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Bioavailability of Two Oral-Suspension Formulations of a Single Dose of Nitazoxanide 500 mg: An Open-Label, Randomized-Sequence, Two-Period Crossover, Comparison in Healthy Fasted Mexican Adult Volunteers

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Author(s): Mario González-de la Parra | Juana Isabel Balderas-Acata | Esteban Patricio Ríos-Rogríguez Bueno1, | Fabiola Pérez-Becerril | Clara Espinosa-Martínez | Victoria Burke- Fraga

Journal: Journal of Bioequivalence & Bioavailability
ISSN 0975-0851

Volume: 3;
Issue: 3;
Start page: 043;
Date: 2011;
Original page

Keywords: Nitazoxanide | Tizoxanide | Bioequivalence | Bioavailability | Pharmacokinetics | HPLC | Mexican population

ABSTRACT
Nitazoxanide is an oral broad-spectrum parasiticidal agent. In Mexico, the oral powder for suspension ofnitazoxanide is indicated for the treatment of antiprotozoal and anthelmintic infections in patients of 1 year or older.The aims of this study were to compare the bioavailability and to determine the bioequivalence of a test andreference formulation of oral nitazoxanide 500 mg, administered as a suspension, and to generate data regardingthe oral bioavailability of this drug on the Mexican population.This single-dose, randomized-sequence, open-label, 2-period crossover study was conducted on a total of 26Mexican adult subjects of both genders, with a 1-week washout period. Study formulations were administered aftera 10-hour overnight fast. For pharmacokinetic analysis, blood samples were drawn at 0 (baseline), 0.5, 1, 1.5, 2,2.5, 3, 4, 5, 6, 7, 8, 9, 10 and 12 hours after administration. Plasma concentrations of tizoxanide (active metaboliteof nitazoxanide) were determined using HPLC coupled to a mass spectrometry (MS/MS). The test and referenceformulations were to be considered bioequivalent if the 90% CIs for the geometric mean test/reference ratios werewithin a predetermined range of 80% to 125%.The estimated pharmacokinetic parameters of tizoxanide for the reference (Daxon®) and test (Paramix®)formulations were: Cmax (10.40±2.99 μg/ml, 10.73 ± 3.45 μg/ml); AUC0–t (39.57 ± 15.89 μg•h /ml, 43.31 ± 19.13 μg•h /ml); and AUC0–∞ (40.93 ± 16.05 μg•h /ml, 45.00 ± 19.63 μg•h /ml), respectively. The 90% CIs for the geometric meanratios of Cmax, AUC0–t, and AUC0–∞ were: 94.58%-110.21%, 100.43%-116.22%, and 101.00%-116.43%, respectively,the within-subject %CV values were 16.23, 15.49 and 15.05, respectively. All the power values were 100%. In thisstudy a single dose of the test formulation met the regulatory requirements to assume bioequivalence, based on therate and extent of absorption
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