伊维菌素微乳剂在绵羊体内的药代动力学研究

研究伊维菌素微乳剂在绵羊体内的药代动力学,对比高含量伊维菌素微乳剂与普通注射剂型的生物利用度差异。选取12只绵羊,分为2组,按照0.2 mg/kg体重分别皮下注射10 mg/mL伊维菌素注射液和30 mg/mL伊维菌素微乳剂。分别在给药前0.5 h,给药后2、4、6、8、10、12、16、20、24、36、48、96、144、192、240、336 h在颈静脉采集血液备用,用高效液相色谱荧光检测器对绵羊血浆中的伊维菌素进行检测,并利用内标法计算其含量。通过DAS2.1.1软件进行数据统计分析。结果显示,伊维菌素微乳剂组药时曲线下面积(AUC)为3812.17 ng/mL·h,达峰浓度(Cmax)为97.71 ng/mL,达峰时间(Tmax)为12 h,消除半衰期(T1/2z)为43.46 h;伊维菌素注射液组AUC为2501.25 ng/mL·h,Cmax为48.15 ng/mL,Tmax为24 h,T1/2z为44.96 h。说明伊维菌素微乳剂吸收效果好,达峰时间短,达峰浓度高,生物利用度高。

Study on Pharmacokinetics of Ivermectin Microemulsion in Sheep

To study the pharmacokinetics of Ivermectin microemulsion in sheep and the difference of bioavailability between ivermectin microemulsion and ivermectin injection,twelve sheep were selected and divided into two groups.Ivermectin injection and ivermectin microemulsion were administered at 0.2 mg per kg.Blood was collected from the jugular vein at 0.5 h before injection,2,4,6,8,10,12,16,20,24,36,48,96,144,192,240 h and 336 h after injection,respectively.Ivermectin was detected by HPLC fluorescence detector,and the content was calculated by internal standard method.Data analysis was carried out through DAS2.1.1software.The results showed the group of ivermectin microemulsion AUC=3812.17 ng/mL·h,Cmax=97.71 ng/mL,Tmax=12 h,T1/2z=43.46 h,the group of ivermectin injection AUC=2501.25 ng/mL·h,Cmax=48.15 ng/mL,Tmax=24 h,T1/2z=44.96 h.It indicated that the ivermectin microemulsion had better absorption effect,shorter peak time,higher peak concentration and higher bioavailability.