Influence of eutectic mixture as a multi-component system in the improvement of physicomechanical and pharmacokinetic properties of diacerein

Abstract

A multi-component system of diacerein (DIA) with 2, 4 – dihydroxybenzoic acid (DHA) as coformer at various molar compositions was formulated to simultaneously improve solubility, compressibility and bioavailability of DIA by applying acetone assistant grinding technique. Various evaluation parameters pertaining to measure physicomechanical properties were conducted. Thermal analysis revealed a ‘V’- shaped binary phase diagram along with single melting event as a possibility of eutectic formation between drug and coformer. It was further confirmed PXRD and FT-IR. Equidimensional shape with platy nature of eutectic material was observed in SEM images imparting its better flow and compressibility. Solubility and dissolution study showed 2 and 1.8 folds enhancement respectively compared to pure DIA and control batch. Pharmacokinetic study proved 2.1 times higher bioavailability in case of prepared eutectic compared to DIA along with its stable nature. Hence, the multi-component system can become a potential way for the improvement of material characteristics.