对乙酰氨基酚琥珀酸酯在家兔体内的药代动力学研究  

Pharmacokinetics characteristics of paracetamol succinate in rabbits

作　　者：金超[1] 程妍[2] 符华林[1] 蒋公建 舒刚[1] 刘梦娇[1] 周建瑜[1] 戴玉娇 

机构地区：[1]四川农业大学动物医学院药学系,四川雅安625014 [2]四川大学华西药学院,四川成都610041 [3]重庆先锋动物药业有限公司,重庆万州404100 [4]重庆市潼南县动物卫生监督所,重庆潼南402660

出　　处：《湖南农业大学学报（自然科学版）》2014年第4期399-403,共5页Journal of Hunan Agricultural University(Natural Sciences)

基　　金：教育部"长江学者和创新团队发展计划"创新团队项目(IRT0848)

摘　　要：对乙酰氨基酚琥珀酸酯(AP–S)进入动物机体后能很快分解成对乙酰氨基酚(APAP)。为探明对乙酰氨基酚琥珀酸酯在家兔体内的动力学特征,先建立检测APAP的高效液相色谱法(HPLC),再将6只家兔分别单剂量肌肉注射对乙酰氨基酚琥珀酸酯,采用建立的高效液相色谱法检测家兔体内对乙酰氨基酚的血药浓度;用DAS2.0药代动力学软件计算药代动力学参数。结果显示,给家兔单剂量注射对乙酰氨基酚琥珀酸酯后,主要的药代动力学参数Cmax为(95.44±1.42)mg/L,tmax为0.25 h,AUC(0–∞)为(84.08±7.02)mg/L·h。综合分析表明,对乙酰氨基酚琥珀酸酯在动物体内可迅速转化为对乙酰氨基酚,药物达峰时间短,发挥药效快。Acetaminophen succinate（AP-S） can be quickly broken into acetaminophen（APAP） after administrating into animal body. In order to investigate acetaminophen kinetics of succinate in rabbits, HPLC assay for APAP content detection was established first, then single dose of AP-S was injected intramuscularly into 6 rabbits respectively. Drug concentration in serum was detemined by the established HPLC, and the data was analysed by DAS 2.0 pharmacokinetic software to obtain the pharmacokinetic parameters. The results showed that the main pharmacokinetic parameters after intramuscular injection of acetaminophen succinate by a single dose in rabbits were as follows： Cmax is（95.44 ± 1.42） mg/L, tmax is 0.25 h, AUC（0-∞）is（84.08 ± 7.02） mg/（L·h）. Comprehensive analysis showed that acetaminophen succinate in animal body can be quickly converted into acetaminophen, the drug peak time is short, thus, the drug efficacy is displayed quickly.

关 键 词：家兔 对乙酰氨基酚琥珀酸酯 对乙酰氨基酚 药代动力学 高效液相色谱法 

分 类 号：S859.7[农业科学—临床兽医学]