Review article: dual delayed release formulation of dexlansoprazole MR, a novel approach to overcome the limitations of conventional single release proton pump inhibitor therapy

• Published in: Alimentary pharmacology & therapeutics Vol. 29; no. 9; pp. 928 - 937
• Main Authors: METZ, D. C., VAKILY, M., DIXIT, T., MULFORD, D.
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Publishing Ltd 01-05-2009; Blackwell
• Subjects: 2-Pyridinylmethylsulfinylbenzimidazoles - pharmacology; 2-Pyridinylmethylsulfinylbenzimidazoles - therapeutic use; Anti-Ulcer Agents - pharmacokinetics; Anti-Ulcer Agents - pharmacology; Anti-Ulcer Agents - therapeutic use; Biological and medical sciences; Cross-Over Studies; Delayed-Action Preparations - administration & dosage; Delayed-Action Preparations - pharmacokinetics; Delayed-Action Preparations - pharmacology; Dexlansoprazole; Digestive system; Gastroenterology. Liver. Pancreas. Abdomen; Humans; Lansoprazole; Medical sciences; Pharmacology. Drug treatments; Proton Pump Inhibitors - administration & dosage; Proton Pump Inhibitors - pharmacokinetics; Proton Pump Inhibitors - pharmacology; Randomized Controlled Trials as Topic; Dexlansoprazole; Treatment; Benzimidazole derivatives; Controlled release form; Formulation; Dosage form; Antiulcer agent; Review; Release; Bibliographic review; Proton pump inhibitor
• ISSN: 0269-2813; 1365-2036
• DOI: 10.1111/j.1365-2036.2009.03984.x

Summary
Background  Proton pump inhibitors (PPIs) provide the most effective pharmacotherapy for treating acid‐related disorders. However, PPIs do not completely control acid over 24 h with once‐daily dosing.
Aims  To discuss limitations inherent in the pharmacokinetics (PK) and pharmacodynamics of conventional PPI formulations, which provide a single drug release. Also, to consider approaches to extending the duration of acid suppression focusing on dexlansoprazole MR, a PPI with a novel Dual Delayed Release (DDR) formulation.
Method  We reviewed the available literature regarding marketed and investigational PPIs.
Results  Non‐standard dosing of currently marketed PPIs has produced incremental advances in acid control. Multiple approaches are being evaluated to enhance acid suppression with PPIs. Dexlansoprazole MR is a DDR formulation of dexlansoprazole, an enantiomer of lansoprazole, with two distinct drug release periods to prolong the plasma dexlansoprazole concentration–time profile and extend duration of acid suppression. Clinical studies show that dexlansoprazole MR produces a dual‐peak PK profile that maintains therapeutic plasma drug concentrations longer than lansoprazole, with a single‐peak PK profile, and increases the percentage of time that intragastric pH >4.
Conclusions  Novel drug delivery platforms, including the dexlansoprazole MR DDR formulation, may improve acid suppression and offer benefits over conventional single release PPI formulations.