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目的建立测定大鼠血浆中具栖冬青苷浓度的液相质谱联用(LC-MS)法。方法雄性SD大鼠8只,尾静脉注射具栖冬青苷2.86 mg·只~(-1),于指定时间眼眶采血,并用LC-MS法测定血浆中具栖冬青苷的浓度。色谱柱为ZORBAX SB-C_(18)柱(2.1 mm×150 mm,5μm),以乙腈和0.1%甲酸+2 mmol·L~(-1)醋酸铵水溶液(80∶20,V/V)为流动相。离子化方式为电喷雾(ESI),负离子方式检测,具栖冬青苷[M-H]~+,m/z 649.6,替硝唑[M-H]~+,m/z 248.1。采用DAS 2.0软件对其药动学参数进行统计分析。结果具栖冬青苷在大鼠体内呈二室模型分布,主要药动学参数:tβ为(5.20±0.14)h,CL为(51.07±0.22)L·h~(-1)·kg~(-1),ρmax为(22.68±0.72)μg·L~(-1),V_d为(2 355.69±1.68)L·kg~(-1)。结论该方法灵敏度较高,可用于具栖冬青苷在大鼠血浆中的检测及药动学分析。
Objective To establish a liquid chromatography-mass spectrometry (LC-MS) method for the determination of avermectins in rat plasma. Methods Eight male Sprague-Dawley rats were injected intravenously with 2.86 mg · L -1 of benthonicidin at the designated time, and blood samples were collected from the orbital of the rats at the indicated time points. Plasma concentrations of the caridin were determined by LC-MS. The column was composed of ZORBAX SB-C 18 column (2.1 mm × 150 mm, 5 μm) with acetonitrile and 0.1% formic acid and 2 mmol·L -1 ammonium acetate aqueous solution (80:20, V / V) Mobile phase. The ionization mode was electrospray ionization (ESI) and negative ion mode detection. Hesperidin [M-H] ~ +, m / z 649.6, tinidazole [M-H] ~ +, m / z 248.1. The pharmacokinetic parameters were analyzed by DAS 2.0 software. Results There was a two compartment model distribution in the rat model. The main pharmacokinetic parameters were t (5.20 ± 0.14) h, CL (51.07 ± 0.22) L · h ~ (-1) · kg ~ (- 1), ρmax was (22.68 ± 0.72) μg · L -1, V_d was (2 355.69 ± 1.68) L · kg -1. Conclusion The method is sensitive and can be used for the determination and pharmacokinetic analysis of Aconitin in rat plasma.