Bioequivalence and Safety of Bilastine 20 mg Orodispersible Tablets and Conventional Tablets: A Randomized, Single-Dose, Two-Period Crossover Study in Healthy Volunteers Under Fasting Conditions

Drugs R D. 2024 Sep;24(3):405-414. doi: 10.1007/s40268-024-00480-8. Epub 2024 Aug 1.

Abstract

Background and objective: Orodispersible tablets (ODT) rapidly dissolve in the oral cavity and can improve patient's convenience. This pharmacokinetic study assessed the bioequivalence of a novel 20 mg ODT formulation of bilastine compared with bilastine 20 mg tablets in healthy volunteers under fasting conditions.

Methods: A phase I, single-center, open-label, two-period, two-sequence crossover randomized clinical trial was conducted. The study comprised two periods, in which participants were administered a single oral dose of bilastine 20 mg in the form of ODT as the test product, or conventional tablets as the reference product, and a washout of 7 days between each period. Blood samples were collected for up to 72 h. Bioequivalence was established if the 90% confidence intervals of the Cmax and AUC0-t were within the acceptance range (80-125%). Safety was evaluated at the follow-up visit (days 4-7 after the second dose) and throughout the study.

Results: A total of 42 healthy volunteers were randomized, and 41 completed the study. Pharmacokinetic parameters were comparable for both formulations after a single dose of 20 mg. Bilastine ODT and conventional tablets were bioequivalent as the 90% confidence intervals of the test over reference ratios were within the predefined range (80-125%). Both formulations were well tolerated and showed a similar safety profile.

Conclusions: Bilastine ODT was bioequivalent to the reference treatment formulated as conventional tablets when administered as a single oral dose of 20 mg under fasting conditions. Both formulations showed a similar tolerability and safety profile, with no serious adverse events or significant analytical alterations reported.

Trial registration: 2019-004071-39. Date of authorization: 10 December 2019.

Publication types

  • Randomized Controlled Trial
  • Clinical Trial, Phase I

MeSH terms

  • Administration, Oral
  • Adult
  • Area Under Curve
  • Benzimidazoles / administration & dosage
  • Benzimidazoles / adverse effects
  • Benzimidazoles / pharmacokinetics
  • Cross-Over Studies*
  • Fasting*
  • Female
  • Healthy Volunteers*
  • Humans
  • Male
  • Middle Aged
  • Piperidines / administration & dosage
  • Piperidines / adverse effects
  • Piperidines / pharmacokinetics
  • Tablets*
  • Therapeutic Equivalency*
  • Young Adult

Substances

  • Tablets
  • bilastine
  • Benzimidazoles
  • Piperidines