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当前位置: 首页 > 文章 > 马波沙星在多杀性巴氏杆菌感染的小鼠体内的药动学研究 中国兽医科学 2016 (9) 1183-1188
Position: Home > Articles > Pharmacokinetics of marbofloxacin in the mice infected with Pasteurella multocida Chinese Veterinary Science 2016 (9) 1183-1188

马波沙星在多杀性巴氏杆菌感染的小鼠体内的药动学研究

作  者：
卢燕;李亚菲;肖倩雯;赵慧敏;曾振灵
单  位：
广东省农业科学院农产品公共监测中心;华南农业大学兽医学院广东省兽药研制与安全评价重点实验室
关键词：
马波沙星;药动学;上皮细胞衬液;多杀性巴氏杆菌;肺炎模型;小鼠
摘  要：
本试验通过建立多杀性巴氏杆菌感染的小鼠肺炎模型,研究马波沙星在肺部感染小鼠体内的血浆、肺组织、上皮细胞衬液的药动学。小鼠肺部感染多杀性巴氏杆菌后,单剂量皮下注射10 mg/kg的马波沙星。采用高效液相色谱法测定血浆、肺组织、支气管肺泡灌洗液中的药物浓度,用WinNonLin5.2.1软件提供的非房室模型处理药物浓度—时间数据。结果显示,血浆中的主要药代动力学参数达峰时间(t_(max))为0.5 h,达峰浓度(C_(max))为3.58 g/m L,药时曲线下面积(AUC0-24h)为6.91 g/(mL·h),消除半衰期(t1/2β)为2.87 h;肺组织中的主要药代动力学参数tmax为0.25 h,C_(max)为8.14 g/m L,AUC0-24 h为15.89 g/(m L·h),t1/2β为3.56 h;上皮细胞衬液(ELF)中的主要药代动力学参数tmax为0.5 h,Cmax为3.89 g/m L,AUC0-24h为9.58 g/(m L·h),t_(1/2β)为1.98 h,ELF中AUC与血浆游离药物AUC的比值为1.98。结果表明,马波沙星在肺部渗透能力较强,这为马波沙星治疗呼吸道感染提供了实验依据。
译  名：
Pharmacokinetics of marbofloxacin in the mice infected with Pasteurella multocida
作  者：
LU Yan;LI Ya-fei;XIAO Qian-wen;ZHAO Hui-min;ZENG Zhen-ling;College of Veterinary, Medicine South China Agricultural University/Guangdong Provincial Key Laboratory of Veterinary Pharmaceutics Development and safety Evaluation;Public Monitoring Center for Agroproduct of Guangdong Academy of Agricultural Sciences;
关键词：
marbofloxacin;;pharmacokinetics;;epithelial lining fluid;;Pasteurella multocida;;lung infection model;;mice
摘  要：
This study was conducted to evaluate the pharmacokinetic characteristics of marbofloxacin in plasma, lung tissue and epithelial lining fluid(ELF)in a murine lung infection model.Marbofloxacin was administrated to the mice infected with Pasteurella multocida subcutaneously at a single dosage of 10 mg/kg body weight. Marbofloxacin concentration in the plasma, lung tissue and bronchoalveolar lavage fluid(BLAF) was measured by high performance liquid chromatography, and drug concentration-time data were analyzed by using the non-compartment model in Win Non Lin5.2.1 software. The main plasma pharmacokinetic parameters were as follows: the tmax was 0.5 h; the maximum concentration(C_(max)) was 3.58 g/m L; the area under the plasma drug concentration-time curve(AUC0-24h) was 6.91 g/(m L·h)and the elimination half-life(t_(1/2β)) was 2.87 h. The main pharmacokinetic parameters in lung tissue were as follows: the t_(max) was 0.25 h; Cmaxwas 8.14 g/m L; AUC0-24 hwas 15.89 g/(m L·h) and t_(1/2β) was 3.56 h.The main pharmacokinetic parameters in ELF were as follows: tmaxwas 0.5 h; Cmaxwas 3.89 g/ m L; AUC0-24 hwas 9.58g/(mL ·h); t_(1/ 2β) was 1.98 h and the value of AUCELF/ fA UCplasmawas 1.98. The result showed that the penetration of marbofloxacin in ELF was relatively high and the ratio ELF-free plasma AUC0-24 was about 2, providing experimental data when marbofloxacin is used in the treatment of respiratory disease.

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