Bioequivalence study of two generic formulations of 10 mg montelukast tablets in healthy Thai male volunteers

Sripalakit, Pattana; Maphanta, Sirada; Saraphanchotiwitthaya, Aurasorn

doi:10.5414/cpp48628

Cited by 4 publications

(1 citation statement)

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“…Regarding the BE studies, several previous studies have tested the bioequivalence of new generic MT tablets or other dosage forms as granules and disintegrating tablets [ 20 – 23 ]. The PK values of our BE study were compared with similar studies that have been conducted on other populations [ 20 , 24 , 25 ]. It was interesting to find out that our PK values were in accordance with most of these values.…”

Section: Discussionmentioning

confidence: 99%

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

Zaid

Mousa²,

Ghazal³

et al. 2015

Clinical & Translational All

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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.

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Section: Discussionmentioning

confidence: 99%

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

Zaid

Mousa²,

Ghazal³

et al. 2015

Clinical & Translational All

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Pharmacokinetics and Bioequivalence of Two Formulations of Montelukast Sodium Tablets in Healthy Chinese Volunteers Under Fasting and Fed Conditions

Rao,

Wu,

et al. 2024

Clinical Pharm in Drug Dev

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Montelukast sodium is a leukotriene type 1 receptor antagonist that can be used for the prophylaxis and treatment of asthma. However, the pharmacokinetics of montelukast sodium tablets (10 mg) remain unclear in healthy Chinese subjects. Here, a single‐dose randomized, open‐label, 2‐sequence, and 2‐period crossover (7‐day washout period between treatments) study was performed to compare the pharmacokinetics and bioequivalence between the test products and the reference at a single dose of 10 mg among healthy Chinese subjects under fasting and fed conditions. Blood samples were collected at specified time points to analyze the plasma concentrations of montelukast by a validated liquid chromatography‐tandem mass spectrometry method. The results showed that the 90% confidence interval values of the geometric mean ratio of test/reference for the maximum plasma drug concentration, area under the concentration‐time curve from time 0 to the end, and area under the concentration‐time curve from time 0 to infinity were within the range of 80%‐125%. Moreover, both the test and reference formulations were safe and well tolerated, with no occurrence of severe adverse events. These results demonstrate that both the test montelukast sodium tablets and the reference showed similar bioequivalence, safety, and tolerability among healthy Chinese subjects under fasting and fed conditions.

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Montelukast, current indications and prospective future applications

Kittana

Hattab

Ziyadeh-Isleem

et al. 2016

Expert Review of Respiratory Medicine

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Clinical investigations on the pharmacotherapeutic effects of montelukast, in addition to in-vivo studies on animal models of non-respiratory diseases. The data discussed in this review were mainly obtained from clinical randomized trials, real-life studies, and studies based on animal models as approve of concept. As a condition, all of the discussed articles were published in journals cited by Pubmed. Expert commentary: The current clinical data are in favor of montelukast use in the management of chronic asthma as an add-on or alternative therapy to the inhaled corticosteroids. Further clinical trials are required to confirm the effectiveness and feasibility of montelukast for the treatment of conditions other than the current clinical indications.

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Bioequivalence study of two generic formulations of 10 mg montelukast tablets in healthy Thai male volunteers

Cited by 4 publications

References 0 publications

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

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

Pharmacokinetics and Bioequivalence of Two Formulations of Montelukast Sodium Tablets in Healthy Chinese Volunteers Under Fasting and Fed Conditions

Montelukast, current indications and prospective future applications

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