Background: Multiple dosing is required for bosentan in order to achieve steady-state
concentration. 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 the 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.