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丹氟沙星在静脉注射和肌肉注射给药后在褐鳟(Salmo trutta fario)中的血浆和组织分布。

Plasma and tissue disposition of danofloxacin in brown trout (Salmo trutta fario) after intravenous and intramuscular administrations.

机构信息

a Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine , University of Kastamonu , Kastamonu , Turkey.

b Department of Pharmacology and Toxicology, Faculty of Veterinary Medicine , University of Selcuk , Konya , Turkey.

出版信息

Food Addit Contam Part A Chem Anal Control Expo Risk Assess. 2018 Dec;35(12):2340-2347. doi: 10.1080/19440049.2018.1530458. Epub 2018 Oct 23.

DOI:10.1080/19440049.2018.1530458
PMID:30352010
Abstract

Plasma and muscle pharmacokinetics of danofloxacin were investigated after 10 mg/kg intravenous (IV, caudal vein) and intramuscular (IM, right epaxial muscles) administrations in 168 healthy brown trout (Salmo trutta fario) at 10°C-13°C. High-performance liquid chromatography was used to determine its plasma and muscle concentrations. Pharmacokinetic parameters were analysed with a non-compartmental model. After IV administration, elimination half-life (t), area under the concentration-time curve (AUC), mean residence time (MRT), volume of distribution at steady state, total body clearance in plasma and AUC/AUC ratio were 22.22 h, 140.66 hµg/mL, 23.15 h, 2.28 L/kg, 0.07 L/h/kg and 3.79, respectively. After IM administration, t, AUC, MRT, peak concentration (C), time to reach C, bioavailability in plasma and AUC/AUC ratio were 28.28 h, 84.39 hµg/mL, 37.31 h, 4.79 µg/mL, 1 h, 59.99% and 8.46, respectively. Danofloxacin exhibited long t and good bioavailability after IM administration. Therefore, 10 mg/kg IM administration of danofloxacin in brown trout can provide AUC/MIC of > 125 and C/MIC of > 10 to treat diseases caused by susceptible bacteria with ≤ 0.336 µg/mL MIC.

摘要

在 10°C-13°C 下,168 条健康的褐鳟(Salmo trutta fario)静脉(尾静脉)和肌肉(右侧背鳍肌)内分别注射 10mg/kg 的达氟沙星后,研究了其血浆和肌肉药代动力学。采用高效液相色谱法测定其血浆和肌肉浓度。采用非房室模型分析药代动力学参数。静脉注射后,消除半衰期(t)、浓度-时间曲线下面积(AUC)、平均驻留时间(MRT)、稳态分布容积、血浆总清除率和 AUC/AUC 比值分别为 22.22 h、140.66 hµg/mL、23.15 h、2.28 L/kg、0.07 L/h/kg 和 3.79。肌肉内注射后,t、AUC、MRT、峰浓度(C)、达到 C 的时间、血浆生物利用度和 AUC/AUC 比值分别为 28.28 h、84.39 hµg/mL、37.31 h、4.79 µg/mL、1 h、59.99%和 8.46。达氟沙星肌肉内注射后 t 长,生物利用度好。因此,褐鳟肌肉内注射 10mg/kg 的达氟沙星,可提供 AUC/MIC 大于 125 和 C/MIC 大于 10,以治疗敏感菌引起的疾病,MIC 为≤0.336µg/mL。

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