【摘要】 将21头健康杜洛克×长白×大白杂交猪复制成霉形体性肺炎模型后,分别肌肉注射环丙沙星(5.0 mg/kg)进行组织及血浆药代动力学研究。结果显示,环丙沙星在感染猪肺中的浓度-时间数据适合一级吸收二室开放模型,外观正常肺与外观实变肺的主要参数分别是:t1/2Ka为0.19和0.46 h,t1/2α为2.68和2.52 h,t1/2β为8.12和6.87 h,tmax为1.10和1.47 h,Cmax为6.00和4.46μg/g,AUC为38.65和33.33mg/(L.h),Tcp(ther)为57.10和50.59 h。气管、支气管组织中的药物浓度-时间数据适合一级吸收一室开放模型,主要参数分别是:t1/2Ka为0.56和0.38 h,t1/2ke为5.68和5.67 h,tmax为2.08和1.60 h,Cmax为3.73和2.62μg/g,AUC为39.44和26.10 mg/(L.h),Tcp(ther)为50.60和47.16 h。表明,环丙沙星对霉形体性肺炎猪呼吸道组织具有良好的穿透性,组织药物浓度明显高于血浆药物浓度,且消除缓慢。更多还原

【Abstract】 Pharmacokinetics of ciprofloxacin in the lung,trachea and brochi were investigated using 21 piglets infected with Mycoplasma hyopneumoniae after 5.0 mg/kg ciprofloxacin was injected intramusculary.Ciprofloxacin concentrations in the lung versus time data were fitted a two-compartment open model with first order absorption.The parameters in normal lung and in consolidated lung were as follows,respectively:t1/2ka 0.19 h and 0.46 h,t1/2α 2.68 h and 2.52 h,t1/2β 8.12 h and 6.87 h,tmax 1.10 h and 1.47 h,Cmax 6.00 μg/g and 4.46 μg/g,AUC 38.65 mg/(L·h) and 33.33 mg/(L·h),Tcp(ther)57.10 h and 50.59 h.Ciprofloxacin concentrations in the trache and bronchi versus time were fitted to an one-compartment open model with first order absorption.The parameters were as follows,respectively:t1/2ka 0.56 h and 0.38 h,t1/2ke 5.68 h and 5.67 h,tmax 2.08 h and 1.60 h,Cmax 3.73 μg/g and 2.62 μg/g,AUC 39.44 mg/(L·h) and 26.10 mg/(L·h),Tcp(ther) 50.60 h and 47.16 h.These results showed that ciprofloxacin had a rapid and extensive penetration into pneogaster tissues,and the concentrations in the tissues were significantly higher than that in the sera.更多还原