Modification of felodipine properties using spherically agglomerated solid dispersions

Abstract

The objective of the present work was to enhance the solubility, dissolution rate and micromeritic properties of Felodipine (FL) a poorly water soluble antihypertensive, using spherical agglomeration by Quasi Emulsion Solvent Diffusion (QESD) method. In this study methanol, water and dichloromethane were used as good solvent, poor solvent and bridging liquid, respectively. The hydrophilic polymers like Hydroxypropyl β-cyclodextrin, β-cyclodextrin, Lutrol F68, Lutrol F127 were used in agglomeration process. The pure drug (FL) and its agglomerates with different polymers were characterize for their drug loading as well as by Differential Scanning Calorimetry (DSC), X-ray Diffraction (XRD), FTIR spectroscopic studies and Scanning Electron Microscopy (SEM). The DSC results indicated decrease in melting enthalpy related to disorder in the crystalline content. XRD studies also showed changes in crystallanity, IR spectroscopy revealed that there were no chemical changes in the re crystallized agglomerates. The spherically agglomerated solid dispersions with different polymers exhibited marked increase in solubility (53.69±0.53 jig mL-1), dissolution rate (100.09±2.27% in 60 min) and micromeritic properties (bulk density, flow property, comparability) compared with FL. The SEM studies showed that the agglomerate possesses a good spherical shape. © 2011 Academic Journals Inc.