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目的 :鉴定新型抗炎镇痛剂SFZ 4 7[3H 1,2 二氢 2 ( 4 甲基苯胺基 )甲基 1 吡咯里嗪酮 ]在家兔体内的羟基化及其结合型代谢产物。方法 :选择 4只健康家兔单剂量口服 10 0mgSFZ 4 7,收集 0～ 10h的尿样。将未经或经过 β D 葡萄糖苷酸酶 /硫酸酯酶水解的尿样以Sep PakC18固相萃取柱纯化后 ,采用LC/MSn 方法对尿中推测的代谢物分别进行选择离子监测 (SIM )和多级全扫描质谱 (MSn)分析。结果 :在尿中首次检测到SFZ 4 7羟基化及其 β D 葡糖苷酸与硫酸结合型代谢物。结论 :SFZ 4 7在家兔体内主要代谢途径应为苯环上的甲基先氧化成羟甲基和羧基 ,再分别与 β D 葡糖醛酸或硫酸结合
OBJECTIVE: To identify the hydroxylation and its binding metabolites of SFZ 4 7 [3H 1,2 dihydro 2 (4-methylanilino) methyl-1-pyrrolizinone] in rabbits. Methods: Four healthy rabbits were given a single oral dose of 10 0 mg SFZ 4 7 and urine samples were collected for 0-10 hours. The urinary samples without or with β-D glucuronidase / sulfatase were purified by Sep Pak C18 solid phase extraction column, and the selected metabolites in the urine were subjected to selective ion monitoring (SIM) and LC / Multistage full scan mass spectrometry (MSn) analysis. Results: SFZ 4 7 hydroxylation and its β D glucuronide and sulfate binding metabolites were first detected in urine. CONCLUSION: The main metabolic pathway of SFZ 4 7 in rabbits should be the oxidation of methyl groups on the phenyl ring to hydroxymethyl and carboxyl groups, and then to β D glucuronic acid or sulfuric acid respectively