Abstract
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.
Highlights
Emtricitabine (FTC; Emtriva), a potent doxycytidine nucleoside reverse transcritase inhibitor is used to treat human immunodeficiency virus (HIV) infection
As a nucleoside reverse transcriptase inhibitor (NRTI), emtricitabine is readily anabolized by cellular enzymes in a step wise fashion to form its mono phosphate, diphosphate, and 5 ́-triphosphate (TP) form, the active intracellular moiety that inhibits HIV-1 reverse transcriptase (RT) and HBV DNA polymerase (Wilson et al, 1993; Furman et al, 1995; Davis et al, 1996)
The subjects’ mean BMI was 21.56 (18.04 – 25.00) kg/m2. 4 subjects withdrew from the study prior to receiving the formulation (1subject for test and 3 subjects for reference) due to absent for the participation in period 2 and positive for drugs of abuse
Summary
Emtricitabine (FTC; Emtriva), a potent doxycytidine nucleoside reverse transcritase inhibitor is used to treat human immunodeficiency virus (HIV) infection. FTC has demonstrated linear kinetics over a wide dose range and FTC 200mg once a day is the recommended therapeutic dose. Emtricitabine is rapidly and extensively absorbed followed oral administration, with peak plasma concentration occurring within 1.5 hr of dosing and with an oral bioavailability >90% (Wang et al, 2001; Gish et al, 2002). Emtricitabine disposition follows linear kinetics with small intersubject variability and plasma emtricitabine concentrations increased dose propotionally over a wide dose range (100-1200mg) (Wang et al, 1995). Emtricitabine does not appreciably bind to plasma proteins (
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