双醋瑞因及其离子对离体猪皮渗透的研究  

Transdermal permeation of diacerein and its ion-pair complexes across parcine skin in vitro

作　　者：罗黎霞 易伟 汤淮波[1] 吴学文 何丽丽 LUO Li-xia;YI Wei;TANG Huai-bo;WU Xue-wen;HE Li-li(Department of Pharmacy,Chemistry College,Xiangtan University,Xiangtan Hunan 411105;Xiangtan Hospital of Traditional Chinese Medicine,Xiangtan Hunan 411101)

机构地区：[1]湘潭大学化学学院,湖南湘潭411105 [2]湘潭市中医医院,湖南湘潭411101

出　　处：《中南药学》2019年第10期1622-1626,共5页Central South Pharmacy

基　　金：湖南省湘潭市科技计划项目（No.SF-YB20161008）

摘　　要：目的研究双醋瑞因与有机胺形成的离子对对双醋瑞因的经皮渗透速率的影响。方法双醋瑞因与多种有机胺在丙酮中反应,生成物采用核磁共振与傅里叶红外表征,并测定生成物的溶解度、油水分配系数与熔点;采用离体猪耳朵皮研究双醋瑞因及其离子对的经皮渗透性能。结果经核磁共振与傅里叶红外表征双醋瑞因与多种有机胺生成离子对;双醋瑞因离子对的水饱和溶解度急剧增大,油水分配系数与熔点均显著降低;双醋瑞因离子对的体外经皮渗透速率均明显增加,双醋瑞因三乙醇胺离子对的透皮速率最高,已达到双醋瑞因的4.30倍。结论双醋瑞因离子对能明显改变双醋瑞因的理化性质,并能明显提高双醋瑞因的经皮渗透速率。Objective To determine the effect of diacerein and the ion-pair complexes of diacerein and organic amines on the transdermal permeation rate. Methods Diacerein reacted with various organic amines in acetone, and its complexes were confirmed by nuclear magnetic resonance spectroscopy(1 H-NMR) and fourier transform infrared spectroscopy(FTIR). The solubility, oil-water partition coefficient and melting point of diacerein and its complexes were also determined. The percutaneous permeability of diacerein and its ion-pair complexes across porcine skin in vitro was investigated. Results The ion-pair complexes of diacerein reacting with organic amines were confirmed by the FTIR and 1 H-NMR spectroscopy. The water saturation solubility of the ion-pair complexes was markedly increased, and their oil-water partition coefficient and melting point were decreased significantly. The percutaneous permeation rate of diacerein ion-pair complexes was increased significantly. Diacerein-triethanolamine was the highest in all candidates, reaching 4.30 times that of diacerein. Conclusion The physicochemical properties of diacerein ion-pair complexes may be changed obviously, and their transdermal permeation rate can be increased obviously.

关 键 词：双醋瑞因 离子对 体外透皮吸收 猎皮 

分 类 号：R283[医药卫生—中药学] R94[医药卫生—中医学]