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Clinical and Translational Allergy
Published in: Clinical and Translational Allergy 1/2015

Open Access 01-12-2015 | Research

Interchangeability and comparative effectiveness between generic and brand montelukast immediate release tablets after a single oral administration in healthy volunteers

Authors: Abdel Naser Zaid, Ayman Mousa, Nadia Ghazal, Rana Bustami

Published in: Clinical and Translational Allergy | Issue 1/2015

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Abstract

Background

Montelukast is a leukotriene receptor antagonist. The release of leukotrienes causes narrowing and constricting in the respiratory airways. Blocking the action of these leukotrienes, montelukast can be used for the prophylaxis and treatment of chronic asthma.

Objective

The aim of this study was to evaluate the interchangeability and comparative effectiveness between a generic and a brand montelukast 10 mg immediate release tablets (Broncast® and Singulair®, respectively) after a single oral dose among Arab Mediterranean volunteers.

Methods

An open-label, randomized two-period crossover bioequivalence design was conducted in 31 healthy male volunteers with a 1 week washout between each study period and under fasting conditions. The plasma drug concentration was assessed by using a previously validated LC MS/MS method. The ratio between the generic and brand of geometric least squares means was reported for both generic and brand products. Moreover, an in vitro dissolution study was conducted on generic and brand tablets using three different pH media, and similarity and non-similarity factors (f2 and f1) were calculated.

Results

The used bioanalytical method was found to be linear within the range 6.098–365.855 ng/mL. The correlation coefficient was close to 0.999 during the course of the study validation. Statistical comparison of the main pharmacokinetic parameters showed the inexistence of any significant difference between generic and the brand. The point estimates (ratios of geometric means) were 111.939, 111.711, and 112.169 % for AUC0–24, AUC0–∞, and Cmax, respectively. The 90 % confidence intervals (CIs) were within the pre-defined limits of 80.00–125.00 % as specified by the FDA and EMA for bioequivalence studies. F2 and f1 were higher than 50 and lower than 15, respectively in all selected pH media.

Conclusion

Broncast® immediate release film coated tablets (10 mg/tablet) are bioequivalent to Singulair® immediate release film coated tablets (10 mg/tablet), with a comparable safety and efficacy profile. This suggests that these two formulations can be clinically considered interchangeable. The dissolution study suggests that it could be used as premarketing quality control parameter in order to maintain the high quality of the produced product.
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Metadata
Title
Interchangeability and comparative effectiveness between generic and brand montelukast immediate release tablets after a single oral administration in healthy volunteers
Authors
Abdel Naser Zaid
Ayman Mousa
Nadia Ghazal
Rana Bustami
Publication date
01-12-2015
Publisher
BioMed Central
Published in
Clinical and Translational Allergy / Issue 1/2015
Electronic ISSN: 2045-7022
DOI
https://doi.org/10.1186/s13601-015-0081-8

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