Solubility and Bioavailability Enhancement of Poorly Water Soluble Drugs by Using Different Methods

Abstract

The objective of the present research work was to enhance the solubility and dissolution performance of poorly water-soluble antidiabetic drugs. Screening of effective solubility enhancement polymers to prepare amorphous solid dispersions with improved performance. In the present study, binary and ternary solid dispersions (SDs) were developed using different water-soluble polymers and evaluated. Ternary dispersions showing best solubility as well as dissolution were formulated as tablets. newlineMethod: newlineThe binary and ternary solid dispersions were prepared by solvent co-evaporation method using various polymers like Soluplus, and#946;-cyclodextrin, Hydroxypropyl and#946;-cyclodextrin, Kolliphor P188, Affinisol, Lutrol F127, Lutrol F68, Meglumine, Sylloid 244 FP, Gelucire 48/16, Polaxamer 407, and Eudragit EPO etc. in the different combinations. The solid dispersions were characterized by FTIR, DSC, and PXRD. For the screening of the polymers saturation solubility study was performed. Amorphous solid dispersions showing good saturation solubility were studied for the dissolution performance. Ternary solid dispersions showing best solubility as well as dissolution were formulated as tablets and compared with marketed formulation. newlineResult: newlineCanagliflozin Solid Dispersions newlineCanagliflozin (CNF) is the newest sodium /glucose cotransporters 2 (SGLT2) inhibitor used for management of type II diabetes mellitus having poor aqueous solubility. As very few tablet formulations are available in the market, this study aimed to develop an alternative, cost-effective formulation of CNF with enhanced solubility and dissolution profile. For this purpose, binary (F1-F17) and ternary (F18- F25) solid dispersions of CNF were formulated using polymers such as Soluplus, and#946;-cyclodextrin, Hydroxypropyl and#946;-cyclodextrin, Kolliphor P188 and Affinisol in varying ratios. newlineAbstract newlinePage B newlineFrom saturation solubility study and dissolution study, ternary dispersions F18 (CNF/Soluplus/Kolliphor P188 1:1:1) and F19 (CNF/Soluplus/Affinisol 1:1:1) showed 10.44 and 9.26 fold s