新疆医科大学学报

目的:研究自制的阿维菌素缓释注射液在家兔体内的药物动力学过程。方法:健康家兔6只皮下注射10mg/kg阿维菌素缓释注射液,70d内定时从兔耳缘静脉取血,按照所建立的血浆样品预处理方法及高效液相色谱紫外检测(HPLC-UV)法测定血中药物浓度,其血药浓度时间数据经3p87程序处理后,获取药物动力学参数。结果:阿维菌素缓释注射液在家兔血中药物动力学符合二房室模型处置特征,主要药物动力学参数:达峰时间(Tmax)1.43d,峰浓度(Cmax)35.9ng/ml,曲线下面积(AUC)560(ng/ml)×d。结论:此自制的阿维菌素缓释注射液具有近2个月的长效作用时间。

Objective: To study the plasma pharmacokinetics of avermectin sustained-release injection which was made by ourself over a 70-day period in rabbit. Methods: Avermectin sustained-release injection for rabbits (as a single subcutaneous formulation) was used at a dose of 10 mg/kg. The plasma concentration of avermectin were determined using high-performance liquid chromatography (HPLC) with UV detection method. Pharmacokinetic analysis of avermectin sustained-release injection plasma concentrations was performed using 3p87 program. Results: Plasma concentrations were fitted to an equation corresponding to a two-compartmental model with an absorption phase(weight=1/c\+2). That the peak plasma concentration (Cmax) was 35.9 ng/ml, the time to Cmax (Tmax) was 1.43 d, the area under the curve from time 0 to infinity post-injection (AUC) was 560 ng/ml×d. Conclusion: The results indicate that this avermectin sustained-release injection made by ourself has nearly two-month long-acting effect in rabbits.