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建立了液相色谱-串联质谱法测定Beagle犬血浆中的奈必洛尔。以苯海拉明为内标,采用电喷雾电离源正离子模式(ESI+)、多反应监测(MRM)进行定量分析。监测离子对m/z 406.2→m/z 151.0(奈必洛尔)和m/z 256.1→m/z 167.0(苯海拉明)。Beagle犬血浆中的奈必洛尔在40~10 000 pg/ml范围内线性关系良好,方法回收率为85.72%~108.8%,日内、日间RSD小于13.2%。6条Beagle犬空腹及餐后口服单剂量盐酸奈必洛尔片(5 mg)后的主要药动学参数分别为:cmax(2 897±712)和(3 714±1 209)pg/ml,t1/2(2.63±0.56)和(3.52±1.24)h,AUC0→t(9 710±2 643)和(11 892±3 547)pg·h·ml-1,AUC0→∞(9 922±2 716)和(12 329±3 330)pg·h·ml-1。结果表明饮食对奈必洛尔吸收程度有一定影响。
A liquid chromatography-tandem mass spectrometry was established for the determination of nebivolol in plasma of Beagle dogs. Diphenhydramine was used as internal standard, and electrospray ionization source positive ion mode (ESI +) and multiple reaction monitoring (MRM) were used for quantitative analysis. The monitored ion pair m / z 406.2 → m / z 151.0 (nebivolol) and m / z 256.1 → m / z 167.0 (diphenhydramine). The nebivolol in Beagle dog plasma had a good linearity in the range of 40-10 000 pg / ml. The recovery rate was 85.72% -108.8%. The intra-day and inter-day RSD was less than 13.2%. The main pharmacokinetic parameters of 6 Beagle dogs were: cmax (2897 ± 712) and (3714 ± 1 209) pg / ml after fasting and postprandial oral single dose of Nebivolol hydrochloride tablets (5 mg) AUC0 → ∞ (9 710 ± 2 643) and (11 892 ± 3 547) pg · h · ml-1, and AUC0 → ∞ (9 922 ± 2 716) and (12 329 ± 3 330) pg · h · ml-1. The results show that diet has a certain impact on the extent of Nebivolol absorption.