抗球虫新药纳川珠利在大鼠肝S9中的代谢稳定性研究  

Metabolic Stability of a New Anticoccidial Drug Natromezuril in Rat Hepatic S9

作　　者：李素梅[1] 张可煜[1] 王霄旸[1] 李涛[1] 薛飞群[1] 

机构地区：[1]中国农业科学院上海兽医研究所农业部动物寄生虫学重点开放实验室中国农业科学院兽药安全评价与兽药残留研究重点开放实验室,上海200241

出　　处：《动物医学进展》2012年第12期95-98,共4页Progress In Veterinary Medicine

基　　金：国家高技术研究发展计划(863计划)(2011AA10A214);中央级公益性科研院所基本科研业务费专项资金项目(2012JB02)

摘　　要：以大鼠肝S9系统为体外代谢模型,利用高效液相色谱法检测抗球虫新药纳川珠利与大鼠肝S9孵育后的含量,研究纳川珠利在大鼠肝S9系统中的代谢稳定性及可能存在的代谢产物。结果显示,大鼠肝S9系统中,纳川珠利药物浓度在0～1h范围内呈线性消除,符合一级反应的特征,速率常数K=0.004 719min-1,半衰期t 1/2=146.88min,说明纳川珠利在大鼠肝S9系统中具有较高的代谢稳定性;此外,该系统中还监测到纳川珠利的一种代谢产物,它的量也随着时间的增加而增加,约占纳川珠利代谢总量的36%。A high performance liquid chromatograph （HPLC） method for measuring content of a new anticoccidial drug natromezuril after incubation with rat＇s liver S9 is established to study its metabolic stability and possible metabolites. The result demonstrated that drug concentration eliminated linearly in the first hour in the incubation system which accorded with the characteristics of primary reaction. Rate constant K was 0. 004 719 min^-1 and t1/2 was 146.88 rain which illustrated natromezuril＇s high metabolic stability. Besides, a metabolite was detected in the system, the content of which increased as the elimination of natromezuril. We approximately estimated the metabolite accounts for 36 % of metabolism of natromezuril.

关 键 词：抗球虫新药 纳川珠利 肝S9 代谢稳定性 

分 类 号：S852.723[农业科学—基础兽医学]