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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频率为指标评价渗透促进剂的体内外刺激性。结果 0 .0 5 %的去氧胆酸钠和 1%的泊洛沙姆 188分别使TM的表观透过系数增大 1.88和 1.5 5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。
Objective To study the effect of penetration enhancers on the permeability of timolol maleate (TM) cornea and its irritation. Methods Two-chamber diffusion cell method was used to determine the change of TM transmission in isolated rabbit cornea after adding six kinds of penetration enhancers. Corneal hydration values and blink frequency were used as indices to evaluate the in vitro and in vivo irritation of permeation enhancers. Results 0. 05% sodium deoxycholate and 1% poloxamer 188 increased the apparent transmission coefficient of TM by 1.88 and 1.55 times, respectively, with no in vitro or in vitro irritation. Further increasing poloxamer 188 concentration inhibits drug transmission through the cornea. Although laurocapram can significantly increase the permeation of TM, it causes damage to corneal tissue. Conclusion Low concentrations of sodium deoxycholate and poloxamer 188 are less irritating and effective ophthalmic penetration enhancers.