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目的考察Beagle犬体内阿奇霉素药动学行为,为临床合理用药提供参考。方法 Beagle犬分别按照不同给药方式给予阿奇霉素制剂:1日给药(750 mg每日给药2次,总剂量为1.5 g)和连续给药3日,(500 mg每日给药1次,总剂量为1.5 g),采用液相色谱-质谱联用法测定血浆中阿奇霉素的药物浓度。结果阿奇霉素的主要药动学参数如下:ρmax分别为(3.04±1.16)和(2.44±1.99)mg·L~(-1);tmax分别为(1.06±0.55)和(1.03±0.88)h;t1/2分别为(28.64±2.51)和(36.65±17.89)h;AUC0-t分别为(110.83±49.67)和(96.77±31.16)mg·h·L~(-1);AUC0-∞分别为(121.59±53.93)和(112.75±39.81)mg·h·L~(-1);以AUC0-t计算,阿奇霉素的相对生物利用度平均为(120.8±55.0)%。结论 2组间阿奇霉素的AUC、ρmax无统计学差异(P>0.05),可采用大剂量的给药方案。
Objective To investigate the pharmacokinetics of azithromycin in Beagle dogs and to provide a reference for clinical rational drug use. Methods Beagle dogs were given azithromycin according to different administration modes: 1 day (750 mg twice daily, 1.5 g total dose) and 3 consecutive days (500 mg once daily, The total dose was 1.5 g). The plasma concentration of azithromycin was determined by liquid chromatography-mass spectrometry. Results The main pharmacokinetic parameters of azithromycin were as follows: ρmax were (3.04 ± 1.16) and (2.44 ± 1.99) mg · L -1; tmax was 1.06 ± 0.55 and 1.03 ± 0.88 h respectively; t1 / 2 were (28.64 ± 2.51) and (36.65 ± 17.89) h respectively; AUC0-t was (110.83 ± 49.67) and (96.77 ± 31.16) mg · h · L -1, respectively; AUC0- 121.59 ± 53.93 and 112.75 ± 39.81 mg · h · L -1, respectively. The relative bioavailability of azithromycin was (120.8 ± 55.0)% with AUC0-t. Conclusion There was no significant difference in the AUC and ρmax of azithromycin between the two groups (P> 0.05).