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建立了液相色谱-串联质谱(LC-MS/MS)法测定犬血浆中的泮托拉唑(1)对映异构体,并应用于1在Beagle犬体内立体选择性药动学研究。采用d_5-1作内标,使用Lux Cellulose-4手性色谱柱。质谱采用电喷雾电离源(ESI源),多反应监测模式(MRM),监测离子对m/z 384.2→m/z 200.0(1)和m/z 389.1→m/z 205.1(d_5-1)。犬血浆样品中(S)-1和(R)-1在2~4 000 ng/ml范围内线性关系良好。Beagle犬立体选择性药动学研究结果表明,单独给药或以外消旋体给药时,(S)-1和(R)-1在Beagle犬体内的药动学行为基本一致。对映体单独给药后,血浆中未检测到其异构体,表明未发生构型转化。
The enantiomers of pantoprazole (1) in canine plasma were determined by liquid chromatography-tandem mass spectrometry (LC-MS / MS) and applied to the study of stereoselective pharmacokinetics in Beagle dogs. Using d_5-1 as an internal standard, a Lux Cellulose-4 chiral column was used. The mass spectra were monitored by electrospray ionization (ESI source), multiple reaction monitoring (MRM) and monitored ion pairs m / z 384.2 → m / z 200.0 (1) and m / z 389.1 → m / z 205.1 (d_5-1). There was a good linear relationship between (S) -1 and (R) -1 in dog plasma samples in the range of 2-4000 ng / ml. Beagle dog stereoselective pharmacokinetic study results show that, either singly administered or racemate administration, (S) -1 and (R) -1 in Beagle dogs pharmacokinetic behavior is basically the same. After enantiomers were administered alone, no isomers were detected in plasma, indicating that no conformational conversion occurred.