Polymeric recrystallized spherical agglomerates of felodipine by quasi-emulsion solvent diffusion method

The objective of the present work was to study the effect of different polymers on the solubility and dissolution rate of Felodipine (FL) a poorly water soluble antihypertensive, by spherically agglomeration using acetone, water and dichloromethane as good solvent, poor solvent and bridging liquid, respectively. The quasi-emulsion solvent diffusion technique was used as a method for spherical agglomeration. The hydrophilic polymers like polyvinyl pyrrolidone, polyvinyl alcohol, and polyethylene glycol were used in agglomeration process. The pure drug (FL) and its agglomerates with different polymers were characterize by differential scanning calorimetry (DSC), Powder X-ray diffraction (PXRD), IR spectroscopic studies and scanning electron microscopy (SEM). The DSC results indicated that decrease in melting enthalpy related to disorder in the crystalline content. PXRD studies also showed changes in crystallanity, IR spectroscopy revealed that there were no chemical changes in the recrystallized agglomerates. The spherical agglomerates with different polymers exhibited marked increase in solubility (41.01 μg mL-1) and dissolution rate (98.83% in 120 mins) as compared with FL. The SEM studies showed that the agglomerates posseeses a good spherical shape. The recrystallized agglomerates also exhibited higher micromeritic properties (bulk density, tapped density and angle of repose).

Author(s): Amit R. Tapas, Pravin S. Kawtikwar, and Dinesh M. Sakarkar

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