摘要
本文研究了挥发油类促进剂对噻吗洛尔经离体鼠皮肤的促进作用，探讨了凝胶控释型贴剂的透皮吸收机理。采用双室渗透扩散装置和紫外分光光度法，通过大鼠皮肤进行了贴剂的体外释放与渗透试验。结果表明，桉油、松节油、薄荷素油及与丙二醇的复合物均能有效地促进噻吗洛尔的渗透。首次发现２％桉油与丙二醇（１∶１）混合物为最佳透皮吸收促进剂，其作用比３％Ａ－ｚｏｎｅ与丙二醇（１∶３）混合物强。研究表明，该贴剂经皮渗透的主要屏障为角质层，压敏胶可明显减慢凝胶骨架中药物的渗透速率。大鼠皮肤渗透动力学试验表明，噻吗洛尔溶液的渗透呈零级动力学，而凝胶骨架贴剂中药物的渗透可用Ｈｉｇｕｃｈｉ方程来表述。
The effects of various volatile oils enhancers on the permeation of timolol through excised rat skin were observed. The mechanism of transdermal absorption of timolol maleate gelmatrix diffusion controlled patches was investigated. The in vitro drug diffusion from gel matrix and the permeation tests across excised rat skin were carried out by two compartment diffusion cells and UV spectrophtometry method. It was found that the permeation rate of timolol was considerably enhanced by eucalyptus oil (EO), turpentine oil, and pepperment oil or in the propylene glycol (PG) combination. In this studies matrix consisting of 2% eucalyptus oil+propylene glycol (PG) (1∶1) was found to be the optimal enhancer for the penetration of timolol. The effects of mixed enhancers on rat skin penetration were ordered as follows: 2% EO+PG(1∶1)>3% Azone+PG(1∶3). Furthermore, it seemed that the main barrier to the in vitro penetration of timolol patches through rat skin was stratum corneum. The pressure sensitive adhesive could significantly reduce the value of permeation coefficient of the drug in the gel matrix patches. The permeation process of timolol solution was found to follow zeroorder kinetics and the permeation rate of drug from the hydrogel formulations could be described by Higuchi′s Equation.
出处
《中国药科大学学报》
CAS
CSCD
北大核心
1997年第6期326-330,共5页
Journal of China Pharmaceutical University
基金
国家自然科学基金
关键词
马来酸噻吗洛尔
凝胶控释型
促进剂
透皮吸收
Timolol maleate
Gelmatrix diffusion controlled patches
Enhancer
Barrier function
Transdermal absorption
