Abstract
Moxifloxacin is a synthetic fluoroquinolone with a broad spectrum of antibacterial activity. It is indicated for the treatment of respiratory tract, skin and intra-abdominal infections. The aim of this study was to compare the bioavailability and to determine the bioequivalence of a test and reference formulation of oral moxifloxacin 400 mg, administered as a tablet, and to generate data regarding the oral bioavailability of this drug in Mexican population. This single-dose, randomized-sequence, open-label, two-period, crossover study was conducted on a total of 26 healthy Mexican adult subjects of both genders, with an eight-day washout period. Study formulations were administered after a 10-hour overnight fast. For pharmacokinetic analysis, blood samples were drawn at 0 (baseline), 0.25, 0.5, 0.75, 1, 1.5, 2, 3, 4, 5, 6, 8, 12, 24, 48 and 72 hours after administration. Plasma concentrations of moxifloxacin were determined using HPLC coupled with a fluorescence detector. The test and reference formulations were considered bioequivalent if the 90% CIs for the geometric mean test/reference ratios were within a predetermined range of 80% to 125%. The 90% CIs for the geometric mean ratios of Cmax, AUC0–t and AUC0–∞were 88.67% to 108.70%, 97.44% to 102.50%, and 97.70% to 104.82 %, respectively. In this study a single dose of the test formulation met the regulatory requirements for assuming bioequivalence, based on the rate and extent of absorption.
Highlights
Moxifloxacin hydrochloride is a synthetic fluoroquinolone antibacterial agent with a broad spectrum of activity, encompassing Gram-negative and Gram-positive bacteria, indicated for the treatment of respiratory infections [1,2].Moxifloxacin is well absorbed following oral administration with an absolute bioavailability of 91.8%. [3].Its mean elimination half-life is approximately 12 hours under steady-state conditions [4].Moxifloxacin shows linear pharmacokinetics after single doses ranging from 50 to 800 mg [5] and its bioavailability is not affected by the concomitant intake of food [6].The reference tablet formulation (Avelox®, Bayer de México, S.A. de C.V, Mexico City, Mexico) is marketed in Mexico
Itwas selected as the reference formulation because it is included in the list of Drug Reference Medications issued by the Mexican Federal Commission for the Protection against Sanitary Risks (COFEPRIS)
All the power values were >0.8, suggesting that the sample size was sufficient for the purpose of the study. These results indicated that the bioequivalence criteria were met, regardless of the exclusion of the outlier
Summary
Moxifloxacin hydrochloride is a synthetic fluoroquinolone antibacterial agent with a broad spectrum of activity, encompassing Gram-negative and Gram-positive bacteria, indicated for the treatment of respiratory infections [1,2].Moxifloxacin is well absorbed following oral administration with an absolute bioavailability of 91.8%. [3].Its mean elimination half-life is approximately 12 hours under steady-state conditions [4].Moxifloxacin shows linear pharmacokinetics after single doses ranging from 50 to 800 mg [5] and its bioavailability is not affected by the concomitant intake of food [6].The reference tablet formulation (Avelox®, Bayer de México, S.A. de C.V, Mexico City, Mexico) is marketed in Mexico. Moxifloxacin is well absorbed following oral administration with an absolute bioavailability of 91.8%. Moxifloxacin shows linear pharmacokinetics after single doses ranging from 50 to 800 mg [5] and its bioavailability is not affected by the concomitant intake of food [6]. The reference tablet formulation (Avelox®, Bayer de México, S.A. de C.V, Mexico City, Mexico) is marketed in Mexico. Itwas selected as the reference formulation because it is included in the list of Drug Reference Medications issued by the Mexican Federal Commission for the Protection against Sanitary Risks (COFEPRIS). It is important to point out that the reference medications (formulations) are indicated in a list that is mandatory for bioequivalence studies performed in Mexico
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