【摘要】 皮下注射伊维菌素 (IVM )微球悬液 (5 0mg/kg及 10 0mg/kg)和害获灭 (1%伊维菌素 ,0 5mg/kg) ,RP HPLC UV法定量 ,研究了IVM在家兔体内的药物动力学。害获灭皮下注射给药 ,药 时数据符合一级吸收一室开放模型 ,主要动力学参数为 :t1/2ka=7 2 4± 2 96h ;t1/2ke=36 38± 8 6 6h ;tmax=2 1 4 6± 4 82h ;Cmax=2 2 53± 2 32ng/ml;AUC =174 9± 318ng/1.h ,其动力学参数表现比较明显的个体差异 ,且与其它动物有明显差别。微球皮下注射一周后 ,血药浓度呈较稳定状态 ,到第 4 2天 (高剂量组 )和第 32天 (低剂量组 ) ,血浆中测不出H2 B1a(低于 2 5ng/ml)。以房室模型拟合 ,微球高低剂量组均符合有吸收二室开放模型 ,主要药动学参数均表现显著的个体差异。更多还原

【Abstract】 The pharmacokinetics of ivermectin(IVM)loaded in Poly( d,l lactic acid)(PLA)microspheres(MS)in rabbits was investigated.MS suspensions were given to the animals subcutaneously at the IVM dosage of 5 0 and 10 0mg/kg,respectively.IVOMEC(0 5mg/kg,s.c)was concluded in the experiment for comparison.Blood samples were collected after administration and the plasmas were separated.Ivermectin was extracted from the plasma into methylene chloride,and an analytical sample was prepared by evaporating organic solvent and dissolving the residue into methanol.Reversed phase HPLC with UV photometric detection was used to determine ivermectin concentration,at accuracy of 2 5ng/ml.The plasma drug concentration data of IVOMEC could be best described as a one compartment open model with first order absorption.The pharmacokinetic parameters were as follows:t 1/2ka 7 24±2 96h,t 1/2ke 36 38±8 66h,t max 21 46±4 82h,C max 22 53±2 32ng/ml,and AUC 1749±318ng/1.h.After subcutaneous injection of MS,the drug concentration time curve had obvious individual differences.One week after administration,the plasma IVM concentration kept at steady state for 5(high dosage)or 3(low dosage)weeks. [WT5HZ]更多还原