Sumano Hector, Ocampo Luis, Tapia Graciela, Mendoza Corazon de Jesus, Gutierrez Lilia
Departments of Physiology and Pharmacology, National Autonomous University of Mexico (UNAM), Mexico City 04510, Mexico.
Departments of Genetics and Biostatistics, National Autonomous University of Mexico (UNAM), Mexico City 04510, Mexico.
J Vet Sci. 2018 Sep 30;19(5):600-607. doi: 10.4142/jvs.2018.19.5.600.
Pharmacokinetic/pharmacodynamic (PK/PD) ratios of reference enrofloxacin (Enro-R) and enrofloxacin as HCl-2HO (Enro-C), as well as Monte Carlo simulations based on composite MIC and MIC (MIC, minimum inhibitory concentration) spp., were carried out in dogs after their intramuscular (IM) or oral administration (10 mg/kg). Plasma determination of enrofloxacin was achieved by means of high-performance liquid chromatography. Maximum plasma concentration values after oral administration were 1.47 ± 0.19 μg/mL and 5.3 ± 0.84 μg/mL for Enro-R and Enro-C, respectively, and 1.6 ± 0.12 μg/mL and 7.6 ± 0.93 μg/mL, respectively, after IM administration. Areas under the plasma . time concentration curve in 24 h (AUC) were 8.02 μg/mL/h and 36.2 μg/mL/h for Enro-R and Enro-C, respectively, and 8.55 ± 0.85 μg/mL/h and 56.4 ± 6.21 μg/mL/h after IM administration of Enro-R and Enro-C, respectively. The PK/PD ratios and Monte Carlo simulations obtained with Enro-C, not Enro-R, indicated that its IM administration to dogs will result in therapeutic concentrations appropriate for treating leptospirosis. This is the first time enrofloxacin has been recommended to treat this disease in dogs.
对参比恩诺沙星（Enro-R）和盐酸二水恩诺沙星（Enro-C）的药代动力学/药效学（PK/PD）比率，以及基于复合MIC和MIC（MIC，最低抑菌浓度）的蒙特卡洛模拟，在犬只肌肉注射（IM）或口服给药（10 mg/kg）后进行了研究。恩诺沙星的血浆测定通过高效液相色谱法完成。口服给药后，Enro-R和Enro-C的最大血浆浓度值分别为1.47±0.19 μg/mL和5.3±0.84 μg/mL，肌肉注射后分别为1.6±0.12 μg/mL和7.6±0.93 μg/mL。血浆浓度-时间曲线下24小时面积（AUC），Enro-R和Enro-C分别为8.02 μg/mL/h和36.2 μg/mL/h，Enro-R和Enro-C肌肉注射后分别为8.55±0.85 μg/mL/h和56.4±6.21 μg/mL/h。用Enro-C而非Enro-R获得的PK/PD比率和蒙特卡洛模拟表明，对犬只进行肌肉注射将产生适合治疗钩端螺旋体病的治疗浓度。这是首次推荐恩诺沙星用于治疗犬只的这种疾病。
