Ussing chamber技术评价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  

Evaluation of P-glycoprotein and organic cation transporter on the transport of levofloxacin by Ussing chamber

作　　者：胡咏梅[1,2] 张珊珊[3] 张磊[3,2] 胡兴萍[3] 许建明[3,2] 

机构地区：[1]安徽医科大学第一附属医院科研处,合肥230022 [2]安徽省消化系病重点实验室,合肥230022 [3]安徽医科大学第一附属医院消化内科,合肥230022

出　　处：《中国临床药理学杂志》2015年第17期1732-1735,共4页The Chinese Journal of Clinical Pharmacology

基　　金：国家自然科学基金青年基金资助项目(81100269)

摘　　要：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 effect of P- glycoprotein（ P- gp）and organic cation transporter（ OCTs） on the transport of levofloxacin by using a model in vitro. Methods A model in vitro was established by rat gastric mucosa combined with Ussing chamber. The concentrations of levofloxacin collected from the transport assay were determined by HPLC and the transport parameters such as apparent permeability coefficient[Papp（ M- S） and Papp（ S- M） ] and the ratio of Papp（ S- M） versus Papp（ M- S） were calculated and compared when the levofloxacin was used solely and co- used with P- gp inhibitor cyclosporin A or OCTs inhibitor cimetidine. Results When cyclosporin A was added, the Papp（ S- M） /Papp（ M- S） of levofloxacin decreased from 2. 20 to 1. 06（ P 0. 05）. There was no significant difference compared with the blank group while cimetidine was added. Conclusion The reasults indicated that P- glycoprotein might be involved in the transport of levofloxacin in this model in vitro,while the organic cation transporter probably not participated in.

关 键 词：左氧氟沙星 胃黏膜 Ussing chamber技术 高效液相色谱法 P-糖蛋白 有机阳离子转运体 

分 类 号：R978.1[医药卫生—药品] R965.1[医药卫生—药学]