头孢喹肟对胸膜肺炎放线杆菌的药动/药效学研究

Pharmacokinetic/Pharmacodynamic Study on Cefquinome against Actinobacillus pleuropeumoniae

目的]测定头孢喹肟对胸膜肺炎放线杆菌的半体内药动-药效学数据,以期为临床提供合理的给药方案。[方法]利用半体内PK/PD模型,研究头孢喹肟对胸膜肺炎放线杆菌的药动学参数。[结果]体外抗菌活性测定结果表明,头孢喹肟在血清中和肉汤中的MIC值均为0.008μg/m L,MBC值均为0.016μg/m L。单次剂量肌内注射1 mg/kg头孢喹肟后,血药浓度-时间曲线符合一级吸收二室模型。硫酸头孢喹肟通过肌内注射,吸收迅速并且在体内的持续时间较长。非线性回归分析表明,头孢喹肟对胸膜肺炎放线杆菌的抗菌效应与PK/PD指数(AUC_(0-24)/MIC)的相关性最强(R^2=0.996 7),C_(max)/MIC为0.8056。产生抑菌、抗菌和清除效应时的AUC_(0-24)/MIC值分别为116.0、175.5和218.5。[结论]单次注射1 mg/kg头孢喹肟,即可对胸膜肺炎放线杆菌起到清除作用。

[Objective]To determine the semi-in vivo PK/PD data of cefquinome against Actinobacillus pleuropeumoniae and provide a rational administration scheme in the clinic.[Method]Using semi-in vivo PK/PD model,the pharmacokinetic parameters of cefquinome against A.pleuropeumoniae were studied.[Result]The determination results of antibacterial activity in vitro showed that the minimum inhibitory concentration(MIC)and minimum bactericidal concentration(MBC)of cefquinome in the serum and broth was 0.008μg/ml and 0.016μg/ml respectively.After single dose(1 mg/kg)of cefquinome by intramuscular injection,the drug concentration-time curve was accordant with the first-order absorption two-compartment model.Cefquinome by intramuscular injection could be absorbed rapidly and persistently effective.Nonlinear regression analysis showed that the antibacterial effect of cefquinome against A.pleuropeumoniae had the strongest relation(R 2=0.996 7)with PK/PD index(AUC 0-24/MIC),C max/MIC was 0.805 6.AUC 0-24/MIC for producing the bacteriostatic effect,antibacterial effect and scavenging effect was 116.0,175.5 and 218.5 respectively.[Conclusion]After single dose(1 mg/kg)of cefquinome,A.pleuropeumoniae could be cleared.