西他沙星在人源肠Caco-2细胞单层模型的吸收转运研究  

Transport of sitafloxacin across Caco-2 cell monolayers

作　　者：丁维明[1] 李桂玲[1] 李眉[1] 王菊仙[1] 杨信怡[1] 

机构地区：[1]中国医学科学院北京协和医学院医药生物技术研究所,北京100050

出　　处：《中国新药杂志》2014年第1期32-35,共4页Chinese Journal of New Drugs

基　　金：国家“重大新药创制”科技重大专项(2012ZX09301002-001);中央级公益性科研院所基本科研业务费专项(IMBF201201)

摘　　要：目的:研究西他沙星在Caco-2细胞模型中的吸收转运特征。方法:利用人源结肠癌细胞系Caco-2细胞单层模型研究西他沙星从绒毛面(AP端)到基底面(BL端)以及BL端到AP端两个方向的转运过程;考察转运时间、浓度、pH值等对西他沙星跨膜转运的影响;采用高效液相色谱法检测药物浓度,计算表观渗透系数P app。结果:西他沙星P app值>1.0×10-6cm·s-1,AP端到BL端P app值随药物浓度升高而减小,BL端到AP端P app值随药物浓度增高而增大。转运量和转运速率随时间和浓度增大而增大,在酸性条件下表观渗透系数P app值最大。结论:西他沙星属于良好吸收的化合物,转运过程可能有被动扩散和载体介导的主动转运共同参与,并且有一定的pH依赖性。Objective： To investigate the transport characteristics of sitafloxacin. Methods： Caco-2 cell monolayer model was applied to study the transport of sitafloxacin. The effects of time, concentration and pH on the transport of sitafloxacin were investigated. The determination of sitafloxacin was performed by HPLC. Results： The value of P pp was higher than 1.0 x 10-6 cm s-I Along with the increasing concentration, the Papp（AP^BL） of sita- floxacin decreased, and the Papp（BL^AP） increased. The transport amount and transport rate increased with time and concentration. Conclusion： Sitafloxacin may have good absorption, and it is possibly transported through the intes- tinal mucosa via a half passive diffusion-half carrier-mediated transport mechanism. The transport is also positively correlated to pH.

关 键 词：西他沙星 CACO-2细胞 转运 表观渗透系数 

分 类 号：R969.1[医药卫生—药理学]