| Research Article |
Open Access |
|
| Bioequivalence of Two Oral Fluconazole Formulations
in Healthy Subjects: a Single Dose, Open-Label,
Randomized, Two-Period Crossover Study |
| Jose Antonio Palma-Aguirre1*, Mireya Lopez-Gamboa1, Teresita
de Jesus Castro-Sandoval1, Roxana Hernández-González1, Julian Mejía-Callejas1,
María de los Angeles Melchor-Baltazar1, Juan Salvador Canales-Gomez2 |
| 1Centro de Estudios Científicos y Clínicos Pharma, SA de CV, Mexico City, Mexico |
| 2Productos Medix, SA de CV Mexico City, Mexico |
| *Corresponding author: |
Jose Antonio Palma-Aguirre, Amores 320,
Col . Del Valle, 03100 Mexico City, Mexico,
E-mail: jpalma@cecycpharma.com |
|
| |
| Received December 17, 2009; Accepted February 04, 2010; Published February 05, 2010 |
| |
| Citation: Palma-Aguirre JA, Mireya LG, de Jesus CST, Hernández-
González R, Mejía-Callejas J, et al. (2010) Bioavailability of Two Oral
Tablet Formulations of citalopram 20 mg: Single-Dose, Open-Label,
Randomized, Two-Period Crossover Comparison in Healthy Mexican
Adult Subjects. J Bioequiv Availab 2: 023-027. doi: 10.4172/jbb.1000026 |
| |
| Copyright: © 2010 Palma-Aguirre JA, et al. This is an open-access
article distributed under the terms of the Creative Commons Attribution
License, which permits unrestricted use, distribution, and reproduction
in any medium, provided the original author and source are credited. |
| |
| Abstract |
| |
| Background |
| Fluconazole is a triazole antifungal agent
labeled for use in the treatment of oropharyngeal and esophageal
candidiasis and cryptococcal meningitis, marketed
in Mexico in several generic trade names. |
| |
| Objective |
| The aim of this study was to compare the
bioavailability and determine the bioequivalence of one test
formulation (fluconazole oral tablet) with its corresponding
list reference-drug formulation in Mexico (a list issued
by Mexican Health Authorities). |
| |
| Methods |
| A single dose, randomized, open-label, 2-period
crossover, postmarketing study was conducted. Eligible
subjects was selected comprising healthy Mexican
adults of either sex, and subjects were randomly assigned
to receive 1 test formulation of fluconazole followed by
the corresponding reference drug formulation, or viceversa,
with a 1-week washout period between doses. After a 12-
hour (overnight) fast, subjects received a single capsule of
fluconazole 150 mg tablet formulation. For the analysis of
bioequivalence, including Cmax, AUC from time 0 (baseline)
to time t (AUC0-t), and AUC from baseline to infinity
(AUC0-∞), blood samples were collected at baseline, 0.5,
1, 1.5, 2, 2.5, 3, 3.5, 4, 6, 8, 12, 24, 48, 72 and 96 hours after
dosing. The formulation was considered bioequivalent if
the geometric mean ratios (test/reference) of the Cmax and
AUC were within the predetermined range of 80% to
125%. Tolerability was determined by clinical assessment,
monitoring vital signs, laboratory analysis results, and subject
interviews regarding adverse events. |
| |
| Results |
| A total of 24 subjects were enrolled in the study
The bioequivalence test drug values were Cmax of 4.44 ±
0.79 μg/mL, tmax of 2.59 ± 1.03 h, AUC0-t of 152.21 ± 28.89
h. μg/mL, AUC0-∞ of 175.13 ± 48.98 h. μg/mL, and reference
drug values of Cmax of 4.38 ± 0.83 μg/mL, tmax of 2.70
± 1.15 h, AUC0-t of 154.67 ± 26.10 r. μg/mL, AUC0-∞ of
174.33 ± 31.10 hr. μg/mL. |
| |
| Conclusions |
| In this study in healthy Mexican adult subjects,
a single dose of fluconazole 150 mg of the test formulation
was found to be bioequivalent to the corresponding
reference formulation according to the regulatory definition
of bioequivalence based on the rate and extent of
absorption. Both formulations were generally well tolerated. |
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