泰地罗新注射液在猪体内的药代动力学及绝对生物利用度研究  

Pharmacokinetics and Absolute Bioavailability of Tildipirosin Injection in Pigs

作　　者：宋婷婷[1] 刘静[1] 瞿红颖 贾兴[1] 耿智霞[1] 郭李珉 刘欣[1] 魏占勇[1] 曹兴元[2] SONG Ting-ting;LIU Jing;QU Hong-ying;JIA Xing;GENG Zhi-xia;GUO Li-min;LIU Xin;WEI Zhan-yong;CAO Xing-yuan(HeBei Yuanzheng Pharmaceutical Co. Ltd/Hebei Technology Innovation Center of Veterinary Drugs,Shijiazhuang 050041, China;China Agricultural University, Beijing 100193, China)

机构地区：[1]河北远征药业有限公司/河北省兽药技术创新中心,石家庄050041 [2]中国农业大学,北京100193

出　　处：《中国兽药杂志》2020年第12期38-43,共6页Chinese Journal of Veterinary Drug

摘　　要：为研究泰地罗新注射液肌内注射和静脉注射在猪体内的药动学特征和绝对生物利用度,16只健康猪采用随机单剂量、平行试验设计,分别以4 mg/kg BW肌内注射(A组)和以1 mg/kg BW静脉注射泰地罗新注射液(B组)。采用UPLC-MS/MS测定猪血浆中泰地罗新的浓度,以药动学分析软件WinNolin 6.4非房室模型计算药动学参数。结果显示,A组达峰时间(Tmax)、达峰浓度(Cmax)、平均消除半衰期(T1/2λz)、平均药时曲线下面积(AUClast)和平均滞留时间(MRTlast)分别为0.58±0.36 h、0.88±0.17μg/mL、33.58±22.01 h、11.00±4.05μg·h/mL、35.60±10.00 h。B组平均AUClast、平均T1/2λz、平均MRTlast、表观分布容积(Vz)、平均体清除率(Cl)分别为3.56±1.62μg·h/mL、50.91±23.47 h、37.53±4.52 h、17.59±8.09 L/kg、0.31±0.14 L/(h·kg)。肌内注射泰地罗新注射液的绝对生物利用度77.15%,在猪体内的药动学特征是吸收迅速,血浆达峰时间短,消除半衰期长,绝对生物利用度高。The pharmacokinetics and absolute bioavailability of tildipirosin were investigated by a parallel experiment design following intramuscular(4 mg/kg BW,group A)and single intravenous(1 mg/kg BW,group B)administration of drug in sixteen healthy pigs.The concentrations of tildipirosin in plasma were determined by UPLC-MS/MS and the pharmacokinetic parameters were analyzed with WinNolin 6.4 program.The peak time(Tmax),peak concentration(Cmax),average elimination half-life(T1/2λz),average area under the curve(AUClast)and mean residence time(MRTlast)in group A were 0.58±0.36 h,0.88±0.17μg/mL,33.58±22.01 h,11.00±4.05μg·h/mL and 35.60±10.00 h,respectively.AUClast,T1/2λz,MRTlast,apparent distribution volume(Vz)and total boby chearance(Cl)in group B were 3.56±1.62μg·h/mL,50.91±23.47 h,37.53±4.52 h,17.59±8.09 L/kg and 0.31±0.14 L/(h·kg),respectively.The intramuscular bioavailability of tildipirosin injection was 77.15%.The pharmacokinetic characteristics of tildipirosin in pigs displayed absorbed quickly,peaked rapidly,long elimination half-life and high absolute bioavailability.

关 键 词：泰地罗新注射液 药代动力学 猪 绝对生物利用度 UPLC-MS/MS 

分 类 号：S859.7[农业科学—临床兽医学]