Kapoor and Subbarao: Formulation Development and Characterization of Itraconazole Granules

Itraconazole is practically insoluble in water; large interindividual and intra-individual variations of its oral bioavailability are reported. The main purpose of this study was to prepare and evaluate itraconazole granules for immediate release as drug delivery formulations. As a part of formulation optimization, different concentrations of hydroxypropyl-methyl cellulose (HPMC) E5 were taken for the preparation of itraconazole granules, and were optimized with different characteristic like size, shape, surface roughness, density, moisture content, assay and dissolution. Formulation optimization includes a detailed study of itraconazole granules with different concentrations of polymer. The results of the study showed that 6% of HPMC E5 is sufficient as a binding agent and gave good shape and surface, low moisture content, 100% assay and 98.24% drug release within one hour. Based on these results, it can be concluded that 6% HPMC E5 is suitable for formulation of itraconazole granules.