Lee S, Johnson D, Klein J, Eppler J
Division of Clinical Pharmacology/Toxicology, Hospital for Sick Children, University of Toronto, Ontario, Canada.
Vet Hum Toxicol. 1995 Jun;37(3):224-5.
As part of a pilot project establishing a porcine model for aspirin overdose, the percentage protein binding of acetylsalicylate (ASA) and salicylate (SA) in porcine and human sera was evaluated in vitro over a range of concentrations. Serum from 2 pigs and 4 humans were spiked with ASA concentrations of 0.5-100 mg/dL and SA concentrations of 1-120 mg/dL. Protein binding for each concentration of ASA and SA was determined using radiolabeled drug and ultrafiltration with the Centrifree micropartition system. The percentage protein binding for ASA in pig and human sera were similarly low (< 50%) for all concentrations evaluated. Percentage protein binding for SA for pig and human sera were high (approximately 90% and 80%) at low therapeutic concentrations, but then declined to approximately 30% at higher toxic concentrations (120 mg/dL). The protein binding of ASA and SA over a range of concentrations was similar for porcine and human sera.
作为建立阿司匹林过量猪模型的试点项目的一部分，在体外评估了猪和人血清中乙酰水杨酸（ASA）和水杨酸（SA）在一系列浓度范围内的蛋白质结合百分比。向2头猪和4名人类的血清中加入浓度为0.5 - 100mg/dL的ASA和浓度为1 - 120mg/dL的SA。使用放射性标记药物和Centrifree微分离系统进行超滤，测定每种浓度的ASA和SA的蛋白质结合情况。在所评估的所有浓度下，猪和人血清中ASA的蛋白质结合百分比同样较低（<50%）。猪和人血清中SA的蛋白质结合百分比在低治疗浓度时较高（分别约为90%和80%），但在较高毒性浓度（120mg/dL）时降至约30%。猪和人血清中ASA和SA在一系列浓度范围内的蛋白质结合情况相似。
