APPLICATION OF SOME NOVEL TECHNIQUES FOR SOLUBILITY ENHANCEMENT OF MEFENAMIC ACID, A POORLY WATER SOLUBLE DRUG

Abstract

Mefenamic acid (MFA), a potent non-steroidal anti-inflammatory drug (NSAID), has a low oral bioavailability due to poor aqueous solubility and insufficient dissolution. In order to improve the same, various techniques were employed viz., evaporative precipitation into aqueous solution (EPAS), spherical agglomeration (SA) and solid dispersion using solvent evaporation and melt mixing. The formulations were characterised by differential scanning calorimetry (DSC) and X-Ray powder diffractometry (XRD) and were investigated for drug content studies, solubility studies, in vitro study and in vivo evaluation of anti-inflammatory activity. The formulations of MFA prepared by spherical agglomeration technique have satisfactory good drug content and the formulations with SLS and HPMC show a significant increase in solubility in case of SA technique. In case of solid dispersion, all carriers show improvement in the dissolution rate of the drug The DSC studies show no change in the polymorphism in most of the formulations The XRD studies of the formulations show no change in their crystalline form. The formulation containing HPMC & SLS as drug carrier show better anti-inflammatory effect with comparison to pure drug confirming the improved bioavailability of this drug.