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用于评估马波沙星对仔猪多杀性巴氏杆菌体内抗菌活性的整合药代动力学-药效学(PK/PD)模型。

Integrated pharmacokinetic-Pharmacodynamic (PK/PD) model to evaluate the in vivo antimicrobial activity of Marbofloxacin against Pasteurella multocida in piglets.

作者信息

Zeng Qing Lin, Mei Xian, Su Jia, Li Xiao Hong, Xiong Wen Guang, Lu Yan, Zeng Zhen Ling

机构信息

National Laboratory of Safety Evaluation of veterinary Drugs, College of Veterinary Medicine, South China Agricultural University, Guangzhou, China.

National Laboratory of Safety Evaluation (Environmental Assessment) of Veterinary Drugs, College of Veterinary Medicine, South China Agricultural University, Guangzhou, China.

出版信息

BMC Vet Res. 2017 Jun 15;13(1):178. doi: 10.1186/s12917-017-1099-z.

Abstract

BACKGROUND

Marbofloxacin is a veterinary fluoroquinolone with high activity against Pasteurella multocida. We evaluated it's in vivo activity against P. multocida based on in vivo time-kill data in swine using a tissue-cage model. A series of dosages ranging from 0.15 to 2.5 mg/kg were administered intramuscularly after challenge with P. multocida type B, serotype 2.

RESULTS

The ratio of the 24 h area under the concentration-time curve divided by the minimum inhibitory concentration (AUCTCF/MIC) was the best PK/PD index correlated with the in vivo antibacterial effectiveness of marbofloxacin (R2 = 0.9279). The AUCTCF/MIC necessary to achieve a 1-log CFU/ml reduction and a 3-log CFU/ml (90% of the maximum response) reduction as calculated by an inhibitory sigmoid E model were 13.48 h and 57.70 h, respectively.

CONCLUSIONS

Marbofloxacin is adequate for the treatment of swine infected with P. multocida. The tissue-cage model played a significant role in achieving these PK/PD results.

摘要

背景

马波沙星是一种对多杀巴斯德菌具有高活性的兽用氟喹诺酮类药物。我们使用组织笼模型,基于猪体内时间-杀菌数据评估了其对多杀巴斯德菌的体内活性。在用B型2血清型多杀巴斯德菌攻击后,以0.15至2.5mg/kg的一系列剂量进行肌肉注射。

结果

浓度-时间曲线下24小时面积除以最低抑菌浓度(AUCTCF/MIC)的比值是与马波沙星体内抗菌效果相关性最好的药代动力学/药效学指标(R2 = 0.9279)。通过抑制性S型E模型计算,实现1-log CFU/ml降低和3-log CFU/ml(最大反应的90%)降低所需的AUCTCF/MIC分别为13.48小时和57.70小时。

结论

马波沙星适用于治疗感染多杀巴斯德菌的猪。组织笼模型在获得这些药代动力学/药效学结果中发挥了重要作用。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/847a/5471993/9d969d8f467f/12917_2017_1099_Fig1_HTML.jpg

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