陈国庆 1邓梦梦 1谢等龙 1程阳颖 1张燕 1齐雪佳 1李世杰 1曹兴元2
作者信息
- 1. 浙江海正动物保健品有限公司,浙江 杭州 311400
- 2. 中国农业大学动物医学院,北京 海淀 100193
- 折叠
摘要
Abstract
To evaluate the pharmacokinetics and absolute bioavailability of the newly developed moxidectin pour-on in pigs,this study established a high-performance liquid chromatography(HPLC)method to determine the concentration of moxidectin in pig plasma and validated the specificity,linear range,detection limit,quantification limit,accuracy,precision,and stability of this method.A total of 24 2.5-month-old hybrid pigs were randomly divided into three groups(A,B,and C),with 8 pigs in each group.Group A received a single intravenous injection of moxidectin solution at a dose of 1.25 mg/(kg·bw)(100 mg/mL),while groups B and C were given a single pour-on dose of 1.25 and 2.50 mg/(kg·bw)moxidectin pour-on,respectively.Pharmacokinetic curve was measured by HPLC,and the pharmacokinetic parameters and absolute bioavailability were calculated.The results showed that the moxidectin plasma concentration determination method for pigs demonstrated good specificity,with a good linear relationship in the range of 0.5-500 ng/mL.The detection limit was 0.4 ng/mL,and the quantification limit was 0.5 ng/mL.The method showed good accuracy,precision,and stability.Animal experiment results indicated that pigs in Group C had highly significant higher blood drug concentrations at all time points compared with Group B(P<0.001).The maximum concentration of moxidectin in the plasma[Cmax,(7.50±1.26)ng/mL]and the area under the curve[AUClast,(72.50±26.55)ng·day/mL)in Group C were highly significant higher than those in Group B[Cmax(1.12±0.15)ng/mL,AUClast(13.21±2.23)ng·day/mL](P<0.001).The elimination half-life[T1/2,(8.11±1.30)d]was highly significant shorter in Group C compared with Group B[(15.79±4.15)d](P<0.001).The mean residence time[MRT,(9.31±1.27)d]was significantly lower in Group C than in Group B[(13.13±3.03)d](P<0.05).The time to reach Cmax[Tmax,(1.72±2.05)d]was lower in Group C than in Group B[(2.94±1.45)d],but the difference was not significant(P>0.05).The AUClast in Group A was highly significant higher than that in Groups B(P<0.001),while the T1/2 was significantly lower than that in Group B(P<0.05).After pour-on administration of moxidectin at doses of 1.25 and 2.50 mg/(kg·bw),the absolute bioavailability was 3.11%and 8.53%,respectively.The results indicate that moxidectin pour-on is rapidly absorbed through the skin and eliminated slowly.The findings from this study can provide reference for determining the appropriate dosage of moxidectin pour-on for controlling internal and external parasites in pigs.关键词
莫昔克丁浇泼剂/药代动力学/绝对生物利用度/猪Key words
moxidectin pour-on/pharmacokinetics/absolute bioavailability/pig分类
畜牧业
