Gao Tiantian, Liu Xuesong, Qiu Di, Li Yanan, Qiu Zongsheng, Qi Jingjing, Li Shuxin, Guo Xiaoyan, Zhang Yan, Wang Ziqi, Gao Xiang, Ma Yuhui, Ma Tianwen
Heilongjiang Key Laboratory for Laboratory Animals and Comparative Medicine, College of Veterinary Medicine, Northeast Agricultural University, Harbin 150030, China.
Heilongjiang Province Key Laboratory of Veterinary Drugs, Branch of Animal Husbandry and Veterinary of Heilongjiang Academy of Agricultural Sciences, Qiqihar 161005, China.
Vet Sci. 2025 Mar 22;12(4):294. doi: 10.3390/vetsci12040294.
Cefquinome is used to treat septicemia caused by () and respiratory infections caused by subsp. in foals. However, studies reporting the use of cefquinome to target as pathogens of sepsis are lacking. Therefore, this study aimed to determine the optimal dosage regimen for cefquinome against using a PK/PD model. After the administration of 1 mg/kg cefquinome (intramuscularly or intravenously), blood samples were collected at different time points to determine the serum concentration of cefquinome via HPLC. The pharmacokinetic parameters were evaluated via NCA (WinNonlin 5.2.1 software). The main pharmacokinetic parameters of cefquinome in foals were as follows: after intravenous administration, the elimination half-life (T) was 2.35 h, the area under the curve (AUC) was 12.33 μg·h/mL, the mean residence time (MRT) was 2.67 h, and the clearance rate (CL) was 0.09 L/h/kg. After intramuscular administration, the peak concentration (C) was 0.89 μg/mL, the time to reach the maximum serum concentration (T) was 2.16 h, T was 4.16 h, AUC was 5.41 μg·h/mL, MRT was 4.92 h, CL was 0.15 L/h/kg, and the absolute bioavailability (F) was 43.86%. An inhibitory sigmoid Emax model was used to integrate the PK/PD indices with ex vivo antimicrobial effects to identify pharmacodynamic targets (PDTs). According to the dose calculation formula, the doses of intramuscularly administered cefquinome required to achieve bacteriostatic effects, bactericidal effects, and bactericidal elimination were 1.10, 1.66, and 2.28 mg/kg, respectively. However, further studies are warranted to verify the therapeutic efficacy of cefquinome in clinical settings.
头孢喹肟用于治疗马驹由（）引起的败血症以及由亚种引起的呼吸道感染。然而，缺乏关于使用头孢喹肟针对作为败血症病原体的（）的研究报道。因此，本研究旨在使用药代动力学/药效学（PK/PD）模型确定头孢喹肟针对（）的最佳给药方案。给予1mg/kg头孢喹肟（肌肉注射或静脉注射）后，在不同时间点采集血样，通过高效液相色谱法（HPLC）测定头孢喹肟的血清浓度。通过非房室分析法（NCA，WinNonlin 5.2.1软件）评估药代动力学参数。头孢喹肟在马驹中的主要药代动力学参数如下：静脉注射后，消除半衰期（T）为2.35小时，曲线下面积（AUC）为12.33μg·h/mL，平均驻留时间（MRT）为2.67小时，清除率（CL）为0.09L/h/kg。肌肉注射后，峰浓度（C）为0.89μg/mL，达到最大血清浓度的时间（T）为2.16小时，T为4.16小时，AUC为5.41μg·h/mL，MRT为4.92小时，CL为0.15L/h/kg，绝对生物利用度（F）为43.86%。使用抑制性S型Emax模型将PK/PD指数与体外抗菌效果相结合，以确定药效学靶点（PDTs）。根据剂量计算公式，达到抑菌效果、杀菌效果和杀菌清除所需的肌肉注射头孢喹肟剂量分别为1.10、1.66和2.28mg/kg。然而，需要进一步研究以验证头孢喹肟在临床环境中的治疗效果。
