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目的评价P-糖蛋白及有机阳离子转运体对左氧氟沙星跨胃黏膜转运的影响。方法用大鼠胃黏膜与Ussing chamber技术建立胃黏膜体外模型,分为空白组及加入P-糖蛋白抑制剂(环孢素A)或有机阳离子转运体抑制剂(西咪替丁)的抑制剂组并进行双向转运实验,用高效液相色谱法对左氧氟沙星进行定量分析,计算其表观渗透系数(Papp)。结果加入环孢素A后,50μg·m L-1左氧氟沙星Papp(S-M)/Papp(M-S)由2.20变为1.06(P<0.05);加入西咪替丁后,50μg·m L-1左氧氟沙星Papp(S-M)/Papp(M-S)与空白组比较,差异无统计学意义。结论 P-糖蛋白参与左氧氟沙星跨胃黏膜转运过程,而有机阳离子转运体不参与左氧氟沙星跨胃黏膜转运过程。
Objective To evaluate the effects of P-glycoprotein and organic cation transporter on the gastric mucosal transport of levofloxacin. Methods Gastric mucosa and Ussing chamber were used to establish gastric mucosa model in vitro. The model was divided into blank group and inhibitor of cyclosporine A or organic cation transporter inhibitor (cimetidine) Group and bidirectional transport experiments, using high performance liquid chromatography for quantitative analysis of levofloxacin, calculate the apparent permeability coefficient (Papp). Results After addition of cyclosporin A, Papp (SM) / Papp (MS) of levofloxacin of 50 μg · mL -1 changed from 2.20 to 1.06 (P <0.05). After adding cimetidine, 50 μg · m L -1 Levofloxacin Papp (SM) / Papp (MS) compared with the blank group, the difference was not statistically significant. Conclusion P-glycoprotein is involved in the trans-gastric mucosal transport of levofloxacin, while the organic cation transporter is not involved in the trans-gastric mucosal transport of levofloxacin.