Yang F, Yang F, Wang G, Shi W, Kong T, Yang P, Bai D, Zhou B
College of Animal Science and Technology, Henan University of Science and Technology, Luoyang, China.
Jiangxi Bolai Pharmacy Co., Ltd., Jiujiang, China.
J Vet Pharmacol Ther. 2018 Aug;41(4):599-604. doi: 10.1111/jvp.12495. Epub 2018 Feb 21.
The pharmacokinetics of orbifloxacin was studied after a single dose (7.5 mg/kg) of intravenous or intramuscular administration to crucian carp (Carassius auratus) reared in freshwater at 25°C. Plasma samples were collected from six fish per sampling point. Orbifloxacin concentrations were determined by high-performance liquid chromatography with a 0.02 μg/ml limit of detection, then were subjected to noncompartmental analysis. After intravenous injection, initial concentration of 5.83 μg/ml, apparent elimination rate constant (λ ) of 0.039 hr , apparent elimination half-life (T ) of 17.90 hr, systemic total body clearance (Cl) of 75.47 ml hr kg , volume of distribution (Vz) of 1,948.76 ml/kg, and volume of distribution at steady-state (Vss) of 1,863.97 ml/kg were determined, respectively. While after intramuscular administration, the λ , T , mean absorption time (MAT), absorption half-life (T ), and bioavailability were determined as 0.027 hr , 25.69, 10.26, 7.11 hr, and 96.46%, respectively, while the peak concentration was observed as 3.11 ± 0.06 μg/ml at 2.0 hr. It was shown that orbifloxacin was completely but relatively slowly absorbed, extensively distributed, and slowly eliminated in crucian carp, and an orbifloxacin dosage of 10 mg/kg administered intravenously or intramuscularly would be expected to successfully treat crucian carp infected by strains with MIC values ≤0.5 μg/ml.
在25°C淡水中饲养的鲫鱼(Carassius auratus)静脉注射或肌肉注射单剂量(7.5毫克/千克)奥比沙星后,对其药代动力学进行了研究。每个采样点从6条鱼中采集血浆样本。采用高效液相色谱法测定奥比沙星浓度,检测限为0.02微克/毫升,然后进行非房室分析。静脉注射后,分别测定初始浓度为5.83微克/毫升、表观消除速率常数(λ)为0.039小时⁻¹、表观消除半衰期(T½)为17.90小时、全身总体清除率(Cl)为75.47毫升·小时⁻¹·千克⁻¹、分布容积(Vz)为1948.76毫升/千克以及稳态分布容积(Vss)为1863.97毫升/千克。而肌肉注射后,λ、T½、平均吸收时间(MAT)、吸收半衰期(Tₐ)和生物利用度分别测定为0.027小时⁻¹、25.69小时、10.26小时、7.11小时和96.46%,同时在2.0小时观察到峰值浓度为3.11±0.06微克/毫升。结果表明,奥比沙星在鲫鱼体内吸收完全但相对缓慢,分布广泛且消除缓慢,静脉注射或肌肉注射10毫克/千克的奥比沙星剂量有望成功治疗感染MIC值≤0.5微克/毫升菌株的鲫鱼。