渗透促进剂对马来酸噻吗洛尔角膜透过性的影响

目的：研究渗透促进剂对马来酸噻吗洛尔（TM）角膜透过性的影响。并对其刺激性进行评价。方法：使用双室扩散池方法测定加入6种渗透促进剂后离体兔眼角膜对TM透过量的变化。以角膜水化值和眨眼值频率为指标评价渗透 促进剂的体内外刺激性。结果：0．05％的去氧胆酸钠和1％的泊洛沙姆188分别使TM的表现透过系数增大1．88和1．55倍而未见体内外刺激性。进一步提高泊洛沙姆188浓度抑制药物透过角膜。月桂氮Zhuo酮虽能显著增加TM的透过量却对角膜组织造成损伤。结论：低浓度的去氧胆酸钠和泊洛沙姆188为刺激性小、有效的眼用渗透促进剂。

Effects of penetration enhancers on the permeability of timolol maleate through isolated rabbit cornea

OBJECTIVE To study the effects of penetration enhancers on the transcorneal permeability of timolol maleate (TM) and evaluate their ocular irritancy.METHODS The influence of six compounds on TM permeating through isolated rabbit cornea were investigated using two chamber diffusion cells.The corneal hydration level and blinking frequency were recorded as in vitro and in vivo irritancy index.RESULTS 0.05% sodium deoxycholate and 1% poloxamer 188 improved the apparent permeability of TM as much as 1.88 and 1.55 times respectively without irritancy observed, but further increasing poloxamer 188 concentration led to lower permeability of TM.0.05% Azone caused corneal tissue damage although it showed the maximum permeation enhancing effect.CONCLUSION The low concentrations of sodium deoxycholate and poloxamer 188 may be effective ophthalmic penetration enhancers with less irritancy.