摘要
以离体小鼠皮肤为屏障、人参皂苷Rg_1为指标,考察了11种咪唑类离子液体对促进三七总皂苷经皮渗透的影响。激光共聚焦显微镜(CLSM)考察结果表明,咪唑类离子液体能促进荧光素钠在小鼠皮肤中的渗透深度和渗透量。继而初步考察了咪唑类离子液体的构效关系。结果表明,离子液体的促渗作用受取代基链长、数目和类型的影响。双取代离子液体比单取代和三取代离子液体促渗作用强;在双取代离子液体结构引入羟基基团可增大促渗作用,而引入羧基基团则减弱促渗作用;双取代促渗剂与常用促渗剂(月桂氮酮、N-甲基-2-吡咯烷酮和1,2-丙二醇)的促渗作用相当,甚至更优。
The effects of eleven imidazolium ionic liquids （MILs） on percutaneous penetration of Panax notoginseng saponins were investigated with excised mouse skin as a barrier and ginsenoside Rg1 as an index. The results of confocal laser scanning microscopy （CLSM） showed that the MILs could enhance the penetration depth and penetration amount of sodium fluorescein. Furthermore, the structure-activity relationship of these MILs was preliminarily investigated. The results showed that the enhancement effect of the MILs affected by the length of side chain, number and type of substituent groups. The enhancement effects of di-substituted MILs were better than those of mono- and tri- substituted ones. When a hydroxyl group was introduced into one of the di-substituted MILs, its effect was enhanced; when a carboxyl group was introduced, its effect was weakened. Compared with the commonly used enhancers （azone, N-methyl-2-pyrrolidone and 1,2-propanediol）, the enhancement effects of di-substituted MILs were similar or even superior.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2015年第12期1317-1322,共6页
Chinese Journal of Pharmaceuticals
基金
云南省应用基础研究计划青年项目(2014FD012)
云南省人才培养项目(KKSY201326118)
关键词
咪唑类离子液体
三七总皂苷
人参皂苷RG1
经皮渗透
促渗剂
imidazolium ionic liquid
Panax notoginseng saponins
ginsenoside Rgl
percutaneous penetration
permeation enhancer
作者简介
张定（1989-），女，硕士研宄生，专业方向：中药外用制剂。E-mail：zding888@126．com
通信联系人：王承潇（1985-），男，博士，讲师，从事中药外用制剂研究。Tel：018388186612 E—mail：wcx1192002@126．com
