Pharmacokinetic and bioequivalence study of emtricitabine/tenofovir disoproxil fumarate tablets in healthy Chinese subjects
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Objective: This study was conducted to evaluate the pharmacokinetics and bioequivalence of two emtricitabine (FTC)/tenofovir disoproxil fumarate (TDF) tablets: a newly developed generic formulation (test) and a branded formulation (reference) in healthy Chinese subjects under fasting and fed states.

Methods: A randomized, open-label, two-way crossover study was conducted in 64 healthy Chinese subjects. Subjects were randomized to receive a single oral dose of FTC 200 mg/TDF 300 mg of test or reference tablets according to an open crossover design under fasting and fed states. Plasma canagliflozin levels of FTC/TDF were determined by liquid chromatography tandem mass spectrometry (LC-MS/MS), and the pharmacokinetic parameters of 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 89.03 - 101.98%, 94.90 - 101.36%, and 94.94 - 101.56%, respectively, and fed Cmax, AUC0-t, and AUC0-∞ were 94.12 - 108.87%, 96.89 - 104.05%, and 96.69 - 104.28%, respectively.

Conclusions: The two types of FTC/TDF tablets were bioequivalent under both fasting and fed condition, and both were generally well tolerated.