Abstract
Pluronic F68 is a surfactant which can inhibit CYP3A4, an enzyme responsible for hepatic metabolism of many drugs including itraconazole. This study investigated the effect of incorporation of Pluronic F68 as a ternary component in solid dispersions of itraconazole with hydroxypropyl-methylcellulose (HPMC) on the dissolution rate of itraconazole. Binary solid dispersions with HPMC, reduced the drug crystallinity, increased the equilibrium solubility but showed slow dissolution. Binary dispersions with Pluronic produced eutectic systems but the increase in solubility and dissolution was lower than that of HPMC systems. Ternary system comprising optimum proportions of drug with Pluronic and HPMC enhanced the dissolution rate showing dissolution efficiency comparable to that obtained with the marketed product of itraconazole. The study thus presented a system capable of increasing the dissolution rate of itraconazole with a potential for increased oral bioavailability by inhibiting its pre-systemic metabolism as well.
Highlights
Itraconazole is a potent broad-spectrum triazole antifungal drug with activity against histoplasmosis, blastomycosis and onychomycosis [1, 2]
The aim of this study was to investigate the effect of incorporation of Pluronic F68 as a component of the ternary system with HPMC and itraconazole on the solubility and dissolution rate of itraconazole
The study employed the simple solid dispersion technique and incorporated an excipient which can increase the bioavailability of itraconazole directly by enhancing the dissolution rate of the drug and indirectly by reducing its hepatic metabolism
Summary
© El Maghraby and Alomrani; licensee Österreichische Apotheker-Verlagsgesellschaft m. b.
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