替米沙坦在Caco-2细胞模型中体外转运研究.pdfVIP

替米沙坦在Caco一2细胞模型中的体外转运研究 沈 杰1’。，焦 正2，李中东2，施孝金2，童如镜1，钟明康2 (1．上海市华东医院药剂科，上海200040；2复旦大学附属华山医院药剂科，上海 200040) [关键词] 替米沙坦；Caco一2细胞；P糖蛋白；吸收 [摘要] 转运的影响。结果：TMS在Caco一2细胞中的转运存在外排作用，并且外排作用随着浓度的增加趋于饱和； 从吸收机制上初步解释了P—gP的外排作用可能是TMS生物利用度低，个体差异大的原因。 characteristicsoftelmisartaninthehumanintestinalcelllineCaco-2 Transport SHEN Jiel，一，JIAO Zhen92，LIZhong—don92，SHIXiao—jin2，TONGRu—jin91，ZHONGMing—kan92 ofPharmacy，Huadong 200040，China；2．Departmentof (1．Department Hospital，SHANGHAI han Univemity，SHANGHAI200040，China) Hospital，Fudan [KEYWORDS]telmisartan；Caco一2 cell；P—glycoprotein；absorption in humanintestinal the oftelmisartanvitro．METHODS：A [ABSTRACT]AIM：Tostudy characteristics transport cellCaco-2modelinvitroculturedbeen to characteristicsoftelmisartan． epithelial had appliedstudythe舰nsport Theeffectsof and onthe oftelmisartanwereinves— concentration，pHP—glycoprotein(P—gP)inhibitorstransport of was was theCaco一2 TMS andthe ceHs，the pH transport tigated．RESULTS：In absorptivetransport dependent enhancedat acidiconthe side．The of to basolater- weakly pH apical apical comparison alto showedthateffluxeffects limittheoral ofTMS．Inthe apical(BL—AP)transports might absorption presence ofamioderone(10 irdaibitorsof Pratiowasdecreased txmol／L)andCyclosporin(10p。mol／L)，potent P—gP，the data that