摘要
目的研究不同的促渗剂对氟比洛芬凝胶体外经皮渗透的影响。方法采用改良Franz扩散池,用大鼠全皮进行体外经皮渗透实验,考察不同的促渗剂(二甲基亚砜、丙二醇、氮酮、尿素、薄荷醇、油酸、N-甲基吡咯烷酮)及其组合对氟比洛芬凝胶体外经皮渗透的影响,以HPLC法测定各时间点接受室中药物浓度,求算经皮吸收的有关参数,比较各促渗剂的促渗作用。结果质量分数为20%丙二醇、5%薄荷醇、5%油酸、10%N-甲基吡咯烷酮可使氟比洛芬凝胶经皮渗透速率分别提高至无渗透促进剂凝胶的1.20、1.71、1.21、1.59倍,12h累积透过量分别提高至无渗透促进剂凝胶的1.27、1.76、1.22、1.41倍。尿素、氮酮对氟比洛芬凝胶经皮渗透显示了抑制作用,且随着浓度的增加抑制作用增加。促渗剂联用取得的促渗效果更佳,质量分数5%薄荷醇+质量分数20%丙二醇可使氟比洛芬凝胶经皮渗透速率提高至无渗透促进剂凝胶的3.25倍,12h累积透过量提高至无渗透促进剂凝胶的3.78倍。结论单用促渗剂对氟比洛芬凝胶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凝胶经皮渗透速率和累积透过量。
Objective To study the effect of different penetration enhancers on the permeation of flurbiprofen gel across rat skin in vitro.Methods Using the modified Franz diffusion cell,the permeation enhancing effects of different enhancers on the transdermal absorption of flurbiprofen across rat skin were evaluated.HPLC method was established to determine drug content in the receiver at specified time points.Results Compared to the control group,the flux of flurbiprofen across rat skin was enhanced by 1.20,1.71,1.21 and 1.59 times by using 20% propylene glycol,5% menthol,5% oleic acid and 10% N-Methyl-pyrrolidone,respectively.Accordingly,the accumulated amount of flurbiprofen in the skin in 12 h increased by 1.27,1.76,1.22 and 1.41 times.The mixture of 5% menthol + 20% propylene glycol was found to be the most effective penetration enhancer in this study.Conclusions Compared to single enhancers,a combined use of enhancers,especially menthol and propylene glycol,can significantly increase the flux and accumulation of flurbiprofen in the rat skin.
出处
《中国药剂学杂志（网络版）》
2008年第4期176-183,共8页
Chinese Journal of Pharmaceutics：Online Edition
关键词
药剂学
促渗
体外经皮渗透试验
氟比洛芬
促渗剂联合使用
凝胶
pharmaceutics
penetration enhancer
transdermal absorption in vitro
flurbiprofen
enhancer combination
gelatum
