Hu J H, Zhu Y
Pharmaceutical Department, Changhai Hospital, Shanghai.
Yao Xue Xue Bao. 1996;31(1):48-53.
The result of permeability test of ketoprofen (KP) in vitro showed that the penetration process could be described by zero-order kinetics. Azone (AZ), oleic acid (OA), 1-methyl-2-pyrrolidone (2P), dimethylformamide (DMF), propylene glycol (PG) and lauryl alcohol (LA), six penetration enhancers, on the percutaneous absorption of KP were carried out by using isolated shaved mouse skin. These enhancers exhibited different effects. Among the enhancers, OA, AZ, 2P and PG enhanced the skin permeation of KP. Their order of effect was OA > AZ > 2P > PG. AZ and 2P in combination with OA were shown to have synergistic effect. But DMF, LA and PG at high levels inhibited the permeation of KP.
酮洛芬（KP）体外渗透试验结果表明，渗透过程可用零级动力学描述。采用离体剃毛小鼠皮肤，对氮酮（AZ）、油酸（OA）、1-甲基-2-吡咯烷酮（2P）、二甲基甲酰胺（DMF）、丙二醇（PG）和月桂醇（LA）六种渗透促进剂对KP经皮吸收的影响进行了研究。这些促进剂表现出不同的效果。在这些促进剂中，OA、AZ、2P和PG增强了KP的皮肤渗透。它们的作用顺序为OA＞AZ＞2P＞PG。AZ和2P与OA联合使用具有协同作用。但高浓度的DMF、LA和PG抑制了KP的渗透。
