Sex-by-formulation interaction assessed through a bioequivalence study of efavirenz tablets

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Título

Sex-by-formulation interaction assessed through a bioequivalence study of efavirenz tablets

Tema

BIOEQUIVALENCIA
EVAVIRENZ
BIBLIOGRAFIA NACIONAL QUIMICA
2016

Abstract

Although sex-related differences in gastrointestinal physiology have been vastly reported, its impact on drug oral
bioavailability and bioequivalence (product discrimination) is often ignored. On this work results from an
average bioequivalence study between tablets containing 600 mg of the antiretroviral efavirenz (EFV), carried
out with 14 healthy subjects (8 female and 6 men) in a randomized 2-period, 2-treatment crossover design,
are analyzed from a sex-based approach. Sequences were balanced within each sex group. Considering all
subjects, no differences were observed on EFV absorbed amount, as shown by the estimated 90CI of the AUC96
Test/Reference bioequivalence ratio (T/R): 0.950–1.05. However, results were not conclusive due to the 90CI
for CMAX T/R was 0.743–1.07. Over this parameter, a significant sex-by-formulation interaction was detected:
90CI CMAX T/R was 0.838–1.36 in women and 0.540–0.920 in men; with a 52% relative difference between
point estimates. Formulation differences were therefore evidenced only by male subjects. In vitro dissolution
and disintegration tests for both products were carried out in two aqueous media: A) SLS 0.25% and B) HCl/KCl
pH 1.2. T/R results for dissolution efficiency and tablet disintegration times of formulations in both A and B
media were highly correlated with CMAX T/R bioequivalence results observed in women and men respectively,
showing that a dissimilar gastrointestinal environment between sexes affected EFV oral absorption. This work
shows how sex-by-formulation interaction can affect bioequivalence conclusions. Sex effect on product discrimination
should be specially disclosed in bioequivalence studies, mainly for drugs aimed to be given to both sexes.

Autor

Ibarra, Manuel
Magallanes, Laura
Lorier, Marianela
Vázquez, Marta

Fuente

European Journal of Pharmaceutical Sciencesv. 85, 2016. -- p. 106-111

Editor

Elsevier

Fecha

2016

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PDF

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Tipo

Artículo

Identificador

http://dx.doi.org/10.1016/j.ejps.2016.02.001

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Original Format

PDF
Fecha de agregación
May 6, 2016
Colección
Bibliografía Nacional Química
Tipo de Elemento
Document
Etiquetas
,
Citación
Ibarra, Manuel, “Sex-by-formulation interaction assessed through a bioequivalence study of efavirenz tablets,” RIQUIM - Repositorio Institucional de la Facultad de Química - UdelaR, accessed December 13, 2019, http://riquim.fq.edu.uy/items/show/3961.
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