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

摘要

What is already known about this subject Systemic esomeprazole exposure is decreased when administered simultaneously with food. What this study adds Taking esomeprazole within 15 min of eating a high-fat, high-calorie meal results in reduced systemic drug exposure. 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.