The aim of the present study was to elucidate the pharmacokinetic profiles of amoxicillin trihydrate (AMX) in Siamese freshwater crocodiles (Crocodylus siamensis ). Crocodiles were administered a single intramuscular injection of AMX, at a dose of either 5 or 10 mg/kg body weight (b.w.). Blood samples were collected at preassigned times up to 120 hr. The plasma concentrations of AMX were measured using a validated liquid chromatography tandem‐mass spectrometry method. AMX plasma concentrations were quantifiable for up to 72 hr (5 mg/kg b.w.) and 96 hr (10 mg/kg b.w.). The elimination half‐life (t_1/2λz) of AMX following dosing at 5 mg/kg b.w. (8.72 ± 0.61 hr) was almost identical to that following administration at 10 mg/kg b.w (8.98 ± 1.13 hr). The maximum concentration and area under the curve from zero to the last values of AMX increased in a dose‐dependent fashion. The average binding percentage of AMX to plasma protein was 21.24%. Based on the pharmacokinetic data, susceptibility break point, and the surrogate PK‐PD index (T > MIC, 0.25 μg/ml), intramuscular administration of AMX at dose of 5 mg/kg b.w. every 4 days might be appropriate for the treatment of susceptible bacterial infections in freshwater crocodiles.

中文翻译：

---

肌肉内给药两次后，阿莫西林三水合物在淡水鳄鱼（Crocodylus siamensis）中的药代动力学特征。

本研究的目的是阐明三水阿莫西林（AMX）在暹罗淡水鳄鱼（Crocodylus siamensis）中的药代动力学特征。鳄鱼肌肉注射AMX单次注射，剂量为5或10 mg / kg体重（bw）。在预先指定的时间（最多120小时）收集血液样本。使用经过验证的液相色谱串联质谱法测量AMX的血浆浓度。AMX血浆浓度可长达72小时（5 mg / kg bw）和96小时（10 mg / kg bw）定量。消除半衰期（T _{1 /2λ ž}）以5 mg / kg bw（8.72±0.61 hr）给药后的AMX）与以10 mg / kg bw（8.98±1.13 hr）给药后的AMX几乎相同。从AMX的零值到最后值的最大浓度和曲线下面积以剂量依赖的方式增加。AMX与血浆蛋白的平均结合百分比为21.24％。根据药代动力学数据，药敏点和替代PK-PD指数（T> MIC，0.25μg/ ml），每4天5 mg / kg bw的肌内注射AMX可能适合治疗淡水鳄鱼中易感细菌感染。