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考察了有机胺及不同透皮促进剂在乙醇肉豆蔻异丙酯二元溶剂系统中对洛索洛芬(LP)的透皮促进作用。采用药物透皮试验扩散仪,以离体大鼠腹部皮肤为渗透屏障,pH 7.4的磷酸盐缓冲液为接收液进行体外渗透实验,用HPLC测定浓度;比较加入不同有机胺的种类和比例以及不同的透皮促进剂组合对LP的透皮促进作用。加入不同的有机胺对LP的促渗作用不同,以二乙醇胺最为明显,且二乙醇胺与LP的量相同时作用最为显著。联合应用3%的氮酮和3%的薄荷醇对LP的透皮促进作用最为显著。等量的二乙醇胺+3%氮酮+3%薄荷醇是LP经皮给药较理想的促渗剂。
The effects of organic amines and different transdermal accelerators on the transdermal enhancement of loxoprofen (LP) were investigated in a binary solvent system of ethyl myristoleate. Using drug transdermal test diffusor, in vitro rat abdominal skin as an osmotic barrier, pH 7.4 phosphate buffer solution as the receiving solution for in vitro penetration test, the concentration was determined by HPLC; comparing the different types and proportions of different organic amines, and different Of the transdermal enhancer combination on the transdermal promoting effect of LP. Addition of different organic amines had different effects on the enhancement of LP. The most obvious effect was on diethanolamine, and the effect was most significant when the amount of diethanolamine and LP was the same. The combination of 3% Azone and 3% Menthol had the most significant effect on LP penetration. The same amount of diethanolamine + 3% Azone + 3% menthol is the ideal penetration enhancer for LP transdermal delivery.