马来酸噻吗洛尔透皮贴剂的制备及释药机理研究  

Studies on the tlmolol transdermal therapeutic system

作　　者：冀学芳[1] 平其能[1] 刘国杰[1] 于顺廷[1] 

机构地区：[1]中国药科大学药剂教研室,北京市药品检验所

出　　处：《中国药学杂志》1996年第4期217-219,共3页Chinese Pharmaceutical Journal

摘　　要：目的：制备马来酸噻吗洛尔透皮贴剂，研究其释药机理。方法：利用双室渗透扩散装置，进行离体皮肤体外渗透实验，通过改变扩散液的ｐＨ值及皮肤的状态，研究其释药机理。结果：马来酸噻吗洛尔贴剂的体外释药方程为：Ｑ＝２０７．６ｔ￣（１／２）－１７６．１（ｒ＝０．９９７），２４ｈ累积释药量为８４５．６μｇ／ｃｍ￣２。随着扩散液ｐＨ升高，药物的渗透系数逐渐增大，去除角质层皮肤对药物渗透系数远远大于完整皮肤，且完整皮肤的贮库效应大于去除角质层皮肤。结论：马来酸噻吗洛尔主要以分子型透过皮肤，在经皮渗透过程中存在贮库效应，渗透的主要屏障为角质层。OBJECTIVE:To prepare matrix-type timolol transdermal therapeutic system and study penetrationmechanism. METHODS:Timolol permeation tests in vitro through rat skin in two compartment diffusion cells wereperformed to study the penetration mechanism of timolol by changing pH of donor phase and rat skin condition. RESULTS: The penetration equation of timolol-TTS was Q= 207.6t1/2一176.1(r=0. 997),and the cummulativerelease level in 24 h was 845.6μg/cm￣2 through rat skin in vitro. Timolol permeation coefficient and permeation lev- el increased linearly with increase of the pH in the donor phas. The timolol permeation coefficient of stripped stra- tum corneurn skin was higher than that of whole skin, and the deposit function of whole skin was more effectivethan that of stripped stratum corneum skin. CONCLUSION:Timolol penetrated skin mainly by molecular form. Thebarrier of timolol penetration was in the stratum corneum,and timolol permeating had the deposit function also in the stratum corneum.

关 键 词：马来酸噻吗洛尔 透皮贴剂 制备 释药机理 

分 类 号：R972.5[医药卫生—药品]