Preparation and characterization of various solid dispersion formulations of itraconazole to enhance the drug dissolution profile

Abstract

This study investigated various solid dispersions of itraconazole with different carrier blends to enhance its dissolution. HPMC E5, HPMC E15, PEG 20000 and TPGS 1000 were used to construct 20 % drug containing solid matrices by spray drying method. The formulations were analyzed in terms of dissolution profile, x-ray diffraction (XRD) and/or differential scanning calorimetry (DSC) pattern once immediately after preparation and again after storage for three months at accelerated conditions. The results showed that different excipients could put their effects on the dissolution behavior of the drug mainly through affecting the solid states of the resultant mixtures. In this regard, presence of high portions of HPMC in the resultant matrices was the most promising approach for improving the dissolution rate of itraconazole. The dissolution behavior of the drug after storage was directly related to its relative crystal growth during this period, since the more generated semicrystalline structures showed slower dissolution rates.