Development and Evaluation of Artemether-Aeroperl® 300 Pharma Granular Solid Dispersion Powder with Enhanced Solubility, Dissolution Rate and Physicochemical Characterisation

The objective was to enhance the solubility and dissolution rate of Artemether poorly water soluble antimalarial, by the preparation of solid dispersion (SD) granules. The dispersion granules were prepared using a hot melt granulation technique which involved the preparation of a homogenous dispersion of ARTM in surfactant melt, followed by its adsorption onto the surface of AEROPERL® 300 Pharma, an inert absorbent using the solvent evaporation method. The dispersion granules were characterized for their in-vitro dissolution rate, moisture content and flow properties. The formulation was further characterized by FTIR,DSC, XRD and SEM analysis. FTIR spectrum revealed some drug excipient interactions. DSC and XRD data indicated the retention of amorphous form of ARTM. SEM confirmed the homogeneity and surface adsorption of the ARTM-Lutrol F127 or ARTM-Lutrol F68 melt on AEROPERL® 300 Pharma leading to an enhanced surface area and thus the dissolution rate. The optimized dispersion granules were filled inside the capsules and evaluated. The in-vitro dissolution rate of these capsules was significantly better in comparison with pure drug. Physical characterisation enabled us to understand the effects of formulation variables on the dispersion granules of ARTM.