Ludwig B
Dtsch Tierarztl Wochenschr. 1989 May;96(5):243-8.
If the principal pharmacokinetic parameters of a veterinary drug-such as its elimination half-life from blood plasma, volume of distribution, plasma protein binding and metabolism-are known, then the presence and concentration of residues in animal tissue after administration of the drug can be predicted. This makes it possible to reduce the number of animals required by conventional residue testing and satisfies a legitimate demand of animal welfare groups. Using radioactively labelled drugs, the ratio of the parent substance to its metabolites can be established. Thus as a rule the determination of parent substance is sufficient for the routine determination of residues in foodstuffs. This is true in particular of sulfonamides. The pharmacokinetics of this class of substances are such that their main metabolites are eliminated from the animal's body faster than the parent substance. Other examples given are ceftriaxone, carprofen und climazolam.
如果一种兽药的主要药代动力学参数已知,比如其从血浆中的消除半衰期、分布容积、血浆蛋白结合率和代谢情况,那么给药后动物组织中残留的存在及浓度就可以预测。这使得减少传统残留检测所需动物数量成为可能,并满足了动物福利组织的合理需求。使用放射性标记药物,可以确定母体物质与其代谢物的比例。因此,通常测定母体物质就足以进行食品中残留的常规测定。磺胺类药物尤其如此。这类物质的药代动力学特点是其主要代谢物从动物体内消除的速度比母体物质快。给出的其他例子有头孢曲松、卡洛芬和氯咪唑仑。