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同时测定比格犬体内的阿洛西林钠/舒巴坦钠及其药动学

Simultaneous determination of azlocillin sodium/sulbactam sodium in beagle dogs and the related study on pharmacokinetics
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摘要 目的注射用阿洛西林钠/舒巴坦钠(质量比为4∶1)中阿洛西林钠及舒巴坦钠在比格犬体内的药动学。方法比格犬给予受试制剂和参比制剂后,采用液相色谱-质谱联用法同时测定血浆中阿洛西林和舒巴坦的浓度。结果阿洛西林的主要药动学参数如下:ρmax分别为(119.34±25.27)mg·L-1和(140.64±28.48)mg·L-1;t1/2分别为(1.61±1.29)h和(1.85±1.91)h;AUC0-t分别为(61.62±15.30)mg·h·L-1和(64.97±13.70)mg·h·L-1;AUC0-∞分别为(65.22±15.72)mg·h·L-1和(68.93±15.37)mg·h·L-1;以AUC0-t计算,阿洛西林的相对生物利用度平均为(97.1±23.3)%;舒巴坦的主要药动学参数如下:ρmax分别为(47.30±15.57)mg·L-1和(41.97±14.19)mg·L-1;t1/2分别为(0.46±0.23)h和(0.53±0.35)h;AUC0-t分别为(26.82±7.49)mg·h·L-1和(23.67±6.05)mg·h·L-1;AUC0-∞分别为(28.05±8.59)mg·h·L-1和(25.50±8.61)mg·h·L-1;以AUC0-t计算,舒巴坦的相对生物利用度平均为(104.8±24.5)%。结论该方法适用于药动学研究。所得主要药动学参数表明,制剂间阿洛西林及舒巴坦的药动学参数AUC及ρmax均无显著性差异,两药组成复方后不影响各自在比格犬体内的药动学行为。 Objective To study pharmacokinetics of injective azlocillin sodium/sulbactam sodium(4:1) in beagle dogs.Methods A single intravenous at a dose of azlocillin sodium and sulbactam sodium was given to beagle dogs.Concentration was simultaneously determined by liquid chromatography-mass spectrometry method.Results The main pharmcokinetics parameters of azlocillin were as follows:ρmax were(119.34 ±25.27) mg·L-1and(140.64 ± 28.48) mg·L-1;t1/2were(1.61 ± 1.29) h and 和(1.85 ± 1.91) h;AUC0-twere(61.62 ± 15.30) mg·h·L-1and(64.97 ± 13.70) mg·h·L-1;AUC0-∞were(65.22 ±15.72) mg·h·L-1and(68.93 ± 15.37) mg·h·L-1;According to the calculation of AUC0-t,the relative bioavailability of Azlocillin is(97.1 ± 23.3) %.The main pharmcokinetics parameters of sulbactam were as follows:ρmaxwere(47.30 ± 15.57) mg·L-1and(41.97 ± 14.19) mg·L-1;t1/2were(0.46 ± 0.23) h and(0.53 ±0.35) h;AUC0-twere(26.82 ± 7.49) mg·h·L-1和(23.67 ±6.05) mg·h·L-1;AUC0-∞were(28.05 ±8.59)mg·h·L-1和(25.50 ±8.61)mg·h·L-1;According to the calculation of AUC0-t,the relative bioavailability of sulbactam is(104.8 ± 24.5) %.Conclusions This LC/MS method is simple,sensitive and accurate.It is suitable for injective azlocillin sodium/sulbactam sodium(4:1) pharmacokinetic study.There are no significant difference in pharmacokinetic parameters of AUC,Cmax and t1/2between the two agents of azlocillin and sulbactam.The compound preparation of the two drugs does not affect their dynamic behavior in beagle dogs.
出处 《沈阳药科大学学报》 CAS CSCD 北大核心 2014年第7期568-574,共7页 Journal of Shenyang Pharmaceutical University
关键词 阿洛西林钠 舒巴坦钠 高效液相色谱 质谱 药动学 azlocillin sodium sulbactam sodium HPLC/MS pharmacokinetics
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