噻吗洛尔的透皮特性及影响其透皮吸收的因素

采用V-C水平扩散池对噻吗洛尔穿透完整无毛小鼠和人皮肤以及去角质层无毛小鼠和人皮肤的透过特性进行了摸索。对影响噻吗洛尔透皮吸收的因素如水合、介质pH以及各种透皮促进剂对其穿透率的影响进行了系统的研究。本文应用YWC-C₁₈健合固定相,以水-乙腈-三乙胺(87:13:1)为流动相系统,对噻吗洛尔进行了体外反相高效液相色谱法检测。实验结果表明噻吗洛尔透皮吸收的可行性,其透皮穿透率随着水合时间的适当延长、介质pH值的增大以及各类透皮促进剂的使用有显著性的增加。其中10%和1%azone合用体现了较好的协同作用。本结果为噻吗洛尔TTS的进一步研制提供了实验基础。

TRANSDERMAL PROPERTIES OF TIMOLOL AND FACTORS AFFECTING ITS PERMEABILITY IN VITRO

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.