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.