达泊西汀在MDCKII/MDCKII-BCRP细胞模型上的跨膜转运机制
Study on the transmembrane transport mechanism of Dapoxetine on the MDCKII/MDCKII-BCRP cell lines
作者：李瑞娜;张晞倩;李蓉;王凌;蒋学华;
Author：
收稿日期： 年卷（期）页码：2018,33(05):-507-510
期刊名称：华西药学杂志
Journal Name：WEST CHINA JOURNAL OF PHARMACEUTICAL SCIENCES
关键字：达泊西汀;MDCKII-BCRP细胞;人乳腺癌耐药蛋白;机制;跨膜转运;双向转运实验;表观渗透系数;外排率;抑制剂;净外排率;不良反应
Key words：
基金项目：
中文摘要
目的研究达泊西汀在MDCKII/MDCKII-BCRP单层细胞模型中的跨膜转运机制。方法应用MDCKII和MDCKIIBCRP单层细胞模型,在改变转运温度、达泊西汀转运浓度以及是否存在抑制剂的条件下,比较达泊西汀的表观渗透系数(P_(app))、外排率(ER)、净外排率(NER)。结果随着温度下降以及人乳腺癌耐药蛋白(BCRP)抑制剂的加入,达泊西汀的NER值从2. 1分别降到1. 0、1. 1;4～16μmol·L~(-1)达泊西汀给药后,其NER值先高于1. 5,后降至1. 5以下。结论达泊西汀是BCRP的底物,应注意达泊西汀与其他BCRP抑制剂共服用可能会产生药物相互作用,增加其不良反应发生的风险。
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