沙拉沙星在猪体内的药动学研究  

Pharmacokinetic Studies of Sarafloxacin in Pigs

作　　者：丁焕中[1] 曾振灵[1] 冯淇辉[1] 陈杖榴[1] 

机构地区：[1]华南农业大学兽医药理研究室,广州510642

出　　处：《畜牧兽医学报》2002年第1期55-58,共4页ACTA VETERINARIA ET ZOOTECHNICA SINICA

摘　　要：7头健康杂种猪 ,按照随机拉丁方设计 ,进行静注、肌注及内服沙拉沙星 (5mg/kg)的药动学研究。血浆样品经甲醇沉淀血浆蛋白 ,高速离心 ,用反相高效液相色谱法测定猪血浆中沙拉沙星的浓度 ,MCPKP计算机程序处理血浆药物浓度 时间数据。健康猪静注给药的药时数据适合二室开放模型 ,主要药物动力学参数为t1/ 2α0 88±0 2 8h ;t1/ 2 β3 0 6± 0 5 0h ;V11 36± 0 2 4L/kg ;Vd(area) 2 5 0± 0 42L/kg ;ClB0 5 7± 0 0 7L·kg-1·h-1;AUC8 90±1 0 3mg·L-1·h。健康猪肌注给药的药时数据适合一级吸收一室模型 ,主要药物动力学参数为 :t1/ 2ka0 2 5± 0 18h ;t1/ 2ke3 5 3± 1 0 1h ;tmax0 94± 0 49h ;Cmax1 30± 0 37μg/ml;AUC 7 6 6± 1 38mg·L-1·h ;F86 48%± 15 15 %。健康猪内服给药的药时数据适合一级吸收一室模型 ,主要药物动力学参数为 :t1/ 2ka0 5 1± 0 2 9h ;t1/ 2ke6 72± 2 78h ;tmax2 45± 0 89h ;Cmax0 36± 0 2 1μg/ml;AUC　 4 5 4± 1 0 6mg·L-1·h ;F5 1 99%± 14 6 7%。沙拉沙星在健康猪体内的主要药动学特征为 :吸收迅速 ,达峰时间短 ,表观分布容积大。肌注给药吸收完全 ;内服给药吸收不完全 ,消除缓慢。Pharmacolinetics of sarafloxaxin were investigated in 7 healthy cross bred pigs following a single intravenous,intramuscular and oral administration of the drug at the dose of 5 mg/kg b.w.Blood samples were collected at different intervals after administration and sarafloxacin concentrations were determined by HPLC method with a limit of detection of 0 05 μg/ml.The sarafloxacin concentration time data were fitted to a two compartment open model after single i.v. dosing in healthy pigs.The main pharmacokinetic parameters were as follows:t 1/2α 0 88±0 28 h;t 1/2β 3 06±0 50 h;V 11 36±0 24 L/kg;V d(area) 2 50±0 42 L/kg;Cl B 0 57±0 07 L·kg -1 ·h -1 ;AUC 8 90±1 03 mg·L -1 ·h.The drug concentration time data were fitted to a one compartment model with first order absorption after single i.m.dosing in healthy pigs.The main pharmacokinetic parameters were as follows:t 1/2ka 0 25±0 18 h;t 1/2ke 3 53±1 01 h;t max 0 94±0 49 h;C max 1 30±0 37 μg/ml;AUC 7 66±1 38 mg·L -1 ·h;F86 48%±15 15%.The drug concentration time data were fitted to a one compartment model with first order absorption after single p.o.administration in healthy pigs.The mainpharmacokinetic parameters were as follows:t 1/2ka 0 51±0 29 h;t 1/2ke 6 72±2 78 h;t max 2 45±0 89 h;C max 0 36±0 21 μg/ml;AUC 4 54±1 06 mg·L -1 ·h;F51 99%±14 67%.The results of present studies showed that sarafloxacin was absorbed fast and distributed extensively in pigs.The drug was completely absorbed after a single i.m.administration and slowly eliminated after p.o.administration in healthy pigs.

关 键 词：沙拉沙星 高效液相色谱 药物动力学 猪 氟喹诺酮类药物 

分 类 号：S859.796[农业科学—临床兽医学]