IMPROVED ACITRETIN DELIVERY THROUGH HAIRLESS MOUSE SKIN BY CYCLODEXTRIN COMPLEXATION

被引：22

作者：

LOFTSSON, T ^{[1
]}

SIGURDARDOTTIR, AM ^{[1
]}

OLAFSSON, JH ^{[1
]}

机构：

[1] UNIV ICELAND,FAC MED,DEPT DERMATOL,REYKJAVIK,ICELAND

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 1995年 / 115卷 / 02期

关键词：

ACITRETIN; COMPLEXATION; CYCLODEXTRIN; PERMEABILITY; SOLUBILITY; TOPICAL ADMINISTRATION;

D O I：

10.1016/0378-5173(94)00302-L

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

The effects of four cyclodextrins, i.e., 2-hydroxypropyl-beta-cyclodextrin, randomly methylated beta-cyclodextrin (M beta CD), gamma-cyclodextrin and 2-hydroxypropyl-gamma-cyclodextrin, on the aqueous solubility of acitretin were investigated. Of the four cyclodextrins tested M beta CD displayed the largest effect. The aqueous solubility of the drug could be increased even further by pH adjustment. Thus, the solubility of acitretin in an aqueous pH 7.5 buffer solution containing 23% (w/v) M beta CD was determined to be 1.96 mg/ml. Acitretin is insoluble in water. The flux of acitretin through hairless mouse skin was determined to be 0.032 mg h(-1) cm(-2) from a pure propylene glycol vehicle but 0.201 mg h(-1) cm(-2) from an aqueous M beta CD containing vehicle.

引用

页码：255 / 258

页数：4

共 7 条

[1] INCREASED SKIN PERMEABILITY FOR LIPOPHILIC MOLECULES [J].