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Bioavailability of a dexlansoprazole delayed-release orally disintegrating tablet: effects of food and mode of administration

Authors Kukulka M, Nudurupati S, Perez MC

Received 31 August 2016

Accepted for publication 11 December 2016

Published 17 February 2017 Volume 2017:10 Pages 47—56


Checked for plagiarism Yes

Review by Single-blind

Peer reviewers approved by Dr Amy Norman

Peer reviewer comments 2

Editor who approved publication: Professor Andreas M Kaiser

Michael Kukulka, Sai Nudurupati, Maria Claudia Perez

Takeda Development Center Americas, Inc., Deerfield, IL, USA

Background: Dexlansoprazole is a proton pump inhibitor (PPI) approved for use in dual delayed-release capsule and orally disintegrating tablet (ODT) formulations.
Aim: To assess effects of food, water, and route of administration on the bioavailability of dexlansoprazole 30-mg ODT.
Methods: Two separate open-label, phase 1, single-dose crossover studies were conducted in healthy adults. In study 1, pharmacokinetic parameters were analyzed in participants receiving dexlansoprazole ODT in a fed or fasted state with and without water. In study 2, the bioavailability of dexlansoprazole after administration via oral syringe or nasogastric (NG) tube, or after swallowing intact with water was compared to ODT administration in the fasted state, swallowed without water. Blood samples for determining dexlansoprazole plasma concentrations and pharmacokinetic parameter estimates were collected before and after dosing.
Results: Equivalent values for area under the plasma concentration–time curve (AUC) were observed in the fed and fasted states, but the maximum observed plasma concentration (Cmax) was 38% lower in the fed state; therefore, bioequivalence was not achieved. A water rinse following standard ODT administration decreased dexlansoprazole bioavailability, with lower Cmax and AUC values than when ODT was administered without a water rinse. Bioequivalence was demonstrated when comparing the alternative routes of administration, including via oral syringe or NG tube with standard ODT administration. Unlike with a water rinse, bioequivalence to standard ODT administration (i.e., without water) was demonstrated when swallowing the ODT intact with water. Rates of adverse events were comparable irrespective of administration route in the fasted state (6.7%–9.3%) and were 12% higher in the fed state than in the fasted state.
Conclusion: The AUC from the dexlansoprazole ODT was equivalent when administered in the fed and fasted states. Equivalent systemic exposure to dexlansoprazole was achieved regardless of the administration route.

Keywords: dexlansoprazole, bioavailability, proton pump inhibitor, orally disintegrating tablet, food effects, mode of administration

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