代谢
恩诺沙星及其活性代谢物环丙沙星在山羊体内的药代动力学研究,以2.5 mg/kg体重的剂量单次肌内给药后进行了调查。通过高效液相色谱法同时测定了恩诺沙星和环丙沙星的血浆浓度。恩诺沙星(1.13微克/毫升)和环丙沙星(0.24微克/毫升)的峰浓度(Cmax)分别在0.8小时和1.2小时观察到。恩诺沙星的消除半衰期(t1/2beta)、分布容积(Vd(area))、总体清除率(Cl(B))和平均滞留时间(MRT)分别为0.74小时、1.42升/千克、1329毫升/小时/千克和1.54小时。环丙沙星的t1/2beta、血浆浓度-时间曲线下面积(AUC)和MRT分别为1.38小时、0.74微克·小时/毫升和2.73小时。恩诺沙星转化为环丙沙星的代谢转化是显著的(36%),恩诺沙星和环丙沙星的血浆浓度之和在4小时内保持在或高于0.1微克/毫升。恩诺沙星似乎适用于治疗与对该药物敏感的病原体相关的山羊疾病。
The pharmacokinetics of enrofloxacin and its active metabolite ciprofloxacin were investigated in goats after a single intramuscular administration of enrofloxacin at 2.5 mg/kg body weight. The plasma concentrations of enrofloxacin and ciprofloxacin were determined simultaneously by a HPLC method. The peak concentrations (Cmax) of enrofloxacin (1.13 microg/ml) and ciprofloxacin (0.24 microg/ml) were observed at 0.8 and 1.2 hr, respectively. The elimination half-life (t1/2beta), volume of distribution (Vd(area)), total body clearance (Cl(B)) and mean residence time (MRT) of enrofloxacin were 0.74 hr, 1.42 l/kg, 1329 ml/hr per kg and 1.54 hr, respectively. The t1/2beta, area under the plasma concentration-time curve (AUC) and the MRT of ciprofloxacin were 1.38 h, 0.74 microg h/ml and 2.73 h, respectively. The metabolic conversion of enrofloxacin to ciprofloxacin was appreciable (36%) and the sum of the plasma concentrations of enrofloxacin and ciprofloxacin was maintained at or above 0.1 microg/ml for up to 4 hr. Enrofloxacin appears to be useful for the treatment of goat diseases associated with pathogens sensitive to this drug.
来源:Hazardous Substances Data Bank (HSDB)