摘要
分别采用静脉注射和内服两种给药途径给予健康蛋雏鸡甲磺酸单诺沙星溶液和甲磺酸单诺沙星脂质体混悬液(剂量为5 mg/kg)。结果显示,两种剂型静注给药的药时数据均符合无吸收二室开放模型,主要药动学参数分别为T1/2α0.349 60、.351 8 h;T1/2β6.411 4、8.193 2 h;AUC3.799 75、.066 0 mg/(L.h);CLβ1.723 2、1.131 7 L/(kg.h)。两种剂型内服给药的药时数据均符合一级吸收一室开放模型,主要药动学参数分别为T1/2 Kα0.301 7、0.524 4 h;T1/2K 4.479 2、5.021 7 h;AUC 3.284 44、.610 6 mg/(L.h);Cmax 0.483 81、.054 8 mg/L;Tp 1.287 3、1.936 2 h;生物利用度分别为86.44%、91.01%。可见这两种剂型的静注与内服给药的体内药动学特征不同。与甲磺酸单诺沙星溶液相比,甲磺酸单诺沙星脂质体血浆半衰期延长,达峰浓度高,有效浓度维持时间持久,内服生物利用度提高。
Danofloxacin mesylate solution and danofloxacin mesylate liposomes were separately administered to the healthy egg chickens by i. v. and p. o.（5 mg/kg）, the concentration-time data were fitted to a two-compartment open model after single intravenous administration of the two dosage forms. The main pharmacokinetic parameters were as follows：T1/2α 0.349 6,0. 351 8 h;T1/2β 6. 411 4,8. 193 2 h;AUC3.799 7,5.0660 mg/（L·h）;CLβ1. 723 2, 1. 131 7 L/（kg·h）, respectively. The concentration-time data were both described by a one-compartment open model with first-order absorption after single p. o administration of the two dosage forms. The main pharmacokinetic parameters were as follows：T1/2 Kα 0. 301 7,0. 524 4 h;T1/2K 4.479 2,5.0217 h;AUC 3. 284 4,4. 6106 mg/（L·h） Cmax0.483 8,1.054 8 mg/L;Tp 1.287 3,1.936 2 h;F 86.44%,91.01% ,respectively. The results showed there were significant differences in pharmacokinetics of danofloxacin in egg chickens between two dosage forms,compared with the danofloxacin mesylate solution, the plasma half-life was prolonged, the peak concentration was elevated, the maintain time of effective concentration was later,and the P. O. bioavailability increased in the danofloxacin mesylate liposomes.
出处
《中国兽医学报》
CAS
CSCD
北大核心
2009年第11期1434-1437,共4页
Chinese Journal of Veterinary Science
基金
哈尔滨市青年科技创新人才资金项目
