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Sci. Pharm. 2009, 77(2), 401-418; doi:10.3797/scipharm.0901-08

Synergistic Enhancement of Itraconazole Dissolution by Ternary System Formation with Pluronic F68 and Hydroxypropylmethylcellulose

1
Department of Pharmaceutics, College of Pharmacy, King Saud University, Riyadh 11451, P.O. Box 2457, Saudi Arabia
2
Department of Pharmaceutical Technology, College of Pharmacy, University of Tanta, Tanta, Egypt
*
Author to whom correspondence should be addressed.
Received: 6 January 2009 / Accepted: 2 March 2009 / Published: 6 March 2009
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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.
Keywords: Itraconazole dissolution; Ternary solid dispersion; HPMC; Pluronic F68 Itraconazole dissolution; Ternary solid dispersion; HPMC; Pluronic F68
This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MAGHRABY, G.M.E.; ALOMRANI, A.H. Synergistic Enhancement of Itraconazole Dissolution by Ternary System Formation with Pluronic F68 and Hydroxypropylmethylcellulose. Sci. Pharm. 2009, 77, 401-418.

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