Quality by Design Formulation Approach for the Development of Orodispersible Tablets of Dexlansoprazole.

Abstract

<h4>Purpose</h4>Dexlansoprazole (DX) is a commercially available proton pump inhibitor (PPI). It is an oral delayed-release (DR) formulation that takes 1-2 h to reach the systemic circulation. To overcome the delayed onset of action of conventional formulation and patient inconvenience, orodispersible tablets (ODTs) have been formulated. Drug delivery systems, especially in elderly and frequent travelers, are limited by conventional dosage forms, and ODTs are an ideal dosage form for the fast onset of action and ease of administration for these patients and are more convenient than conventional tablets for patient compliance.<h4>Methods</h4>The formulation was optimized via Design Expert^® software (version 13.0) and evaluated for in vitro and in vivo attributes. The ODTs were compressed by the most convenient method of compression, that is, direct compression, the formulation contains a combination of citric acid and sodium bicarbonate along with Kyron T-314^® (polymer). Pre- and post-compression evaluations were performed, and a comparative pharmacokinetic study of the DX ODT was carried out in human volunteers.<h4>Results</h4>Drug plasma concentrations were analyzed at different time intervals through high-performance liquid chromatography (HPLC). PK Summit <b>^®</b> software was used to calculate various pharmacokinetic parameters. The pharmacokinetic results revealed that the T_max of 0.4 h was significantly lower than that of conventional DX, indicating rapid onset of action. Stability studies indicated that the formulation was stable under both intermediate and accelerated conditions.<h4>Conclusion</h4>The ODTs exhibited good physical characteristics, with a pleasant taste and disintegrated rapidly in the saliva due to the addition of a superdisintegrant and an effervescent pair. Pharmacokinetics revealed a rapid therapeutic effect with good C_max. Furthermore, this formulation is cost-effective in terms of fewer manufacturing steps and a lower cost for excipients, along with a good stability profile.