【摘要】 选用体重25 kg左右的长×大二元杂健康猪8头,按双周期双交叉试验设计,进行静脉注射与内服阿散酸(10 mg/kg)的药动学研究。采用高效液相色谱法测定猪血浆中阿散酸的浓度,用统计矩原理处理血浆药物浓度-时间数据。结果显示:健康猪静脉注射阿散酸后的主要药动学参数为β=0.55 h-1±0.01h-1,t1/2β=1.26h±0.03 h,Vz=0.30L/kg±0.01 L/kg,Vdss=0.29 L/kg±0.01 L/kg,CL=0.17 L/(kg.h)±0.01 L/(kg.h),MRT=1.75 h±0.07 h,AUC=60.44μg/mL.h±0.01μg/mL.h;内服给药的主要药动学参数为β=0.39 h-1±0.02 h-1,t1/2β=1.79 h±0.09 h,tmax=1.81 h±0.09 h,Cmax=3.43μg/mL±0.53μg/mL,MRT=3.95 h±0.13 h,AUC=15.12μg/mL.h±0.01μg/mL.h,F=24.5%±3.4%。研究结果表明,阿散酸在健康猪体内的药动学特征为内服吸收迅速,血药浓度达峰时间短,但药物峰浓度低,绝对生物利用度低,消除快。更多还原

【Abstract】 Eight healthy crossed-bred(Yorkshire×Landrance)pigs,with an average weight of 25.0kg,were randomly assigned to two dietary treatments,and a randomized two period cross-over design was performed for single intravenous(i.v.) and oral administration of arsanilic acid(ASA)at the dose of 10.0mg/kg.Blood was taken in different preset times following drug administration and the concentrations of arsanilic acid in plasma were determined by HPLC using an ultraviolet detector.The concentrations versus time were analyzed with the moncompartmental approach based on statistical moment theory.In results,the main pharmacokinetics parameters of arsanilic acid in pigs after i.v.administration were as follows:β=0.55h-1±0.01h-1,t1/2β=1.26h±0.03h,Vz=0.30L/kg±0.01L/kg,Vdss=0.29L/kg±0.01L/kg,CL=0.17L/(kg·h)±0.01L/(kg·h),MRT=1.75h±0.07h,AUC= 60.44μg/mL·h±0.01μg/mL·h.The main pharmacokinetics parameters after oral dosing of arsanilic acid in pigs,were as follows:β=0.39h-1 ±0.02h-1,t1/2β =1.79h±0.09h,tmax=1.81h±0.09h,Cmax=3.43μg/mL± 0.53μg/mL,MRT=3.95h±0.13h,AUC=15.12μg /mL·h±0.01μg /mL·h,F=24.5%±3.4%.In conclusion,arsanilic acid was absorbed quickly,and reached the tmax shortly with low Cmax and low bioavailability,and eliminated quickly after oral administration in pigs.更多还原