直线加速器单次照射对卡培他滨体内代谢过程的影响  

Effect of Single-pass Linear Accelerator Radiation on Metablism of Capecitabine in vivo

作　　者：王若琪 李建华 王志鹏 刘欢[1] 张国良 高洁 Wang Ruoqi;Li Jianhua;Wang Zhipeng;Liu Huan;Zhang Guoliang;Gao jie(GLP Center,China Institute for Radiation Protection,Taiyuan,Shanxi 030006;Bethune Hospital of Shanxi Province,Taiyuan,Shanxi 030032)

机构地区：[1]中国辐射防护研究院GLP中心,太原030006 [2]山西白求恩医院肿瘤中心,太原030032

出　　处：《辐射防护通讯》2021年第5期39-43,共5页Radiation Protection Bulletin

基　　金：中国辐射防护研究院院青年基金项目。

摘　　要：采用直线加速器单次照射SD大鼠,检测卡培他滨、5-氟尿嘧啶血药浓度和肠单向灌流流出物中卡培他滨浓度,计算C_(max)、T_(max)、t_(1/2)、AUC和吸收速率常数和药物表观吸收系数。结果表明:(1)分析方法操作简单,可重复性高,可同时测定大鼠血浆样品中原型药物卡培他滨及活性代谢物5-氟尿嘧啶;(2)直线加速器腹部10 Gy单次照射,抑制了卡培他滨在小肠和结肠部位的吸收,导致达峰时间推迟,峰浓度和血药浓度降低,同时排泄加快;没有影响卡培他滨代谢速率。The concentration of capecitabine and 5-fluorouracil in blood and the concentration of capecitabine in the intestinal single-pass perfusion effluent were tested by UPLC-MS/MS after single exposure of SD rats by linear accelerator.C_(max),T_(max),t_(1/2),AUC,absorption rate constant(K_(a))and apparent absorption coefficient(P_(app))were then calculated.It showes that the testing method is simple and reproducible,and can simultaneously determine the prototype drug capecitabine and active metabolite 5-fluorouracil in rat plasma.Our analysis indicate that the single exposure of 10 Gy in the abdomen of linear accelerator has inhibited the absorption of capecitabine into the blood circulation in the small intestine and colon,resulting in delayed peak reaching time,decreased peak concentration and blood drug concentration,and accelerated excretion,while capecitabine metabolic rate hasn’tbeen affected.

关 键 词：直线加速器 卡培他滨 代谢 液相色谱-串联质谱法 

分 类 号：R818[医药卫生—放射医学]