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目的研究左氧氟沙星在胃黏膜体外模型中的跨膜转运特征。方法用大鼠胃黏膜与尤斯灌流室建立胃黏膜体外模型,研究左氧氟沙星跨胃黏膜转运过程,评价药物浓度、方向、p H及P-糖蛋白抑制剂对其转运的影响;用高效液相色谱法检测药物浓度,计算其表观渗透系数。结果左氧氟沙星的转运具有一定的p H值依赖性,并且有显著的方向性差异,P-糖蛋白抑制剂维拉帕米增加了左氧氟沙星的跨膜转运。结论左氧氟沙星在胃黏膜体外模型中的转运机制可能以载体介导的主动转运方式为主,P-糖蛋白参与了其跨膜转运过程。
Objective To study the transmembrane transport characteristics of levofloxacin in gastric mucosa in vitro model. Methods Gastric mucosa in vitro and in vitro were established in rat gastric mucosa and uentral perfusion chamber to study the transmucosal transport process of levofloxacin and the effect of drug concentration and direction, p H and P-glycoprotein inhibitors on its transport. Chromatographic detection of drug concentration, calculate the apparent permeability coefficient. Results The levofloxacin transport had a certain p H value dependence, and there was a significant difference in direction. The p-glycoprotein inhibitor verapamil increased the transmembrane transport of levofloxacin. Conclusions The mechanism of levofloxacin transport in gastric mucosa in vitro may be mediated by the carrier-based active transport mode, and P-glycoprotein is involved in the transmembrane transport process.