Phase behavior of itraconazole-phenol mixtures and its pharmaceutical applications

被引：30

作者：

Park, Chun-Woong ^{[1
,2
]}

Mansour, Heidi M. ^{[3
]}

Oh, Tack-Oon ^{[1
]}

Kim, Ju-Young ^{[1
]}

Ha, Jung-Myung ^{[1
]}

Lee, Beom-Jin ^{[4
]}

Chi, Sang-Cheol ^{[1
]}

Rhee, Yun-Seok ^{[5
,6
]}

Park, Eun-Seok ^{[1
]}

机构：

[1] Sungkyunkwan Univ, Sch Pharm, Suwon 440746, Gyeonggi Do, South Korea

[2] Chungbuk Natl Univ, Coll Pharm, Cheongju 361763, Chungbuk, South Korea

[3] Univ Kentucky, Coll Pharm, Dept Pharmaceut Sci, Drug Dev Div, Lexington, KY 40536 USA

[4] Ajou Univ, Coll Pharm, Suwon 443749, Gyeonggi Do, South Korea

[5] Gyeongsang Natl Univ, Coll Pharm, Jinju 660751, Gyeongnam, South Korea

[6] Gyeongsang Natl Univ, Res Inst Pharmaceut Sci, Jinju 660751, Gyeongnam, South Korea

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 2012年 / 436卷 / 1-2期

关键词：

Itraconazole; Phenol; Eutectic mixture; Topical; Skin permeation; SOLID DISPERSION; BETA-CYCLODEXTRIN; DOSE PHARMACOKINETICS; POLYETHYLENE-GLYCOL; MOLECULAR MOBILITY; T-G; FORMULATION; BIOAVAILABILITY; SOLUBILITY; DELIVERY;

D O I：

10.1016/j.ijpharm.2012.07.054

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

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, H-1-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. (c) 2012 Elsevier B.V. All rights reserved.

引用

页码：652 / 658

页数：7

共 40 条

[1] Single-dose pharmacokinetics of intravenous itraconazole and hydroxypropyl-β-cyclodextrin in infants, children, and adolescents [J].