Pharmacokinetics and bioequivalence of a generic empagliflozin tablet versus a brand-named product and the food effects in healthy Chinese subjects

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 C_max, AUC_0–t, and AUC_0-∞ 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 C_max, AUC_0–t, and AUC_0-∞ 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 C_max, AUC_0–t, AUC_0–∞, or T_max 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.

Keywords:

• Empagliflozin
• pharmacokinetics
• bioequivalence
• LC–MS/MS
• fasting and fed conditions

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.