The Development of Floating Multiple Unit Mini Tablets of Bosentan Using QbD: Characterisation and Pharmacokinetic Study

Abstract

Background: In order to achieve steady state concentration multiple dosing is required for bosentan. Hence formulating bosentan controlled release formulation could be an approach to solve this issue. Objective: The objective is to develop floating multiple unit minitablets of bosentan using Quality by design approach. Methods: Failure mode effect analysis (FMEA) and Taguchi design are employed in order to screen highly critical factors. Box-Behnken design (BBD) was adopted for the process of optimization. Results: The quantity of gelucire 39/01, HPMC K15 M, and sodium bicarbonate was found to be one of the significant factors using Taguchi design. The Box-Behnken design results in the optimised formulation showing floating lag time within 3 min, floating time of nearly 15 h, time to release 50% of drug of 3.6 h, time to release 90% of drug of 11h and better bioavailability compared to pure drug. Conclusion: It can be concluded that floating multiple unit minitablet can be used as an encouraging approach for sustaining the drug release of bosentan.