促进剂对酮洛芬巴布剂体外透皮性的影响探讨  

Study on influence of percutaneous enhancers on transdermal permeation of ketoprofen cataplasm in vitro

作　　者：何文[1] 李勇[2] 张国晴[2] 何杨虎[2] 何平平[2] 

机构地区：[1]武汉大学人民医院药学部,湖北武汉430060 [2]武汉大学药学院,湖北武汉430070

出　　处：《中国医院药学杂志》2007年第12期1681-1684,共4页Chinese Journal of Hospital Pharmacy

摘　　要：目的:通过几种常用促进剂对酮洛芬巴布剂体外促渗作用研究,筛选出适合用于酮洛芬巴布剂的透皮促进剂。方法:分别制备单独含2%或4%的桉叶油、油酸、薄荷脑、聚乙二醇400、月桂氮芯卓酮、聚山梨醇酯-80的酮洛芬巴布剂贴片,以及4%的桉叶油分别与2%的油酸、薄荷脑、聚乙二醇400合用的酮洛芬巴布剂贴片,采用改良Franz透皮扩散池,以离体小鼠背部皮肤为透皮屏障,贴敷12h,以渗透速率及12h累积渗透量为指标,探讨促进剂对酮洛芬体外透皮性的影响。结果:与空白组对照,2%聚山梨醇酯-80、2%月桂氮卓芯酮单独使用不能明显提高酮洛芬的渗透速率(P>0.05),4%聚山梨醇酯-80、4%月桂氮卓芯酮和其他的促进剂都能明显的提高酮洛芬的经皮渗透(P<0.01),对酮洛芬透皮速率提高大小顺序为油酸≥桉叶油>薄荷脑>聚乙二醇400>月桂氮卓芯酮>聚山梨醇酯-80。结论:油酸、桉叶油、薄荷脑、聚乙二醇400均可作为酮洛芬巴布剂透皮促进剂。OBJECTIVE To study the effects of several percutaneous enhancers on the permeation of ketoprofen through skin in vitro in order to screen the suitable transdermal enhancers for ketoprofen cataplasms. METHODS 20% or 40% oleum eucalypti, oleic acid, menthol, PEG400, azone tween 80 wererespectively used to formulate ketoprofen cataplasms, while 40% oleum eucalypti were combined with 20% oleic acid or menthol or PEG400 to formulate ketoprofen cataplasms. Franz diffusion cell was adopted as the apparatus for in vitro skin permeation test and excised mouse back skin as percutaneous permeation barrier. The permeation rate and the cumulative permeation amount of ketoprofen in 12 h were calculated to study the influence of percutaneous enhancers on permeation of ketoprofen in vitro. RESULTS Compared with blank group, 20% tween 80, 2% azone had little enhancement effect on the permeability of ketoprofen（P〉0.05）, while 40% tween 80, 40% azone and all other percutaneous enhancers showed significant enhancing effects on the permeability of ketoprofen （P〈0.01 ）, The order of permeation rate of several percutaneous enhancers with same concentration was： oleic acid≥oleum eucalypti〉menthol〉PEG400〉azone〉tween 80. CONCLUSION Oleum eucalypti, oleic acid, menthol, PEG400 would be the proper percutaneous enhancers in the transdermal preparations of ketoprofen.

关 键 词：酮洛芬 巴布剂 促进荆 透皮给药系统 

分 类 号：R943[医药卫生—药剂学]