Phase behavior of itraconazole-phenol mixtures and its pharmaceutical applications.

Abstract:

:The aims of this study were to examine the phase behavior of itraconazole-phenol mixtures and assess the feasibility of topical formulations of itraconazole using eutectic mixture systems. Itraconazole-phenol eutectic mixtures were characterized using differential scanning calorimetry, Fourier transform infrared spectroscopy, (1)H-nuclear magnetic resonance, and powder X-ray diffractometry. The skin permeation rates of itraconazole-phenol eutectic formulations were determined using Franz diffusion cells fitted with excised hairless mouse skins. Itraconazole can form eutectic compounds with phenol, and the hydrogen-bonding interactions between the carbonyl group in the itraconazole and hydroxyl group in phenol play a major role in itraconazole-phenol eutectic formation. Despite its high molecular weight and hydrophobicity, the drug (i.e., itraconazole) can be permeated through excised hairless mouse skins from itraconazole-phenol eutectic formulations. The findings of this study emphasize the capabilities of the topical application of itraconazole via external preparations.

journal_name

Int J Pharm

authors

Park CW,Mansour HM,Oh TO,Kim JY,Ha JM,Lee BJ,Chi SC,Rhee YS,Park ES

doi

10.1016/j.ijpharm.2012.07.054

subject

Has Abstract

pub_date

2012-10-15 00:00:00

pages

652-8

issue

1-2

eissn

0378-5173

issn

1873-3476

pii

S0378-5173(12)00775-2

journal_volume

436

pub_type

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