Itraconazole properties

Severely neutropenic patients Itraconazole oral solution as treatment for oropharyngeal and/or esophageal candidiasis was not investigated in severely neutropenic patients. Because of its pharmacokinetic properties, itraconazole oral solution is not recommended for initiation of treatment in patients at immediate risk of systemic candidiasis. 

Itraconazole (Sporanox, 13.11) is an approved antifungal (Figure 13.5). The drug has a log P value of 6.5, so its very low aqueous solubility is no surprise. Early efforts to improve the properties of itraconazole focused on making an acid salt. Because of the very weak basicity of all the nitrogens in itraconazole, the idea of an acid salt was soon abandoned. Cocrystals were then explored. A library of amides and acids were... 

Haria M, Bryson HM, Goa KL. Itraconazole. A reappraisal of its pharmacological properties and therapeutic use in the management of superficial fungal infections. Drugs 1996 51(4) 585-620. Erratum in Drugs. 1996 52(2) 253. 

B. Azole antifungals include systemic agents such as keto-conazole, fluconazole, itraconazole, and voriconazole. Topical agents used for the treatment of vaginal candidiasis and thrush include miconazole and clotrimazole. The pharmacologic properties of the systemic azoles differ considerably. Ketoconazole, the first oral azole developed, has poor bioavailability and requires an acidic environment for enhanced absorption. Thus, initial studies required ketoconazole to be administered with a cola to increase bioavailability. Fluconazole, unlike itraconazole and ketoconazole, is hydrophillic and has increased penetration across the blood-brain barrier. Fluconazole is also the only azole that is renally eliminated. 

Grant, S.M. Clissold, S.P. (1989) Itraconazole a review of its pharmacodynamic and pharmacokinetic properties, and therapeutic use in superficial and systemic mycoses. Drugs, 37, 310-344. 

Ketoconazole has been replaced by itraconazole for the treatment of aU mycoses except when cost is the primary determinant. Itraconazole lacks ketoconazole s corticosteroid suppression, while retaining most of its properties and expanding the antifungal spectrum. 

Sterol 14-demethylase inhibitors with more potent activity and/or more optimal pharmacokinetic properties than ketoconazole and itraconazole need to be investigated in clinical trials to evaluate their potential for treating humans with Chagas disease... 

Six, K. Leuner, C. Dressman, J. Verreck, G. Peeters, J. Blaton, N. Augustijns, P Kinget, R. Van den Mooter, G. Thermal properties of hot-stage extrudates of itraconazole and eudragit ElOO. Phase separation and polymorphism. J. Ther. Anal. Calorimet. 2002, 68(2), 591—601. 

Six, K. Verreck, G. Peeters, J. Brewster, M. Van Den Mooter, G. Increased physical stability and unproved dissolution properties of itraconazole, a class II drug, by solid dispersions that combine fast-and slow-dissolving polymers. J. Pharm. Sci. 2004, 93(1), 124—131. 

Verreck, G. Decorte, A. Heymans, K. Adriaensen, J. Cleeren, D. Jacobs, A. Liu, D. et al. The effect of pressurized carbon dioxide as a temporary plasticizer and foaming agent on the hot stage extrusion process and extrudate properties of solid dispersions of itraconazole with PVP-VA 64. Eur. J. Pharm. Sci. 2005, 26(3-4), 349-358. 

Pectin shows significant potential in drug delivery. It is either used on its own or blended with other polymers to meet the desired physicochemical properties. Pectin has been used as an emulsifier to prepare nanoemulsion consisting of itraconazole, a poorly water-soluble drug [Burapapadh et al., 2010]. An increase in pectin content, especially HM pectin leads to a decrease in emulsion droplet size. HM pectin, which is constituted of a high DE, provides a good emulsification property as a high fraction of hydrophobic... 

Matsumoto T, Zografi G (1999) Physical properties of solid molecular dispersions of in-domethacin with poly(vinylpyrrolidone) and poly(vinylpyrrolidone-co-vinyl-acetate) in relation to indomethacin crystallization. Pharm Res 16 1722-1728 MiUer DA, DiNunzio JC, Yang W, McGinity JW, Williams RO 3rd (2008) Enhanced in vivo absorption of itraconazole via stabilization of supersaturation following addic-to-neutral pH transition. Drug Dev Ind Pharm 34 890-902... 

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