Abstract
Objective
The aim of the present study was to assess the bioequivalence of a generic empagliflozin tablet versus a brand-named empagliflozin tablet (Jardiance®) and evaluate the food effects on the pharmacokinetics (PK) of empagliflozin in healthy Chinese subjects.
Methods
Forty-eight healthy volunteers were included in this randomized, open-label, crossover, two-period study (fasting: n = 24, fed: n = 24). A single dose of 25-mg generic (or test) or brand-named (or reference) empagliflozin was administered to each subject in a randomized sequence. Blood samples were collected at the baseline and during the 72 h post-dose, and plasma empagliflozin concentrations were determined by high performance liquid chromatography–tandem mass spectrometry (HPLC–MS/MS). Pharmacokinetic parameters were analyzed with non-compartmental methods. Safety was monitored.
Results
The major PK parameters including Cmax, AUC0–t, and AUC0-∞ were similar between the generic and brand-named tablets under fasting and fed conditions (all p > .05). The 90% confidence intervals of the test/reference ratios of log-transformed Cmax, AUC0–t, and AUC0-∞ were 94.90–106.70%, 100.62–106.99%, and 100.64–106.85%, respectively, under fasting condition, and 94.21–104.91%, 97.31–101.79%, and 97.32–101.83%, respectively, under fed condition. High-fat food did not affect Cmax, AUC0–t, AUC0–∞, or Tmax of empagliflozin (all p > .05). There was no serious adverse event during the study period.
Conclusion
The generic formulation of empagliflozin tablet is bioequivalent to the brand-named product in healthy Chinese volunteers, and well tolerated. High-fat food had no effects on the PK of empagliflozin in healthy Chinese volunteers.
Acknowledgements
The authors gratefully acknowledge all the volunteers for their contribution to this clinical trial. We sincerely thank Shanghai Xihua Scientific Co. Ltd for their support in analyzing the samples.
Disclosure statement
The test and reference empagliflozin tables were provided by Chia Tai Tianqing Pharmaceutical Group Co., Ltd., China.