Formulation And Invitro Characterization Of Macitentan Solid Dispersion By Hot Melt Extrusion Technique

Abstract

Macitentan is indicated for the treatment of WHO group 1 pulmonary arterial hypertension (PAH) both alone and in combination with tadalafil. It is an BCS class-III drug having higher half-life. To improve the biological performance of Macitentan solid dispersion was formulated by using Soluplus, PEG 4000 and Mannitol. Solid dispersions of Macitentan were prepared with different carriers in differentratios of drug and carrier(1:1,1:2, 1:3 and 1:4). Results of prepared solid dispersions of Macitentan by hot melt extrusion method were discussed which includes solubility, melting point determination, drug content uniformity, and invitro dissolutionstudies. Characterization in solid state was done by various analytical techniques such as FT-IRstudies .Finally by comparing all the formulations, formulation (F12) containing Macitentan + Mannitol (1:4) shows better results by solvent evaporation method at the end of 60 min with maximum drug release of 98.35±1.49%, hence it was selected as the best formulation. The optimized formulation follows First order release kinetics