Department of Pharmacology, Faculty of Veterinary Medicine, Kasetsart University, Bangkok, Thailand.
Department of Veterinary Sciences, University of Pisa, San Piero a Grado, Italy.
J Vet Pharmacol Ther. 2022 Nov;45(6):501-507. doi: 10.1111/jvp.13080. Epub 2022 Jun 19.
The study evaluated the pharmacokinetic features of azithromycin (AZM) in 15 freshwater crocodiles (Crocodylus siamensis) in Thailand. The crocodiles were administered a single intramuscular (i.m.) injection of AZM at three different dosages of 2.5, 5, and 10 mg/kg body weight (b.w.). Blood samples were collected at pre-assigned times up to 168 h. The plasma concentrations of AZM were measured using a validated liquid chromatography-tandem mass spectrometry method. The plasma concentration of AZM were quantifiable for up to 168 h after i.m. administration at the three different dosages. A non-compartmental model was used to fit the plasma concentration of AZM versus the time curve for each crocodile. The elimination half-life values of AZM were 33.70, 38.11, and 34.80 h following i.m. injection after dosages of 2.5, 5, and 10 mg/kg b.w., respectively. There were no significant differences among groups. The results indicated that the overall rate of elimination of AZM in freshwater crocodiles was relatively slow. The maximum concentration and area under the curve from zero to the last values of AZM increased in a dose-dependent fashion. The average binding percentage of AZM to plasma protein was 48.66%. Based on the pharmacokinetic data, the susceptibility break-point and the surrogate PK-PD index (T > MIC), the intramuscular administration of AZM at a dose of 10 mg/kg b.w. might be appropriate for the treatment of susceptible bacterial infections (MIC < 4 μg/ml) in freshwater crocodiles.
本研究评估了阿奇霉素(AZM)在泰国 15 条暹罗鳄(Crocodylus siamensis)体内的药代动力学特征。鳄 鱼接受了三种不同剂量(2.5、5 和 10mg/kg 体重)的单次肌肉内(i.m.)注射 AZM。在预定时间内采集至 168 小时的血样。使用经过验证的液相色谱-串联质谱法测量 AZM 的血浆浓度。在三种不同剂量的 i.m.给药后,AZM 的血浆浓度可在长达 168 小时内定量。使用非房室模型拟合每个鳄鱼的 AZM 血浆浓度与时间曲线。AZM 的消除半衰期值分别为 2.5、5 和 10mg/kg b.w. 后 i.m. 注射后 33.70、38.11 和 34.80 小时,各组之间无显著差异。结果表明,AZM 在暹罗鳄体内的总体消除率相对较慢。AZM 的最大浓度和从 0 到最后值的曲线下面积呈剂量依赖性增加。AZM 与血浆蛋白的平均结合百分比为 48.66%。基于药代动力学数据、敏感性折点和替代 PK-PD 指数(T > MIC),10mg/kg b.w. 的肌肉内给药可能适合治疗暹罗鳄的易感细菌感染(MIC < 4μg/ml)。