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[噻吗洛尔的透皮特性及其体外渗透的影响因素]

[Transdermal properties of timolol and factors affecting its permeability in vitro].

作者信息

Xu Y Z, Xu H N

机构信息

Department of Pharmaceutics, School of Pharmacy, Shanghai Medical University.

出版信息

Yao Xue Xue Bao. 1992;27(6):467-71.

PMID:1442076
Abstract

V-C horizontal diffusion cell has been used to carry out the initial study of timolol across intact and stripped hairless mouse skin and human cadaver skin. Also, we have systematically studied the effect of some factors such as hydration time, medium pH value as well as various transdermal enhancers on the permeability of timolol in vitro. We investigated the determination method of timolol by RP-HPLC using YWG-C18 column with water-acetonitrile-triethylamine (87:13:1) as the mobile phase. The results indicated the feasibility of transdermal absorption of timolol. The permeabilities of timolol raised significantly with properly extending of hydration time, increasing of medium pH and with presence of various kinds of transdermal enhancers. With 10% propylene glycol and 1% azone were used conjunctly, they showed obviously synergistic effects. All these studies contributed theoretically and practically to the further development and utilization of timolol in the form of transdermal patch.

摘要

V-C水平扩散池已用于进行噻吗洛尔透过完整和去毛无毛小鼠皮肤以及人尸体皮肤的初步研究。此外,我们还系统地研究了一些因素,如水合时间、介质pH值以及各种透皮促进剂对噻吗洛尔体外渗透性的影响。我们采用YWG-C18柱,以水-乙腈-三乙胺(87:13:1)为流动相,研究了用反相高效液相色谱法测定噻吗洛尔的方法。结果表明噻吗洛尔经皮吸收具有可行性。随着水合时间的适当延长、介质pH值的升高以及各种透皮促进剂的存在,噻吗洛尔的渗透率显著提高。当10%丙二醇和1%氮酮联合使用时,它们表现出明显的协同作用。所有这些研究在理论和实践上都有助于噻吗洛尔透皮贴剂的进一步开发和利用。

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