Abstract
Two studies were conducted in order to assess the bioequivalence of montelukast (CAS
151767-02-1) 10 mg film-coated tablet (FCT) and 5 mg chewable tablet (CT) test formulations
in comparison with the original brands. Under fasting conditions, healthy male and
female volunteers received one 10 mg FCT or 5 mg CT orally as a single dose of a test
or reference formulation. Both studies were designed as open-label, randomized, two-period,
two-sequence, crossover studies with a 7-day washout interval. Plasma samples were
collected up to 24 h after drug administration and montelukast levels were determined
by a validated LC/MS/MS method. Pharmacokinetic parameters were calculated using non-compartmental
analysis and were statistically compared by analysis of variance for test and reference
formulation. Bioequivalence between products was determined by calculating 90% confidence
interval of the ratio test/reference of least-square means of logarithmically transformed
Cmax
and AUC0–t parameters. AUC0–∞ was also analysed to obtain additional information. The calculated 90% confidence
intervals for the ratios of Cmax and AUC0–t parameters were 89.33–110.52 and 92.06–109.46, respectively, in the FCT study, and
91.58–101.86 and 92.15–98.83, respectively, in the CT study, which are all within
the bioequivalence acceptance range of 80–125%. Based on the results, it can be concluded
that the evaluated test FCT and CT formulations are bioequivalent to their respective
reference formulation in terms of rate and extent of absorption.
Key words
Bioequivalence - CAS 151767-02-1 - Healthy volunteers - Montelukast - Pharmacokinetics
- Tablet
