Solubility and Dissolution Enhancement of Poorly Soluble Drug Apixaban by Solid Dispersion
Abstract
Apixaban is an anticoagulant used for the prophylaxis of stroke and systemic embolism in nonvalvular atrial fibrillation, and deep vein thrombosis (DVT) leading to pulmonary embolism (PE), including in patients after a hip or knee replacement surgery. Apixaban has low water solubility, but more soluble in organic solvents like dimethyl sulfoxide (DMSO) and dimethylformamide. Various formulation strategies, such as solid dispersions and cocrystals, are being explored to enhance its solubility and bioavailability. Present work is primarily focused on the development of solid dispersions of apixaban through solvent evaporation technique utilizing a blend of lactose and MCC as a carrier. The dissolution test results showed that the increasing amount of lactose gave a significantly higher percentage of drug release profile. The present study introduced a new APX SD that potentially exhibits better solubility and permeability, thus increasing APX’s bioavailability.
Keywords: Solid dispersion; Apixaban; lactose; MCC; Solvent evaporation; Solubility; Dissolution; Bioavailability
Keywords:
Solid dispersion, Apixaban, lactose, MCC, Solvent evaporation, Solubility, Dissolution, BioavailabilityDOI
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