Effect of timing of dosing in relation to food intake on the pharmacokinetics of esomeprazole

Br J Clin Pharmacol. 2007 Sep;64(3):386-90. doi: 10.1111/j.1365-2125.2007.02889.x. Epub 2007 Apr 10.

Abstract

Aim: To investigate the pharmacokinetics of esomeprazole before a high-fat meal vs. fasting.

Methods: This open-label, randomized, crossover study consisted of two 5-day dosing periods of esomeprazole 40 mg per day. On days 1 and 5, subjects received esomeprazole 15 min before a high-fat meal (fed) or 4 h before a non-high-fat meal (fasting).

Results: On days 1 and 5, ratio of fed to fasting area under the plasma concentration-time curve [0.56, 90% confidence interval (CI) 0.50, 0.64, and 0.78, 90% CI 0.74, 0.82, respectively] and peak plasma concentration (0.34, 90% CI 0.28, 0.41, and 0.47, 90% CI 0.41, 0.52, respectively) were outside of the limits of bioequivalence.

Conclusions: Esomeprazole bioavailability was reduced when taken within 15 min before eating a high-fat meal vs. that while fasting.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Anti-Ulcer Agents / administration & dosage
  • Anti-Ulcer Agents / blood
  • Anti-Ulcer Agents / pharmacokinetics*
  • Area Under Curve
  • Biological Availability
  • Cross-Over Studies
  • Drug Administration Schedule
  • Eating*
  • Esomeprazole / administration & dosage
  • Esomeprazole / blood
  • Esomeprazole / pharmacokinetics*
  • Fasting
  • Female
  • Food-Drug Interactions
  • Humans
  • Male
  • Middle Aged

Substances

  • Anti-Ulcer Agents
  • Esomeprazole