透皮促进剂对酮基布洛芬体外经皮渗透的影响

酮基布洛芬(KP)体外经皮渗透性实验研究表明,KP经皮渗透是一个零级速率过程。利用离体鼠皮为渗透屏障考察KP在月桂氮艹卓酮(AZ)、油酸(OA)、1-甲基-2-吡咯烷酮(2P)、N,N-二甲基甲酰胺(DMF)、月桂醇(LA)、丙二醇(PG)6种透皮促进剂作用下的透皮效果,发现这些透皮促进剂对KP透皮速率的影响有明显差别。其中油酸、月桂氮艹卓酮、1-甲基-2-吡咯烷酮和丙二醇可促进KP吸收透皮,促进强度依次为OA>AZ>2P>PG,并且两种透皮促进剂OA与AZ或2P合用有较好的协同作用,而DMF、月桂醇和高浓度丙二醇则阻滞KP经皮渗透。

EFFECT OF ENHANCERS ON THE PERMEATION OF KETOPROFEN IN VITRO

The result of permeability test of ketoprofen(KP)in vitro showed that the penetra-tion 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),sixpenetration enhancers,on the percutaneous absorption of KP were carried out by using isolated shavedmouse skin,These enhancers exhibited different effects,Among the enhancers,OA,AZ,2P and PGenhanced the skin permeation of KP,Their order of effect was OA>AZ>2P>PG,AZ and 2P incombination with OA were shown to have synergistic effect.But DMF,LA and PG at high levelsinhibited the permeation of KP.