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

钱庆庆; 季闽春; 孙光春

doi:10.3969/j.issn.1006-0111.2018.05.013

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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

钱庆庆, 季闽春, 孙光春

文章导航 > 药学实践与服务 > 2018 > 36(5): 443-445,460

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]. 药学实践与服务, 2018, 36(5): 443-445,460. doi: 10.3969/j.issn.1006-0111.2018.05.013

引用本文:

QIAN Qingqing, JI Minchun, SUN Guangchun. Study on plasma concentration and pharmacoknetics of lamotrigine in cerebral ischemia model rats by LC-MS/MS[J]. Journal of Pharmaceutical Practice and Service, 2018, 36(5): 443-445,460. doi: 10.3969/j.issn.1006-0111.2018.05.013

Citation:

QIAN Qingqing, JI Minchun, SUN Guangchun. Study on plasma concentration and pharmacoknetics of lamotrigine in cerebral ischemia model rats by LC-MS/MS[J]. Journal of Pharmaceutical Practice and Service, 2018, 36(5): 443-445,460. doi: 10.3969/j.issn.1006-0111.2018.05.013

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

doi: 10.3969/j.issn.1006-0111.2018.05.013

复旦大学附属上海市第五人民医院药剂科, 上海 200240

基金项目: 上海市卫计委青年科研项目（20114Y018）

Study on plasma concentration and pharmacoknetics of lamotrigine in cerebral ischemia model rats by LC-MS/MS

Department of Pharmacy, Fifth People's Hospital of Shanghai Affiliated to Fudan University, Shanghai 200240, China

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c_max（1382.87±61.17）μg/L，t_1/2（40.43±6.77）h，AUC_0-∞（123.45±70.70）mg·h/L。全脑缺血损伤模型大鼠中药动学参数c_max（1 713.50±65.11）μg/L，t_1/2（73.72±17.46）h，AUC_0-∞（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t_1/2较长，血药浓度较高，可为后期药效学研究提供依据。
- 拉莫三嗪 /
- 液相色谱-串联质谱法 /
- 大鼠血浆 /
- 药动学
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,c_max (1 382.87±61.17) μg/L,t_1/2 (40.43±6.77) h; AUC_0-∞(123.45±70.70) mg·h/L. In model group, c_max(1 713.50±65.11) μg/L, t_1/2(73.72±17.46) h, AUC_0-∞(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 t_1/2 and higher concentration than that in shame-operated group, which is a valuable information for further pharmacodynamics study.
- lamotrigine(LTG) /
- LC-MS/MS /
- rat plasma /
- pharmacokinetic

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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

doi: 10.3969/j.issn.1006-0111.2018.05.013

复旦大学附属上海市第五人民医院药剂科, 上海 200240

基金项目: 上海市卫计委青年科研项目（20114Y018）

收稿日期: 2017-08-30
修回日期: 2018-09-03

关键词:

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c_max（1382.87±61.17）μg/L，t_1/2（40.43±6.77）h，AUC_0-∞（123.45±70.70）mg·h/L。全脑缺血损伤模型大鼠中药动学参数c_max（1 713.50±65.11）μg/L，t_1/2（73.72±17.46）h，AUC_0-∞（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t_1/2较长，血药浓度较高，可为后期药效学研究提供依据。