Stella V J, Varia S A, Riedy M
J Pharm Sci. 1979 May;68(5):648-50. doi: 10.1002/jps.2600680537.
A rat plasma salicylamide assay was developed using ring-labeled tritiated salicylamide, synthesized by reacting salicylamide with tritium oxide in the presence of heptafluorobutyric acid. The reaction yielded 3H-salicylamide of specific activity up to 8.41 mCi/mmole, 60% yield. Plasma containing 3H-salicylamide and its metabolites was extracted with a toluene-based scintillation fluid, which was subsequently counted. Specificity for free salicylamide was demonstrated by radio chemical and standard fluorescence plasma salicylamide level-time curves. Specificity resulted from nonextraction of the salicylamide sulfate and glucuronide metabolites. Sulfatase and beta-glucuronidase treatment allowed the analysis of plasma sulfate and glucuronide conjugates as free salicylamide. This procedure should be effective for the analysis of salicylamide and its metabolites in the presence of similar phenolic compounds.
利用环标记的氚化水杨酰胺开发了一种大鼠血浆水杨酰胺测定法，该氚化水杨酰胺是通过在七氟丁酸存在下使水杨酰胺与氧化氚反应合成的。该反应产生了比活高达8.41 mCi/mmol、产率为60%的3H-水杨酰胺。含有3H-水杨酰胺及其代谢物的血浆用甲苯基闪烁液萃取，随后进行计数。通过放射化学和标准荧光血浆水杨酰胺水平-时间曲线证明了对游离水杨酰胺的特异性。特异性源于硫酸水杨酰胺和葡糖醛酸代谢物不被萃取。硫酸酯酶和β-葡糖醛酸酶处理允许将血浆硫酸盐和葡糖醛酸共轭物作为游离水杨酰胺进行分析。该方法在存在类似酚类化合物的情况下，对于分析水杨酰胺及其代谢物应该是有效的。
