Effect of timing of dosing in relation to food intake on the pharmacokinetics of esomeprazole.
OBJECTIVE
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.
Sostek
Mark B
MB
AstraZeneca LP, Wilmington, DE, USA. mark.sostek@astrazeneca.com
Chen
Yusong
Y
Andersson
Tommy
T
D000328:Adult; D000897:Anti-Ulcer Agents / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D019540:Area Under Curve; D001682:Biological Availability; D018592:Cross-Over Studies; D004334:Drug Administration Schedule; D004435:Eating; D064098:Esomeprazole / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D005215:Fasting; D005260:Female; D018565:Food-Drug Interactions; D006801:Humans; D008297:Male; D008875:Middle Aged
D000897:Anti-Ulcer Agents; D064098:Esomeprazole