FORMULATION AND INVITRO CHARACTERIZATION OF MACITENTAN SOLID DISPERSION TO FAST DISINTEGRATING TABLETS

Abstract

Macitentan is an endothelin receptor antagonist utilized for the management of pulmonary arterial hypertension to impede disease development.It is a BCS Class II medication. To enhance the biological efficacy of Macitentan, a solid dispersion was formed into an oral disintegrating tablet utilizing PEG 6000, Xylitol, and PVP K30. Solid dispersions of Macitentan were created using several carriers in distinct ratios of drug to carrier (1:1, 1:2, 1:3, and 1:4). The outcomes of the generated solid dispersions of Macitentan using the solvent evaporation method were examined, including solubility, melting point determination, drug content uniformity, and in vitro dissolution investigations.Characterization in the solid state was conducted using several analytical methods, including FT-IR investigations.Ultimately, while evaluating all formulations, formulation (F12) including Macitentan and PVP K30 in a 1:4 ratio demonstrated superior outcomes using the solvent evaporation technique after 60 minutes, achieving maximal drug release; hence, it was designated as the optimal formulation.Fast dissolving tablets were produced from the optimal formulation utilizing several disintegrants at varied concentrations.The pre-compression and post-compression parameters were analyzed, and the findings were presented. All findings fall within permissible limits.The in vitro drug release of the prepared tablets was conducted using a 6.8 pH phosphate buffer. The F12T12 formulation with 50mg of Cropovidone exhibits a drug release of 99.74±1.48% within 20 minutes. The improved formulation adheres to first-order release kinetics.