口服帕托珠利溶液在鸡体内的生物利用度及其与托曲珠利溶液的药动学比较研究  

Bioavailability of Patozuril Solution in Chicken by Oral Administration and Comparative Pharmacokinetics Study with Toltazuril Solution

作　　者：聂雅 张小龙 高嫣珺 王震 王美红 聂贞 蒋玥 许琴瑟[3] 卜仕金[1,2] NIE Ya;ZHANG Xiaolong;GAO Yanjun;WANG Zhen;WANG Meihong;NIE Zhen;JIANG Yue;XU Qinse;BU Shijin(Veterinary of Collge,Yangzhou Unversity,Yangzhou,Jiangsu 225009;Jiangsu Co-innovation Center for Prevention and Control of Important Animal Infectious Diseases and Zoonoses,Yangzhou,Jiangsu 225009;Jiangsu Agri--animal Husbandry Vocational College,Taizhou,Jiangsu 225300)

机构地区：[1]扬州大学兽医学院,江苏扬州225009 [2]江苏高校动物重要疫病与人兽共患病防控协同创新中心,江苏扬州225009 [3]江苏农牧科技职业学院,江苏泰州225300

出　　处：《中国家禽》2022年第4期36-40,共5页China Poultry

基　　金：农业农村部残留项目专项;现代农业产业技术体系建设专项资金(CARS-41)。

摘　　要：为研究帕托珠利溶液口服给药在健康肉鸡的药动学特征和生物利用度,并与其前体药物托曲珠利溶液在鸡口服给药进行药动学比较,试验将30只健康肉鸡(公母各半,平均体重约为1.55 kg)随机分为三组,分别为帕托珠利溶液口服组(5 mg/kg bw)、帕托珠利溶液静注组(5 mg/kg bw)和托曲珠利溶液口服组(5 mg/kg bw)。所有受试动物于给药后按规定时间点采集血样。血药浓度-时间数据使用Winnolin 8.1.0拟合药动学参数。结果显示:帕托珠利溶液单剂量口服后在鸡体内的平均达峰浓度(C_(max))、达峰时间(T_(max))、半衰期(T_(1/2β))和药时曲线下面积(AUC_(0-t))分别为4.52μg/mL、24.00 h、101.78 h和609.23 h·μg/mL;帕托珠利溶液单剂量静注后在鸡体内的AUC0-t为778.27 h·μg/mL,绝对生物利用度(F)为78.67%;托曲珠利溶液单剂量口服后的平均C_(max)、T_(max)、T_(1/2β)和AUC_(0-t)分别为6.17μg/mL、2.80 h、16.65 h和92.00 h·μg/mL。研究表明,帕托珠利溶液口服吸收良好,在鸡体内分布范围较窄,有较高的体清除率但消除缓慢,比托曲珠利口服吸收C_(max)明显延迟,消除半衰期显著延长。To study the pharmacokinetic characteristics and bioavailability of patozuril solution in healthy chicken,and the comparative pharmacokinetics of its prodrug toltrazuril solution in chicken,thirty healthy chickens (half male and female,average weight about 1.55 kg) were randomly divided into three groups,namely the patozuril solution oral group (5mg/kg bw),patozuril solution intravenous injection group (5 mg/kg bw) and toltrazuril solution oral group (5 mg/kg bw).All the test animals were given blood samples at a predetermined time point after the administration.The measured blood concentration-time data were fitted with the pharmacokinetic parameters by Winnolin 8.1.0 version.The results showed that the average peak concentration (C_(max)),peak time (T_(max)),half-life (T_(1/2β)),and area under the drug-time curve (AUC_(max)) in chicken after a single oral dose of pertozuril solution were 4.52μg/mL,24.00 h,101.78 h,and 609.23 h·μg/mL;the average area under the drug-time curve (AUC_(0-t)) in chicken after a single dose of patozuril solution intravenously was 778.27 h·μg/mL,the absolute bioavailability (F) was 78.67%;The C_(max),T_(max),T_(1/2β)and AUC_(0-t) of a single oral dose of toltrazuril solution were 6.17μg/mL,2.80 h,16.65 h and 92.00 h·μg/mL,respectively.The results showed that oral patozuril solution was well absorbed,and had a narrow distribution in chicken,with high body clearance rate but slow elimination;Compared with toltrazuril oral absorption peak concentration of patozuril was significantly delayed,and the elimination half-life was significantly prolonged.

关 键 词：帕托珠利 托曲珠利 鸡 生物利用度 比较药动学 

分 类 号：S852.659.5[农业科学—基础兽医学]