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




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Clinical and Translational Allergy

, 5:37

First Online: 11 November 2015Received: 23 July 2015Accepted: 16 October 2015

Abstract

BackgroundMontelukast 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.

ObjectiveThe 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.

MethodsAn 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.

ResultsThe 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.

ConclusionBroncast 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.

KeywordsMontelukast Bioequivalence Immediate release Safety Efficacy  Download fulltext PDF



Author: Abdel Naser Zaid - Ayman Mousa - Nadia Ghazal - Rana Bustami

Source: https://link.springer.com/



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