乙醇-肉豆蔻酸异丙酯系统中有机胺对酮洛芬经皮渗透的促进作用  

Effect of amines on the percutaneous absorption of ketoprofen in a lipophilic system consisting of ethanol-isopropyl myristate

作　　者：牛喜草[1] 赵利刚[1] 蒋宇轩[1] 马蕊[1] 方亮[1] 

机构地区：[1]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2008年第11期860-865,共6页Journal of Shenyang Pharmaceutical University

摘　　要：目的应用乙醇(E)-肉豆蔻酸异丙酯(IPM)2组分溶液系统,研究在EI系统中有机胺对酮洛芬(KP)的经皮渗透的影响,初步探讨其作用机理。方法用水平扩散池,以离体大鼠皮肤作为渗透屏障进行体外渗透实验。用HPLC测定样品中KP浓度。结果除二乙胺(DEtA)和三乙胺外,当EI系统[m(乙醇)∶m(肉豆蔻酸异丙酯)=90∶10]中加入乙醇胺、二乙醇胺、三乙醇胺、和N-(2-羟乙基)吡啶时,KP在溶液系统中溶解度均略有降低。所有加入有机胺的EI溶液系统均对KP产生明显的渗透促进作用。此外,在DEtA-EI系统中,KP的流量与DEtA的浓度成正比,而E的渗透流量恒定,与KP流量变化无关。结论结果表明,EI系统中有机胺对KP的经皮渗透有促进作用。这种渗透促进作用可能依赖于KP与胺之间所形成的离子对组成。Objective To observe the percutaneous profiles of ketoprofen（KP） through rat abdominal skin using different amines in the ethanol-isopropyl myristate system. Methods 2-Chamber diffusion cells were adopted as the apparatus for in vitro skin permeation, excised rat abdominal skin as barrier. HPLC method with indomethacin as internal standard was established to determine the content of ketoprofen in receiver diffusion cell. Results When ethanolamine, diethanolamine, triethanolamine, diethylamine（DEtA）, triethy- lamine and N- （2-hydroxyethyl）- piperidine were added to the EI[m（isopropyl myristate） ： m （ethanol） = 90： 10] system, a greater enhancing effect was found compared to the EI system. Furthermore, at a fixed concentration of KP, the flux of KP was increased with the increase of the DEtA concentration in the amine- EI system, while the flux E remained unchanged. Conclusions The results demonstrate that the formation of an ion pair between KP and amine may be responsible for the enhanced skin permeation of KP using amine- EI system.

关 键 词：酮洛芬 胺 离子对 经皮吸收 体外实验 

分 类 号：R94[医药卫生—药剂学]