【摘要】 目的:研究依诺沙星(ENX)的角膜透过性,为其处方设计提供理论基础。方法:采用体外扩散实验考察在多种渗透促进剂条件下ENX的离体兔眼角膜透过性。结果:1％的泊洛沙姆F68和2％羟丙基-β-环糊精(HP-β-CD)分别使ENX的表观渗透系数增加1.65和2.05倍,与对照组呈现显著性差异(P<0.01),而0.5％乙二胺四乙酸二钠(EDTA)与0.05％月桂氮革酮(Azone)未能显著增大ENX的表观渗透系数(P>0.05);所有渗透促进剂均未显著改变ENX透过角膜的滞后时间;0.05％Azone和1％ F68对眼组织具有刺激性。结论:2％ HP-β-CD能够显著增加ENX的表观渗透系数,且对角膜无明显刺激性。更多还原

【Abstract】 Objective:To explore the corneal permeability of enoxacin (ENX) in vitro. Methods : The permeable characteristics of ENX across the cornea of an isolated rabbit were studied in vitro using a variety of osmotic enhancers. Results: 1% poloxamer (F68) and 2% HP-β-CD showed a significant increment as much as 1. 65 and 2.05 times in the apparent permeability of ENX, respectively, compared with the ones in the control (P<0.01). However,0.05% Azone and 0.5% EDTA did not improve the apparent permeability of ENX. The enhancers insignificantly changed the lag time pertinent to the corneal permeability.1% poloxamer (F68) and 0.05% Azone were irritable to eye tissues. Conclusion:2% HP-β-CD serves the corneal apparent permeability of ENX better.更多还原