促渗剂对氟比洛芬体外经皮渗透的影响

目的研究不同的促渗剂对氟比洛芬体外经皮渗透的促渗作用。方法采用TK-6A型透皮扩散仪,用人皮进行体外经皮渗透实验,考察不同的促渗剂二甲基亚砜、月桂醇、丙二醇、月桂氮酮(氮酮)、尿素、油酸]及其组合对氟比洛芬体外透皮吸收的促渗作用,以HPLC法测定各时间点接受室中药物浓度,求算透皮吸收的有关参数,比较各促渗剂的促渗作用。结果15%二甲基亚砜、3%氮酮、1%尿素可使氟比洛芬经皮渗透速率分别提高1.8,1.5,1.1倍,促渗剂联用取得的促渗效果更佳,5%油酸 20%丙二醇 1%尿素可使该药物的经皮渗透速率提高6倍。结论单用促渗剂对氟比洛芬经皮渗透促渗效果有限,促渗剂联合使用可以显著提高氟比洛芬经皮渗透速率。

Influence of penetration enhancers on permeation of flurbiprofen in vitro

OBJECTIVE To study the effect of different penetration enhancers on the permeation of flurbiprofen through human skin in vitro.METHODS The enhancing effects of these enhancers on the skin permeation of flurbiprofen were evaluated using human cadaver skin on the modified Franz diffusion cells.HPLC method was established to determine the content of drug in receiver at specified time points. RESULTS The flux of flurbiprofen through human skin was enhanced by 1.8,1.5 and 1.1 times by use of 15% dimethylsulfoxide,3%Azone,1%urea,respectively.The mixture of 5%oleic acid 20%propylene glycol 1%urea was found to be the most powerful penetration enhancers in this study.CONCLUSION The mixture use of enhancers,especially oleic acid,propylene glycol and urea,is found to be effective penetration enhancer for the skin permeation of flurbiprofen.