畜牧与兽医2025,Vol.57Issue(4):51-59,9.
4种酒石酸泰万菌素预混剂在猪体内的对比药代动力学研究
Comparative pharmacokinetic study of four tylvalosin tartrate premixes in pigs
摘要
Abstract
This study aimed to compare the pharmacokinetic characteristics of four domestically developed tylvalosin tartrate premixes(test-ed formulations)and the imported drug ailoxin(reference formulation)in pigs.The relative bioavailability of the five formulations was evalu-ated based on pharmacokinetic parameters to select the formulation with higher bioavailability.Using a parallel experimental design method,30 ternary crossbred pigs(Duroc×Landrace×Yorkshire)were selected and randomly divided into 5 groups,with an equal distribution of males and females in each group.The test formulations and the reference formulation were administered as a single dose via oral gavage at a dose of 25 mg/kg.Then,the blood concentration in the pigs was determined using the UPLC-MS/MS method and analyzed by a non-atrial model using the WinNonlin software to calculate the pharmacokinetic parameters and relative bioavailability of the five formulations.The phar-macokinetic results showed that the elimination half-lives(T1/2)of the subjected formulations 1 to 4 and the reference formulation of Ailoxin were(4.40±1.98),(5.03±1.39),(4.73±1.42),(1.26±0.32),and(3.52±0.86)h,respectively;that the time points to reach the peak values(Tmax)were(4.00±0.00),(0.50±0.00),(0.90±0.22),(0.56±0.13),and(0.50±0.00)h,respectively;that the peak concentrations(Cmax)were(51.86±8.95),(111.00±4.51),(37.95±5.28),(92.13±2.65),and(147.71±29.47)ng/mL,respec-tively;that the areas under the curve(AUClast)at time of administration were(260.15±29.63),(336.68±9.41),(227.93±11.56),(204.33±4.83),and(300.48±32.09)h·ng/mL,respectively;and that the relative bioavailability(F)was 86.58%,112.05%,75.85%,and 68.00%,respectively.These results indicated that the UPLC-MS/MS method established in this experiment was highly effi-cient,accurate and reliable,and could be used for the determination of the concentration of tylvalosin.The parameter results showed that tyl-valosin tartrate premix possessed the characteristics of rapid absorption,short time to reach peak values,faster elimination,and shorter aver-age retention time in the blood in the pig.Comparing the kinetic parameters of four domestic tylvalosin tartrate premixes with those of the im-ported Ailoxin,the elimination half-life of domestic tartrate premix No.2 drug(T1/2)was the largest,the time to reach the peak value(Tmax)was the shortest,the area under the curve(AUClast)was the largest,and the relative bioavailability(F)was the highest.This premix possessed the best performance,and it promised a value of clinical application and a potential for further development.关键词
泰万菌素/对比药代动力学/猪/超高效液相色谱-串联质谱/相对生物利用度Key words
tylvalosin/comparative pharmacokinetics/swine/UPLC-MS/MS/relative bioavailability分类
畜牧业引用本文复制引用
李江,魏小娟,郭丽华,张继瑜,周绪正,姚学强,代国年,程富胜,李冰,周雅馨,白玉彬,王玮玮,翟斌涛..4种酒石酸泰万菌素预混剂在猪体内的对比药代动力学研究[J].畜牧与兽医,2025,57(4):51-59,9.基金项目
甘肃省重点研发计划项目(23YFNA0001) (23YFNA0001)
舟曲县黑土猪产业质量标准体系建设项目(ZQJY-ZC-2023-048) (ZQJY-ZC-2023-048)