麻保沙星在番鸭体内的药代动力学研究

Pharmacokinetics of marbofloxacin in Muscovy ducks

将30只健康番鸭随机分为3组,静脉注射、肌肉注射及内服麻保沙星(2.5mg/kg)后,采用反相高效液相色谱法测定血浆中麻保沙星的浓度,用Kinetica4.4.1药代动力学软件处理所得到的血药浓度-时间数据。结果显示,健康番鸭静脉注射给药的药时数据适合二室开放模型,主要药代动力学参数分别为:t1/2α=(0.45±0.17)h,t1/2β=(3.28±0.33)h,Vc=(0.8±0.1)L/kg,Vd(area)=(1.39±0.28)L/kg,Vd(ss)=(1.25±0.22)L/kg,Cl=(0.23±0.05)L/(h.kg),AUC=(9.24±1.35)mg/(h.L)。健康番鸭肌肉注射给药的药时数据适合一级吸收一室开放模型,主要药代动力学参数分别为:t1/2ka=(0.16±0.06)h,t1/2kel=(2.82±0.36)h,tmax=(0.59±0.11)h,Cmax=(1.8±0.29)μg/mL,AUC=(7.92±1.09)mg/(h.L),F=(90.4±1.73)%。健康番鸭内服给药的药时数据适合一级吸收一室开放模型,主要药代动力学参数分别为:t1/2ka=(0.34±0.09)h,t1/2kel=(4.61±0.57)h,tmax=(1.41±0.3)h,Cmax=(1.13±0.21)μg/mL,AUC=(8.8±1.15)mg/(h.L),F=(96.98±5.16)%。结果表明,麻保沙星在健康番鸭体内的药代动力学特征是:吸收迅速且完全,分布广泛,消除缓慢,组织渗透力强,生物利用度高。

Thirty Muscovy ducks were randomly assigned to three groups of 10 ducks each for the sin-gle intravenous（IV） ,intramuscular（IM） or stomach tube（ST） administrations at a dose of 2.5 mg/kg mar-bofloxacin according to duck body weight. The marbofloxacin concentration in plasma was determined by high performance liquid chromatography with UV. The data were analyzed with the pharmacokinetics com-puter program Kinetica4. 4.1. In results, the relationship of concentration-time was fitted to a two-compart-ment open model after single Ⅳ dosing in healthy Muscovy ducks. The main pharmacokinetic parameters were as follows：t_（1/2α）=（0.45±0.17）h,t_（1/2β）=（3.28±0.33）h,V_c=（0.8±0.1）L/kg,V_（d（area））=（1.39± 0.28）L/kg,V_（d（ss）））=（1.25±0.22）L/kg,Cl=（0.23±0.05）L/（h·kg）,AUC=（9.24±1.35）mg/（h·L）. The concentration-time relationship was fitted to a mono-compartment open model with first-order absorp-tion after single IM dosing in healthy Muscovy ducks. The main pharmacokinetic parameters were as fol-lows：t_（1/2k_α）（0.12±0.06）h,t_（1/2k_（el））=（2.82±0.36）h,t_（max）=（0.59±0.11）h,C_（max）（1.8±0.29）μg/mL, to a mono-compartment open model with first-order absorption after single ST dosing in healthy Muscovy ducks. The main pharmacokinetic parameters were as follows：t_（1/2k_α）=（0.34±0.09）h,t_（1/2k_（el））=（4.61±0.57）h, The results showed that the pharmacokinetic characteristics of marbofloxacin in healthy Muscovy ducks manifested rapid and complete absorption, wide distribution and slow elimination, good tissue penetration and high bioavailability.