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人血浆中茴拉西坦代谢物的HPLC-MS测定及药物动力学研究 被引量:2

Determination of Metabolite of Aniracetam and Pharmacokinetics in Human Plasma by HPLC-MS
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摘要 建立了HPLC-MS法测定人血浆中茴拉西坦代谢产物对甲氧基苯甲酰胺基丁酸(2)的浓度。以N,N-二甲基-3,4-亚甲氧基苯乙胺(3)为内标,采用Thermo C18色谱柱,流动相为30mmol/L乙酸铵溶液(含0.5%甲酸和0.01%三氟乙酸)-乙腈(84:16),HPLC-MS采用ESI+电离源,选择正离子检测模式,检测的离子为m/z 135(2,M+H)和163(3,M+ H)。2在0.058~14.03μg/ml浓度范围内线性良好,回收率在90%以上。18名健康志愿者口服茴拉西坦胶囊0.2g后的药动学参数AUC0→t、AUC0→∞、tmax、Cmax和t1/2分别为(9.21±1.72)μg·h·ml-1、(9.30±1.75)μg·h·ml-1、(0.47±0.11)h、(9.44±2.13)μg/ml和(0.66±0.10)h。 A HPLC-MS method for determination of metabolite of aniracetam -- p-anisamidobutyric acid (2) in human plasma was established. N,N-Dimethyl-3,4-methylenedioxy-methamphetamine (3) was used as internal standard. A Thermo C18 column was used with the mobile phase of 30mmol/L ammonium acetate solution (containing 0.5 % formic acid and 0.01% trifluoroacetic acid) -acetonitrile (84: 16). The analytes were ionized in the electro spray ionization (ESI^+) ion source of the mass spectrometer and detected in the selected ion monitoring (SIM) mode. SIM ions were m/z 135 (M+H) for 2 and 163 (M+H) for 3. The calibration curve of 2 A was linear in range of 0.058 - 14.03μg/ml. The recovery was above 90%. Eighteen volunteers were orally administrated 0.2g of aniracetam, the pharmacokinetic parameters were A UC0→t (9.21 ± 1.72) μg·h·ml^-1, AUC0→∞= (9.30 ± 1.75) μg·h·ml^-1, tmax (0.47 ± 0.11 ) , Cmax (9.44 ± 2.13) μg·ml^- 1 and t1/2 (0.66 ± 0.10) h, respectively.
出处 《中国医药工业杂志》 CAS CSCD 北大核心 2006年第6期418-420,共3页 Chinese Journal of Pharmaceuticals
关键词 茴拉西坦 对甲氧基苯甲酰胺基丁酸 N N-二甲基-3 4-亚甲氧基苯乙胺 高效液相色谱-质谱 测定 药物动力学 aniracetam p-anisamidobutyric acid N,N-dimethyl-3,4-methylenedioxy-metharnphetamine HPLC-MS determination pharmacokinetics
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