Albarellos G A, Montoya L, Landoni M F
Area de Farmacología, Departamento de Fisiopatología y Etiopatogenia, Facultad de Ciencias Veterinarias, Universidad de Buenos Aires, Chorroarín 280 (1427), Buenos Aires, Argentina.
Vet J. 2005 Sep;170(2):222-9. doi: 10.1016/j.tvjl.2004.05.011.
The pharmacokinetic properties of marbofloxacin, a third generation fluoroquinolone, were investigated in six cats after single intravenous (IV) and repeat oral (PO) administration at a daily dose of 2 mg/kg. Marbofloxacin serum concentration was analysed by microbiological assay using Klebsiella pneumoniae ATCC 10031 as micro-organism test. Serum marbofloxacin disposition was best described by bicompartmental and mono-compartmental open models with first-order elimination after IV and oral dosing respectively. After IV administration, distribution was rapid (T(1/2(d)) 0.23+/-0.24 h) and wide, as reflected by the steady-state volume of distribution of 1.01+/-0.15 L/kg. Elimination from the body was slow with a body clearance of 0.09+/-0.02 L/h kg and a T(1/2) of 7.98+/-0.57 h. After repeat oral administration, absorption half-life was 0.86+/-1.59 h and T(max) of 1.94+/-2.11 h. Bioavailability was almost complete (99+/-29%) with a peak plasma concentration at the steady-state of 1.97+/-0.61 mug/mL. Drug accumulation was not significant after six oral administrations. Calculation of efficacy predictors showed that marbofloxacin has good therapeutic profile against Gram-negative and Gram-positive bacteria with a MIC(50) value <0.25 microg/mL.
在6只猫中,以2mg/kg的日剂量单次静脉注射(IV)和重复口服(PO)给药后,研究了第三代氟喹诺酮类药物马波沙星的药代动力学特性。采用肺炎克雷伯菌ATCC 10031作为微生物测试,通过微生物学测定法分析马波沙星血清浓度。静脉注射和口服给药后,马波沙星血清处置分别用双室和单室开放模型最佳描述,消除均为一级动力学。静脉注射后,分布迅速(T(1/2(d)) 0.23±0.24小时)且广泛,稳态分布容积为1.01±0.15L/kg反映了这一点。从体内消除缓慢,机体清除率为0.09±0.02L/h·kg,T(1/2)为7.98±0.57小时。重复口服给药后,吸收半衰期为0.86±1.59小时,达峰时间为1.94±2.11小时。生物利用度几乎完全(99±29%),稳态时血浆峰浓度为1.97±0.61μg/mL。口服6次后药物蓄积不显著。疗效预测指标计算表明,马波沙星对革兰氏阴性菌和革兰氏阳性菌具有良好的治疗谱,MIC(50)值<0.25μg/mL。