艾司奥美拉唑对柳氮磺吡啶在大鼠体内药动学行为的影响
x

请在关注微信后,向客服人员索取文件

篇名: 艾司奥美拉唑对柳氮磺吡啶在大鼠体内药动学行为的影响
TITLE: Effects of Esomeprazole on Pharmacokinetic Behavior of Sulfasalazine in Rats
摘要: 目的:建立测定大鼠血浆中柳氮磺吡啶(SSZ)代谢产物磺胺吡啶(SP)浓度的方法,并探讨艾司奥美拉唑(ESOM)对SSZ在大鼠体内药动学行为的影响。方法:将雄性SD大鼠随机分为SSZ组和SSZ+ESOM组,每组6只。SSZ+ESOM组大鼠连续灌胃艾司奥美拉唑肠溶片[90mg/(kg·d)]14天;第15天时,两组大鼠单次灌胃柳氮磺吡啶肠溶片(90mg/kg),并在给药后0.5、1、1.5、2、3、4、6、8、10、12、24、36、48、72h时于其眼内眦取血。血浆经甲醇沉淀蛋白后,以地西泮为内标,以AgilentXDR-C18为色谱柱,以甲醇-0.1%甲酸溶液(梯度洗脱)为流动相,采用液相色谱-串联质谱法检测血浆中SSZ代谢产物SP的浓度;采用DAS3.0.1软件计算药动学参数并进行组间比较。结果:SP检测质量浓度的线性范围为2~1000ng/mL,方法学考察结果符合《中国药典》相应要求。SSZ+ESOM组和SSZ组大鼠体内SP的AUC0-t、tmax、t1/2z、cmax、MRT0-t等药动学参数比较,差异均无统计学意义(P>0.05)。结论:所建方法简便、快速、灵敏度高,可用于血浆中SSZ代谢产物SP浓度的检测;ESOM对SSZ在大鼠体内的药动学行为无明显影响。
ABSTRACT: OBJECTIVE:To develop a metho d for determining the plasma concentration of sulfasalazine (SSZ)metabolite sulfapyridine(SP)in rats ,and to investigate the effects of esomeprazole (ESOM)on the pharmacokinetic behavior of SSZ in rats. METHODS:Male SD rats were randomly divided into SSZ group and SSZ+ESOM group ,with 6 rats in each group. SSZ+ESOM group were given Esomeprazole enteric-coated tablets [ 90 mg/(kg·d)] intragastrically for 14 days. On the 15th day ,the rats in 2 groups were given Sulfasalazine enteric coated tablets (90 mg/kg)intragastrically,and blood sample was collected from the inner canthus at 0.5,1,1.5,2,3,4,6,8,10,12,24,36,48,72 h after administration. After protein precipitation with methanol , using diazepam as internal standard ,Agilent XDR-C 18 column was adopted with methanol- 0.1% formic acid solution (gradient elution)as mobile phase. The concentration of SSZ metabolite SP in plasma was determined by LC-MS/MS. The pharmacokinetic parameters were calculated by using DAS 3.0.1 software and compared between 2 groups. RESULTS :The linear range of SP were 2-1 000 ng/mL. The methodology met the requirements of Chinese Pharmacopeia . There was no statistical significance in pharmacokinetic parameters of SP between 2 groups,such as AUC 0-t,tmax,t1/2z,cmax,MRT0-t(P>0.05). CONCLUSIONS :The established method is simple ,rapid and sensitive ;it can be used for the concentration determination of SSZ metabolite SP in plasma. ESOM has no significant effect on the pharmacokinetic behavior of SSZ in rats.
期刊: 2021年第32卷第13期
作者: 贾茹,魏世杰,张文萍,买淑霞,蒋韶婓,党宏万
AUTHORS: JIA Ru,WEI Shijie,ZHANG Wenping ,MAI Shuxia ,JIANG Shaofei ,DANG Hongwan
关键字: 柳氮磺吡啶;磺胺吡啶;艾司奥美拉唑;液相色谱-串联质谱法;药动学行为
KEYWORDS: Sulfasalazine;Sulfapyridine;Esomeprazole;LC-MS/MS;Pharmacokinetic behavior
阅读数: 261 次
本月下载数: 15 次

* 注:未经本站明确许可,任何网站不得非法盗链资源下载连接及抄袭本站原创内容资源!在此感谢您的支持与合作!