液相色谱-串联质谱法测定全脑缺血损伤模型大鼠体内拉莫三嗪血药浓度及药动学研究
投稿时间:2017-08-30  修订日期:2018-09-03  点此下载全文
引用本文:钱庆庆,季闽春,孙光春.液相色谱-串联质谱法测定全脑缺血损伤模型大鼠体内拉莫三嗪血药浓度及药动学研究[J].药学实践杂志,2018,36(5):443~445,460
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作者单位E-mail
钱庆庆 复旦大学附属上海市第五人民医院药剂科, 上海 200240  
季闽春 复旦大学附属上海市第五人民医院药剂科, 上海 200240  
孙光春 复旦大学附属上海市第五人民医院药剂科, 上海 200240 SGC_hospital@yeah.net 
基金项目:上海市卫计委青年科研项目(20114Y018)
中文摘要:目的 建立液相色谱-串联质谱法(LC-MS/MS)测定大鼠血浆样品中拉莫三嗪浓度的方法,并进行药动学研究。方法 取12只SD大鼠,假手术组、脑缺血损伤模型组各6只,拉莫三嗪10 mg/kg灌胃,分别于5 min,0.25、0.5、1、2、4、6、8、12、24、36 h眼眶隐静脉丛取血,采用LC-MS/MS法测定其血药浓度,并用DAS软件计算药动学参数。结果 拉莫三嗪的药动学参数属于一级动力学两房室模型,拉莫三嗪在假手术大鼠体内的药动学参数cmax(1382.87±61.17)μg/L,t1/2(40.43±6.77)h,AUC0-∞(123.45±70.70)mg·h/L。全脑缺血损伤模型大鼠中药动学参数cmax(1 713.50±65.11)μg/L,t1/2(73.72±17.46)h,AUC0-∞(188.15±76.37)mg·h/L。结论 本方法适用于大鼠血浆中拉莫三嗪浓度的测定。假手术组和模型组大鼠拉莫三嗪灌胃后均于2 h达到峰值,但模型组拉莫三嗪的t1/2较长,血药浓度较高,可为后期药效学研究提供依据。
中文关键词:拉莫三嗪  液相色谱-串联质谱法  大鼠血浆  药动学
 
Study on plasma concentration and pharmacoknetics of lamotrigine in cerebral ischemia model rats by LC-MS/MS
Abstract:Objective To establish a sensitive method for determination of concentration of lamotrigine (LTG) in rat plasma and to study the pharmacokinetics by LC-MS/MS. Methods 12 rats were divided evenly into model group and shame-operated group. LTG was given as single dose of 10 mg/kg via intragastrical administration. Blood samples were collected from orbital saphenous venous plexus at 5 min,0.25,0.5,1,2,4,6,8,12,24 and 36 h after dosing. The LTG concentrations in rat plasma were assayed by LC-MS/MS. The pharmacokinetic parameters were calculated by DAS software. Results In shame-operated group,cmax (1 382.87±61.17) μg/L,t1/2 (40.43±6.77) h; AUC0-∞(123.45±70.70) mg·h/L. In model group, cmax(1 713.50±65.11) μg/L, t1/2(73.72±17.46) h, AUC0-∞(188.15±76.37) mg·h/L. Conclusion The method is proved to be suitable for the determination of LTG in rat plasma. LTG concentration reached peak value at 2 h in both groups. However, model group had a longer t1/2 and higher concentration than that in shame-operated group, which is a valuable information for further pharmacodynamics study.
keywords:lamotrigine(LTG)  LC-MS/MS  rat plasma  pharmacokinetic
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