Walters C L, Gillatt P N, Palmer R C, Smith P L, Reed P I
Department of Biochemistry, University of Surrey, Guildford, UK.
IARC Sci Publ. 1987(84):351-4.
Application of the WHO Nitrosation Assay Procedure (NAP test) to a range of potentially nitrosatable drugs has given rise to considerable variations in the formation of volatile N-nitrosamines and N-nitroso compounds as a group. No nitrosation whatsoever was observed with 40 mM nitrite in some instances. In simulating more closely the conditions likely to be encountered in the human stomach, however, the order of susceptibility of the drugs to N-nitrosation has proved to be very different. At a constant nitrite concentration of 25 microM, which is considered to represent the upper limit of those likely to be encountered in the acidic human stomach, the drugs giving rise to the greatest yields of products reacting as N-nitroso compounds from a maximum adult dose were the penicillins, G, V, cloxacillin and ampicillin.
将世界卫生组织亚硝化测定程序（NAP 试验）应用于一系列潜在可亚硝化的药物时，挥发性 N-亚硝胺和 N-亚硝基化合物作为一个整体的形成出现了相当大的差异。在某些情况下，使用 40 mM 亚硝酸盐时未观察到任何亚硝化现象。然而，在更接近模拟人体胃中可能遇到的条件时，药物对亚硝化的敏感顺序已证明有很大不同。在恒定的 25 microM 亚硝酸盐浓度下，这一浓度被认为代表了在酸性人体胃中可能遇到的上限，从最大成人剂量产生作为 N-亚硝基化合物反应的产物产量最高的药物是青霉素 G、V、氯唑西林和氨苄西林。
