摘要
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 investigate the transport characteristics of levofloxacin.Method A model was established in vitro by gastric mucosa combined with Ussing chamber for studying the gastric mucosa transport mechanisms of levofloxacin.The effects of concentration of donor solutions,direction,pH and P- glycoprotein（ P- gp） inhibitor on the transport of levoflo-xacin were investigated.The concentrations of levofloxacin were determined by high performance liquid chromatography（ HPLC） and the transport parameters such as apparent permeability coefficient（ Papp） was calculated.Results The transport of levofloxacin obeyed a passive diffusion in a pH- dependent manner,and significant differences between the Papp of two directions.The P-gp inhibitor verapamil enhanced the transport amount of levofloxacin.Conclusion The reasults indicated that carrier- mediated transport manner might play a major role in the transport of levofloxacin in this model in vitro and P-gp probably participated in the transport of levofloxacin.
出处
《中国临床药理学杂志》
CAS
CSCD
北大核心
2015年第1期25-27,30,共4页
The Chinese Journal of Clinical Pharmacology
基金
国家自然基金青年基金资助项目(81100269)
