Mori Y, Sakai Y, Kuroda N, Yokoya F, Toyoshi K, Horie M, Baba S
Drug Metab Dispos. 1984 Nov-Dec;12(6):767-71.
The urinary metabolites of 2-(4-(2-thienylcarbonyl)phenyl)propionic acid (suprofen, S) in rats were analyzed by radio-GC, GC/MS, or 1H NMR technique. Radio-GC analysis of trimethylsilylated materials after TLC separation of intact urine showed the presence of three radioactive peaks with the retention times corresponding to the authentic S, 2-(4-(2-thienylhydroxymethyl)phenyl)propionic acid, and 2-(4-carboxyphenyl)propionic acid. About 40% of the total radioactivity appearing in the 0-24-hr urine was accounted for by the three metabolites and their conjugates. The identification of these metabolites was confirmed by comparison of the MS spectra of urine, in which rats were administered an equimolar mixture of S and S[phenyl-d4], with those of synthetic standards. The labile metabolites of S, corresponding to about 32% of the total radioactivity appearing in the 0-24-hr urine, were isolated and purified by ether extraction from the fresh urine and GC/MS or HPLC. GC/MS of the methylated metabolite revealed the consistent presence of the ion peaks at m/z 304, 245, 217, and 141, indicative of a dimethylated product with monohydroxy group on the thiophene ring. Analysis of the 1H NMR spectrum demonstrated the metabolite to be 2-(4-(5-hydroxy-2-thienylcarbonyl)phenyl)propionic acid.
采用放射性气相色谱法（radio-GC）、气相色谱/质谱联用法（GC/MS）或核磁共振氢谱技术（1H NMR）分析了大鼠体内2-(4-(2-噻吩甲酰基)苯基)丙酸（舒洛芬，S）的尿液代谢产物。完整尿液经薄层色谱（TLC）分离后，对三甲基硅烷化产物进行放射性气相色谱分析，结果显示存在三个放射性峰，其保留时间分别对应于标准品S、2-(4-(2-噻吩羟甲基)苯基)丙酸和2-(4-羧基苯基)丙酸。0至24小时尿液中出现的总放射性约40%由这三种代谢产物及其结合物构成。通过比较给大鼠注射S与S[苯基-d4]等摩尔混合物后的尿液质谱图与合成标准品的质谱图，证实了这些代谢产物的鉴定。对应于0至24小时尿液中出现的总放射性约32%的S的不稳定代谢产物，通过从新鲜尿液中用乙醚萃取并经GC/MS或高效液相色谱法（HPLC）进行分离和纯化。甲基化代谢产物的GC/MS分析显示，在m/z 304、245、217和141处始终存在离子峰，表明该产物为噻吩环上带有单羟基的二甲基化产物。1H NMR谱分析表明该代谢产物为2-(4-(5-羟基-2-噻吩甲酰基)苯基)丙酸。
