Tsuchiya T, Terakawa M, Ishibashi K, Noguchi H, Kato R
Arzneimittelforschung. 1980;30(10):1650-3.
Following i.v. administration of 14C-labelled 2-(2',6'-dichloroanilino) phenylacetic acid (14C-diclofenac) (25 mg/kg) to dogs, 65% of the dose of total radioactivity was excreted in the bile in the first 6 h. A trace of unchanged diclofenac and three metabolites were demonstrated in the bile by 2-dimensional TLC. Two of these metabolites were identified as diclofenac acyl-glucuronide (80% of total radioactivity in the bile) and taurine conjugate (10%); the third was an unknown metabolite (2%). Diclofenac acyl-glucuronide was hydrolyzed by weak alkaline and beta-glucuronidase. Intraduodenally administered diclofenac acyl-glucuronide was absorbed, and then excreted in the bile again. This suggests that diclofenac acyl-glucuronide is hydrolyzed in the intestine, and undergoes enterohepatic circulation. The plasma half-life of diclofenac was 1.3 h in dogs.
给狗静脉注射14C标记的2-(2',6'-二氯苯胺基)苯乙酸（14C-双氯芬酸）（25毫克/千克）后，在最初6小时内，总放射性剂量的65%经胆汁排出。二维薄层色谱法显示胆汁中有微量未变化的双氯芬酸和三种代谢物。其中两种代谢物被鉴定为双氯芬酸酰基葡萄糖醛酸（占胆汁中总放射性的80%）和牛磺酸共轭物（10%）；第三种是未知代谢物（2%）。双氯芬酸酰基葡萄糖醛酸可被弱碱性物质和β-葡萄糖醛酸酶水解。十二指肠内给药的双氯芬酸酰基葡萄糖醛酸被吸收，然后再次经胆汁排出。这表明双氯芬酸酰基葡萄糖醛酸在肠道内被水解，并经历肝肠循环。双氯芬酸在狗体内的血浆半衰期为1.3小时。
