Effect of terpenes on skin permeation of non-ionized and ionized ketotifen

被引:0
|
作者
Obata, Y [1 ]
Ozawa, Y [1 ]
Takayama, K [1 ]
Nagai, T [1 ]
机构
[1] Hoshi Univ, Dept Pharmaceut, Shinagawa Ku, Tokyo 1428501, Japan
来源
STP PHARMA SCIENCES | 1999年 / 9卷 / 05期
关键词
skin permeation; ketotifen; pH-partition theory; fumaric acid; ion-pair; pretreatment; d-limonene; l-menthol;
D O I
暂无
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Thc permeability coefficient of ketotifen increased with increase in pH of donor solution, suggesting that skin permeation of ketotifen was virtually obeyed the pH-partition theory, although the contribution of the ionized form of ketotifen cannot be neglected Pretreatment with 2% d-limonene for 1 hour enhanced the permeability coefficient of non-ionized and ionized ketotifen. On the other hand, 1 hour pretreatment with 2% l-menthol slightly increased the non-ionized ketotifen value, bird greatly enhanced the ionized ketotifen value. The pH in the receiver solution after the permeation study was decreased by l-menthol pretreatment. After pretreatment with l-menthol, the permeability coefficient of ionized form of ketotifen and monovalent ionized form of fumaric acid was similar. A possible mechanism is that relatively hydrophobic ion-pair would be formed between rite ionized form of ketotifen nod monovalent ionized form of fumaric acid and the resultant ion-pair could permeate through the hydrophobic route in rite stratum corneum. Pretreatment with terpenes caused no leaching of lipids.
引用
收藏
页码:497 / 503
页数:7
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