甲巯咪唑水凝胶贴剂的制备和体外透皮性能  

Preparation of thiamazole hydrogel patch and its in vitro percutaneous permeability

作　　者：魏小藏[1] 刘卫[1] 周小顺[1] 左新河[2] 陈如泉[2] 杨祥良[1] 

机构地区：[1]华中科技大学生命科学与技术学院药物研究所,湖北武汉430074 [2]湖北中医学院附属医院,湖北武汉430060

出　　处：《中国医院药学杂志》2008年第5期348-351,共4页Chinese Journal of Hospital Pharmacy

基　　金：湖北省“十一五”科技攻关重大专项“现代透皮制剂技术研究开发”(课题编号:2006AA304A07)

摘　　要：目的:制备甲巯咪唑水凝胶贴剂,研究不同促渗剂对甲巯咪唑经皮渗透的促进作用,并与市售甲巯咪唑软膏进行比较,对甲巯咪唑水凝胶贴剂的体外透皮性能进行评价。方法:以具有良好生物相容性的亲水性高分子材料制备甲巯咪唑水凝胶贴剂,采用透皮扩散试验仪,以离体大鼠皮肤为屏障进行经皮渗透实验,高效液相色谱法测定接收池中药物的浓度,计算药物累积渗透量。结果:甲巯咪唑水凝胶贴剂制备工艺简单,各类促渗剂对甲巯咪唑的经皮渗透有不同程度的促进作用,其中月桂氮酮的促渗作用最为显著。以2%月桂氮酮为促渗剂的甲巯咪唑水凝胶贴剂的经皮渗透符合零级动力学过程,药物经皮渗透速率为39.60μg.cm-2.h-1,其24h单位面积累积渗透量为950.39μg.cm-2,高于对照制剂甲巯咪唑软膏。结论:甲巯咪唑水凝胶贴剂可以开发为甲巯咪唑的新型经皮给药制剂。OBJECTIVE To prepare thiamazole hydrogel transdermal patch and investigate the effect of penetration enhancer on the percutaneous permeability of thiamazole. To evaluate the percutaneous permeability of thiamazole hydrogel transdermal patch in vitro and compare its characteristic with thiamazole ointment. METHODS The thiamazole hydrogel transdermal patch was prepared with high polymer hydrophilic materials as matrix. The permeation flux of thiamazole was determined in vitro using Franz diffusion cell fitted with mouse skin. The content of thiamazole was measured by HPLC. RESULTS The experiment results showed that thiamazole hydrogel transdermal patch could be easily prepared. The penetration enhancers were found to increase the penetration of thiamazole and azone had the best penetration enhancing effect. The permeation of thiamazole hydrogel transderrnal patch containing 2% azone was in accordance with the zero-order kinetic. In comparison with thiamazole ointment, thiamazole hydrogel transdermal patch presents higher permeation rate of 39. 60μg·cm^-2 · h^-1 and cumulative permeation amount of 950. 39μg·cm^-2 . CONCLUSION Thiamazole hydrogel transdermal patch has good potential for transdermal delivery of thiamazole.

关 键 词：甲巯咪唑 水凝胶贴剂 制备 促渗剂 透皮性能 

分 类 号：R943[医药卫生—药剂学]