摘要
本文描述了阿维菌素长效注射液与阿维菌素普通注射液(阿福丁注射液)药物动力学的比较研究。绵羊血浆经提取、纯化、真空干燥和荧光衍生化后,用荧光高效液相色谱法进行检测。用3P87药代动力学分析软件对所测得的结果进行分析,得出以下药代动力学结果:阿维菌素长效注射液和阿福丁注射液在绵羊体内均呈二室代谢模型。长效注射液以1mg/kg体重进行颈部皮下注射得到以下药动学参数:吸收半衰期t1/2α=9.59h,消除半衰期t1/2β=292.97h,达峰时间tmax=47.46h,最大血药浓度Cmax=13.91ng/mL,曲线下面积AUC=6235.48ng/(mL·h),消除率ClB=0.034L/(kg·h),表观分布容积Vd=13.7L/kg。将阿福丁注射液以0.2mg/kg体重进行颈部皮下注射得到以下药动学参数:吸收半衰期t1/2α=9.05h,消除半衰期t1/2β=144.34h,达峰时间tmax=12.63h,最大血药浓度Cmax=8.52ng/mL,曲线下面积AUC=1017.35ng/(mL·h),消除率ClB=0.22L/(kg·h),表观分布容积Vd=14.5L/kg。研究结果表明:阿维菌素长效注射液比普通注射液吸收慢、消除慢,在体内维持有效血药浓度的时间长,长效注射液维持有效血药浓度(0.5ng/mL血浆)的时间长于49d,而阿福丁注射液不足21d。
Study on pharmacokinetics of two kinds of injection of avermectin,common injection(control)and prolonged injection(test), was carried out. AVM was extracted with methanol from plasma samples and cleaned up by C 18 solid phase extraction (SPE) column, dried and derived. Then the samples were analyzed by HPLC. Prolonged AVM absorption halflife (P<0.05) and delayed plasma peak concentration were observed following the SC administration of the AVMTEST formula. The plasma drug residual time and elimination halflife of AVM were significantly longer after injection with the AVMTEST formula. AVM plasma concentrations were above 0.5 ng/mL for less than 21 days with control and more than 49 days with test.
出处
《中国兽药杂志》
2003年第3期18-21,共4页
Chinese Journal of Veterinary Drug
