犬口服国产麻保沙星溶液的生物利用度研究  

Bioavailability of Marbofloxacin in Dogs by Oral Administrate

作　　者：刘利锋[1] 高丽丽[1] 苏凤[1] 江善祥[1] 

机构地区：[1]南京农业大学动物医学院.南京210095

出　　处：《畜牧兽医学报》2010年第10期1317-1321,共5页ACTA VETERINARIA ET ZOOTECHNICA SINICA

摘　　要：本研究旨在考察国产麻保沙星溶液在健康犬体内的药动学特征及生物利用度。选用8只健康犬,按照随机拉丁方设计,进行单次不同单剂量(2.75mg·kg-1)分别静注麻保沙星溶液和口服麻保沙星溶液制剂。血浆样品经乙腈沉淀血浆蛋白,高速离心,用反相高效液相色谱法测定犬血浆中麻保沙星的浓度,3P97药动学计算软件处理血浆药物浓度-时间数据。健康犬静注给药的药物动力学最佳数学模型为无吸收开放二室模型,主要药动学参数为:T1/2α(0.34±0.14)h,T1/2β(7.74±1.70)h,V(1.03±0.60)L·kg-1,CL(0.22±0.08)L·h-1;AUC(14.05±4.25)mg·mL-1·h。口服给药的药物动力学最佳数学模型为一级吸收二室模型。主要药动学参数为:T1/2α((2.82±1.86)h,T1/2β(16.03±9.27)h,V/F(2.25±0.34)L·kg-1,CL/F(0.21±0.05)L·h-1,Tmax(1.55±0.62)h,Cmax(0.89±0.21)μg·mL-1,AUC(13.66±2.77)mg·mL-1·h。肌注麻保沙星冻干粉针的生物利用度为97.22%。麻保沙星在健康犬体内口服的主要药动学特征为吸收较快,达峰时间短,半衰期较长,生物利用度高。This experiment was conducted to investigate the pharmacokinetics and bioavailability of marbofloxacin in healthy dogs.A single oral or i.v.administration of the drug at the dose of 2.75 mg·kg-1 to 8 dogs were performed in an open randomized crossover test.Blood samples were collected at different intervals after administration and concentrations of marbofloxacin were determined by HPLC method.The concentration-time date were analyzed with 3P97 computer program to get the pharmacokinetics parameters.The drug concentration-time data were fitted to a no absorbed two-compartment open model after i.v.administration in pigs.The main pharmacokinetic parameters were as follows T1/2α（0.34±0.14）h,T1/2β（7.74±1.70）h,V（1.03±0.60）L·kg-1,CL（0.22±0.08）L·h-1;AUC（14.05±4.25）mg·mL-1·h.The drug concentration-time data were fitted to a two-compartment model with first order absorption after single oral administration in dogs.The main pharmacokinectic parameters were as follows：T1/2α（（2.82±1.86）h,T1/2β（16.03±9.27）h,V/F（2.25±0.34）L·kg-1,CL/F（0.21±0.05）L·h-1,Tmax（1.55±0.62）h,Cmax（0.89±0.21）μg·mL-1,AUC（13.66±2.77）mg·mL-1·h.Marbofloxacin was rapidly absorbed and the drug was completely absorbed after single oral administration and have a good bioavailability in dogs.

关 键 词：麻保沙星 生物利用度 犬 

分 类 号：S859.7[农业科学—临床兽医学]