不同浓度甲基纤维素凝胶基质中布洛芬经皮释药特性研究  

Percutaneous permeation of ibuprofen in different concentrations of methyl cellulose gel

作　　者：陈莉[1] 张莉[1] 段姚尧[1] 申去非[1] 王晓辉[1] 齐刚[1] 

机构地区：[1]武警医学院生药学与药剂学教研室,天津300162

出　　处：《武警医学》2009年第8期671-674,共4页Medical Journal of the Chinese People's Armed Police Force

基　　金：武警医学院青年基金(WYQ-2004-4)

摘　　要：目的研究不同浓度的甲基纤维素对凝胶剂中布洛芬经皮渗透特性的影响。方法采用改良的Franz扩散池,以离体鼠皮为透皮屏障,用紫外分光光度法测定接受液中布洛芬的含量。考察不同用量凝胶基质中布洛芬在0.5、1、1.5、2、3、4、5、6、8、10、24、48、72 h时的累积透过量,采用滞留时间法评价不同浓度的甲基纤维素水凝胶的经皮释药特性。结果2.5%和5%甲基纤维素的布洛芬凝胶剂外观较好。且随着基质浓度的降低,凝胶剂中布洛芬的累积透过量显著增加。5%甲基纤维素的布洛芬凝胶剂的稳态流量(J_(ss))为3854.4μg/(cm^2.h),滞留时间(T_(lag))为1.2549 h,表观扩散系数(D_(app))达到44.9657,和皮肤/供体相分配系数(K_(app))为0.0394。结论选用5%甲基纤维素作为布洛芬凝胶剂的基质较好。Objective To study the effects of methyl cellulose gel in different concentrations on percutaneous permeation of ibuprofen in vitro. Methods Using improved Franz type diffusion cell and excised rat skin in vitro as transdermal barrier,the concen- trations of ibuprofen in samples were determined by UV spectro photometry. The cumulative permeation quantities of ibuprofen in gels were observed at 0.5,1,1.5,2,3,4,5,6,8,10,24,48, and 72 h, separately. The characteristics of percutaneous permeation for ibupro- fen in methyl cellulose gel were evaluated by lag time method. Results With methyl cellulose at the concentrations of 2.5 % and 5 %, the appearances of ibuprofen gel were very good. With decrease in concentration of methyl cellulose, the amount of transdermal absorp- tion of ibuprofen in gels increased significantly, and the steady - state flux（ Jss ） of ibuprofen in 5% methyl cellulose gel was 3854.4 μg/ （ cm2 · h） ,the lag time（Tlag）was 1. 2549 h,the diffusion coeffJcent（D,pp）Was 44. 9657,and the skin/donor phase partition coefficient （Kapp ）was 0. 0394. Conclusions 5% methyl cellulose gel is a good drug vehicle for ibuprofen transdermal system.

关 键 词：布洛芬 滞留时间法 凝胶剂 透皮吸收 甲基纤维素 

分 类 号：R914.2[医药卫生—药物化学]