respectively, and fed C_max, AUC_0–t, and AUC_0–∞ were 90.15 – 107.17%, 97.38 – 102.19%, and 96.78 – 101.92%, respectively. The mean values of t_max were prolonged in the test compared with the reference formulations. In addition, the mean values of t_max and C_max for both formulations were significantly different under fed compared with fasting conditions, while there was no significant difference in AUC_0–t or AUC_0–∞.
Conclusion: The two types of canagliflozin tablets were bioequivalent under both fasting and fed states, and both were generally well tolerated.

Author Details

Authors

• Wei Hu^{1, 2}
• Yaru Yang²
• Qian Zhang²
• Yang Yang²
• Renpeng Zhou²
• Chao Lu²
• Zeyuan Liu¹

Departments

• ¹ Department of Clinical Pharmacology, Affiliated Hospital of Academy of Military Medical Sciences, Beijing, and
• ² Department of Pharmacology, The Second Hospital of Anhui Medical University, Hefei, China

Address


Prof. Zeyuan Liu

Department of Clinical Pharmacology
Affiliated Hospital of Academy of Military Medical
Sciences
8 East Street, Fengtai District, Beijing 100071, China
Email: [email protected]

Citation