埃索美拉唑对奥希替尼在大鼠体内药动学的影响

The Effect of Esomeprazole on the Pharmacokinetics of Osimertinib in Rats

目的:探讨埃索美拉唑对奥希替尼在大鼠体内药动学的影响。方法:将12只大鼠随机分两组,一组给予超纯水,另一组给予埃索美拉唑溶液(10mg·kg-1),连续给药5天,第6天给两组大鼠灌胃给予奥希替尼(5mg·kg-1),于给药后不同时间点采集血样,采用HPLC法测定血浆中奥希替尼的含量,计算药动学参数,研究埃索美拉唑对奥希替尼在大鼠体内药动学的影响。结果:体内研究发现,埃索美拉唑并未显著降低奥希替尼的AUC(0-∞)、Cmax和Tmax。结论:埃索美拉唑并未影响奥希替尼在大鼠体内的吸收,对PPIs类药物会影响p H依赖性药物体内吸收的研究有一定的意义。

Objective:To make an investigation with regards to the effect of Esomeprazole on the pharmacokinetics of Osimertinib in Wistar rats.Methods:Twelve Wistar rats were divided into Osimertinib+pure water group and Osimertinib+Esomeprazole(l0mg·kg-1).Plasma concentration of Osimertinib was determined by HPLC.Results:In-vivo,the main pharmacokinetic parameters AUC(0-∞)、Cmax and Tmax were not decreased significantly.Conclusion:The oral absorption of Osimertinib was not inhibited obviously by Esomeprazole,which had certain significance on the effect of oral absorption of pH-dependent drugs by PPIs.