Bioequivalence studies for two different strengths of montelukast in healthy volunteers: 10 mg film-coated tablets and 5 mg chewable tablets

Drug Res (Stuttg). 2013 Sep;63(9):477-83. doi: 10.1055/s-0033-1347235. Epub 2013 Jun 18.


In order to assess the bioequivalence of 2 different formulations of montelukast, a pivotal trial for the montelukast 10 mg film-coated tablets formulation and a pivotal trial for the montelukast 5 mg chewable tablets formulation were conducted.For the 10 mg study, 34 healthy subjects were enrolled in a single centre, randomised, single-dose, open-label, 2-way crossover study, with a minimum washout period of 7 days, while for the 5 mg study, 42 healthy subjects were included in another study with a similar design. For both studies, plasma samples were collected up to 24 h post-dosing and drug levels were determined by reverse liquid chromatography and detected by tandem mass spectrometry detection.Pharmacokinetic parameters used for bioequivalence assessment, area under the concentration-time curve from time zero to time of last non-zero concentration (AUC0-t) and from time zero to infinity (AUC0-inf) and maximum observed concentration (Cmax), were determined from the drug concentration data using non-compartmental analysis.In the 10 mg study, the 90% confidence intervals obtained by analysis of variance were 99.62-120.51% for Cmax, 102.25-117.37% for AUC0-t and 101.96-116.67% for AUC0-inf, which were within the predefined acceptable range of 80.00-125.00%.In the 5 mg study, the 90% confidence intervals were 91.14-98.46% for Cmax, 93.02-98.42% for AUC0-t and 93.09-98.63% for AUC0-inf, which were within the predefined acceptable range of 80.00-125.00%.Bioequivalence between formulations was concluded both in terms of rate and extent of absorption for both strengths.

Publication types

  • Randomized Controlled Trial

MeSH terms

  • Acetates / administration & dosage
  • Acetates / adverse effects
  • Acetates / pharmacokinetics*
  • Adult
  • Cross-Over Studies
  • Cyclopropanes
  • Female
  • Humans
  • Leukotriene Antagonists / pharmacokinetics*
  • Male
  • Middle Aged
  • Quinolines / administration & dosage
  • Quinolines / adverse effects
  • Quinolines / pharmacokinetics*
  • Sulfides
  • Tablets
  • Therapeutic Equivalency


  • Acetates
  • Cyclopropanes
  • Leukotriene Antagonists
  • Quinolines
  • Sulfides
  • Tablets
  • montelukast