头孢维星在犬体内的药动学及生物利用度研究

Pharmacokinetics and Bioavailability of cefovecin in dogs

关键词:  头孢维星  HPLC  药动学  生物利用度  犬

Key words:  cefovecin  HPLC  pharmacokinetics  bioavailability  dogs

摘要:

建立了一种头孢维星在犬血浆中的高效液相色谱检测法，并研究了头孢维星在犬体内的药动学特征及生物利用度。选用健康家犬12只，按单剂量（8mg/kg b.w.）分别静脉注射或皮下注射头孢维星，利用建立的方法对头孢维星在犬血浆中的浓度进行测定，采用WinNonlin5.2.1程序的非房室模型处理药时数据。结果显示，静脉注射组的主要药动学参数为t1/2β=129.15±35.79h；MRT=152.56±44.95h；λz=0.005 9±0.002 3 h-1；Cl=1.24±0.56 mL/(h?kg)；AUC=6 942.88±2 462.48μg?h/mL；V=170.20±28.09 mL/kg。皮下注射组的主要药动学参数为t1/2β=136.94±20.96h；MRT= 167.77±28.15h；Tmax=0.83±0.26h；Cmax=59.51±7.99μg/mL；λz=0.005 2±0.000 9 h-1；Cl=1.05±0.21 mL/(h?kg)；AUC=7 332.58±1 118.30μg?h/mL；V=203.81±30.09 mL/kg；F=105.61%。结果表明，头孢维星在家犬体内表现出吸收迅速、消除缓慢、表观分布容积大、生物利用度高等药动学特点。

Abstract:

Abstract: A method for determination of cefovecin in plasma of dogs by HPLC and study the pharmacokinetics and bioavailability of cefovecin in dogs, a single intravenous(i.v.) or subcutaneous(s.c) administration of cefovecin at a dosage of 8 mg/kg b.w. was performed in 12 healthy dogs. Plasma concentrations of cefovecin were determinded by the HPLC method and the pharmacokinetics parameters were calculated by noncompartmental analysis with WinNonLin 5.2.1 software. After intravenous administration, the main pharmacokinetics parameters were as follow: t1/2β=129.15±35.79h; MRT=152.56±44.95h; λz=0.005 9±0.002 3h-1; Cl=1.24±0.56 mL/(h?kg); AUC=6 942.88±2 462.48μg?h/mL; V=170.20±28.09mL/kg.After subcutaneous administration, the main pharmacokinetics parameters were as follow: t1/2β=136.94±20.96h; MRT= 167.77±28.15h; Tmax=0.83±0.26h; Cmax=59.51±7.99μg/mL; λz=0.005 2±0.000 9 h-1; Cl=1.05±0.21 mL/(h?kg); AUC=7 332.58±1 118.30μg?h/mL; V=203.81±30.09 mL/kg; F=105.61%. the result showed cefovecin with characteristics in dogs were as follow:fast absorption, slow elimination, bigvolume of distribution and high bioavailablability.