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RP/HPLC测定吡虫啉血药浓度及其大鼠灌胃药代动力学评价
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龚小见,苏敏,赵超,周欣 1.贵州师范大学贵州省山地环境信息系统与生态环境保护重点实验室2.贵州师范大学贵州省药物质量控制及评价技术工程实验室3.贵州师范大学天然药物质量控制研究中心 
基金项目:贵州省高层次创新人才培养项目(黔科合人才(2015)4033号)
中文摘要:建立了大鼠血浆中吡虫啉的反相高效液相色谱(RP/HPLC)分析方法,并用于吡虫啉在大鼠体内的代谢动力学行为及特征研究。血浆样品经甲醇萃取,反相HPLC法测定血浆中的吡虫啉浓度。色谱柱为Agilent ZORBAX C18柱(4.6 mm×250 mm,5 μm ),流动相为甲醇-水(30∶70),进样量20 μL,检测波长245 nm,流速1.0 mL/min。在最佳条件下,吡虫啉的线性范围为0.5~100 mg·L-1(r2=0.999 8),检出限为10 μg·L-1,平均加标回收率为74.7%。大鼠单剂量灌胃给予 68.1 mg·kg-1吡虫啉,分别测定给药后不同时间下血浆中吡虫啉的浓度,并计算代谢动力学参数。灌胃给药后吡虫啉的Cmax为23.557 mg/L,tmax为7.333 h,t1/2α为4.472 h,AUC(0-t)为276.727 mg·h/L。代谢动力学结果显示,吡虫啉在大鼠体内呈二隔室模型分布,以一级药代动力学方式消除。该方法简便可靠,能够满足血浆中吡虫啉测定及药代动力学研究的要求。
中文关键词:吡虫啉  药代动力学  反相高效液相色谱(RP/HPLC)
 
Determination of Imidacloprid in Rats Plasma by RP/HPLC and Its Pharmacokinetics in Rats Receiving Intragastric Administration
Abstract:A reversed phase high performance liquid chromatographic(RP/HPLC) method was established for the determination of imidacloprid in rat plasma,which was used to investigate the imidacloprids pharmacokinetics in rats by intragastric administration.The plasma sample was extracted with methanol,then determined by RP/HPLC.The sample was separated on a C18 column(4.6 mm×250 mm,5 μm ) with a mobile phase of methanol-water(30∶70) at a flow rate of 1.0 mL·min-1,and detected at a wavelength of 245 nm.The imidacloprid concentration in plasma was detected at predetermined time intervals after SD rats were intragastrically given a single dose of lutein suspension at 68.1 mg·kg-1,then the concentration time curve was plotted and the pharmacokinetic parameters were calculated.The main parameters for intragastric administration were follows:Cmax=23.557 mg/L,tmax=7.333 h,t1/2α=4.472 h,AUC(0-t)=276.727 mg·h/L.There was a linear relationship for imidacloprid (r2=0.999 8) in the concentration range of 0.5-100 mg·L-1 with a detection limit of 10 μg·L-1.The average recovery for the analyte was 74.7%.The pharmacokinetic results in rats showed that imidacloprid was distributed in two compartment models in rats,and eliminated by the first order pharmacokinetics.The method was simple and reliable,and could satisfy the requirements for the detection of imidacloprid and its pharmacokinetic study in rat plasma.
Key Words:imidacloprid  pharmacokinetics  reversed phase high performance liquid chromatography(RP/HPLC)
引用本文:龚小见,苏敏,赵超,周欣.RP/HPLC测定吡虫啉血药浓度及其大鼠灌胃药代动力学评价[J].分析测试学报,2018,37(12):1500-1503.
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