生物等效性和生物利用度杂志

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A Bioequivalence Study Comparing Two Formulation of Emtricitabine Capsules

A.T. Bapuji, M. Nagesh, D. Ramaraju, Syed Syedba, Ravi Kiran, S. Ravinder and D.Chandrapal reddy

This investigation was carried out to evaluate the bioavailability of emtricitabine 200mg capsules (Test) of Aurobindo Pharma Ltd, India, relative to reference product, Emtriva 200mg capsules, manufactured by Gilead Sciences, Inc., USA. The bioavailability study was carried out on 36 healthy male volunteers who received a single dose of emtricitabine 200mg of the test (T) and the reference ( R ) products in the fasting state, in a randomized, balanced, 2-way cross-over design. After dosing, serial blood samples were collected for a period of 48 hours. Plasma obtained from blood was analyzed for emtricitabine by a sensitive and validated simultaneous liquid-chromatographic and mass-spectrometric (LC-MS/ MS) assay. The maximum plasma concentrations (Cmax), area under the plasma concentration-time curve up to the last measurable concentration (AUC0-t), and to infinity (AUC0-α) and the time to maximum concentration (tmax) were analyzed statistically. The parametric confidence intervals (90%) were calculated. It was found that the test/reference (T/R) ratios for the pharmacokinetic parameters (AUC0-t), (AUC0-α) and (Cmax) were well within the Bioequivalence acceptance range of 80 – 125% as per international regulatory guidelines. Therefore, the two formulations were considered to be bioequivalent.