FORMULATION AND IN VITRO EVALUATION OF SELEXIPAG CONTROLLED RELEASE TABLETS

Abstract

Selexipag has a short biological half-life of 0.8-2.5 hours and having less bioavailability which necessitates multiple daily dosing. Hence the present study was aimed to develop a controlled release formulation of Selexipag to reduce the dose related side effects and to reduce the dosage regimen. The present research project aimed to develop a Control release oral formulation of hypertension drug Selexipag, the present research comprising Selexipag used for the symptomatic relief of pulmonary arterial hypertension. Polymers like HPMC K15 M, Carbopol 940, Pectin and Gellan Gum were used for controlling the drug release, and the polymers are mixed in a predetermined ratio. Totally 12 formulations were prepared and evaluated for pre-compression and post-compression parameters, and all the results were found to be within the limits. From the drug and excipients compatibility studies (FT-IR) it was confirmed that the drug and excipients used weren’t have any interactions. The in vitro dissolution studies revealed that the F9 formulation containing 6mg of Pectin controls the drug release up to 12 hours. So Pectin containing F9 formulation was considered to be suitable for the formulation of Selexipag controlled release tablet and the drug release kinetics revealed that the F9 formulation shows zero order kinetics with super case- II transport mechanism.