Bioequivalence study of eltrombopag 75 mg film-coated tablets under fasting conditions during the Covid-19 pandemic in healthy Caucasian male subjects

BMC Pharmacol Toxicol. 2024 Oct 23;25(1):80. doi: 10.1186/s40360-024-00803-0.

Abstract

This study aims to determine the bioequivalence of the reference preparation and the test preparation containing eltrombopag when both were given during the COVID-19 pandemic while fasting. Participants in the research were healthy male Caucasian subjects. One film-coated tablet of the test preparation or one film tablet of the reference preparation, equivalent to 75 mg of eltrombopag, was given to the participants in a randomized order throughout each treatment session. At pre determined blood sampling points, blood samples were taken to determine the pharmacokinetics of eltrombopag. Eltrombopag concentrations in the samples were determined using an LC-MS/MS technique verified using ESI(-). The study results were used to calculate the rate (the maximum plasma concentration, or Cmax) and extent (area under the concentration-time curve of plasma, or AUC(0-72) and AUC(0-t) of eltrombopag absorption from the test preparation and reference preparation. The 90% confidence intervals (CI) of the ln-transformed AUC(0-72), AUC(0-t), and Cmax of eltrombopag met the bioequivalence requirements of 80.00-125.00%. Both trial preparations had a similar and very satisfactory safety profile.

Keywords: Bioavailability; Bioequivalence study; Eltrombopag; Pharmacokinetic.

Publication types

  • Equivalence Trial
  • Randomized Controlled Trial

MeSH terms

  • Adult
  • Area Under Curve
  • Benzoates* / administration & dosage
  • Benzoates* / blood
  • Benzoates* / pharmacokinetics
  • COVID-19
  • COVID-19 Drug Treatment
  • Cross-Over Studies
  • Fasting*
  • Healthy Volunteers
  • Humans
  • Hydrazines* / administration & dosage
  • Hydrazines* / blood
  • Hydrazines* / pharmacokinetics
  • Male
  • Pyrazoles* / administration & dosage
  • Pyrazoles* / blood
  • Pyrazoles* / pharmacokinetics
  • Tablets* / pharmacokinetics
  • Tandem Mass Spectrometry / methods
  • Therapeutic Equivalency*
  • White People
  • Young Adult

Substances

  • Benzoates
  • eltrombopag
  • Hydrazines
  • Pyrazoles
  • Tablets