Schneider H T, Nuernberg B, Dietzel K, Brune K
Department of Medicine I, University of Erlangen-Nuernberg, FRG.
Br J Clin Pharmacol. 1990 Jan;29(1):127-31. doi: 10.1111/j.1365-2125.1990.tb03613.x.
In view of evidence in animals that enterohepatic recirculation of non-steroidal anti-inflammatory drugs contributes to small intestinal mucosal damage we have investigated the extent of biliary elimination of three nonsteroidals. Ibuprofen (n = 3), diclofenac (n = 2) and indomethacin (n = 3) were given to six patients with a percutaneous transhepatic cholangiodrainage placed in the bile duct system. One patient received all three drugs. The mean biliary elimination of ibuprofen was 0.82% of the given dose compared with 50.41% urinary excretion. When diclofenac or indomethacin was administered 4.62% and 6.40% of the dose were found in bile, whereas 34.73% and 32.22% (means) were recovered from urine, respectively. The mean percentage eliminated in bile as unchanged drug and active phase II metabolites was 0.15% for ibuprofen, 1.09% for diclofenac and 5.02% for indomethacin.
鉴于动物实验证据表明非甾体抗炎药的肠肝循环会导致小肠黏膜损伤，我们研究了三种非甾体抗炎药的胆汁排泄程度。对6例经皮经肝胆道引流置于胆管系统的患者给予布洛芬（n = 3）、双氯芬酸（n = 2）和吲哚美辛（n = 3）。1例患者接受了所有三种药物。布洛芬的平均胆汁排泄量为给药剂量的0.82%，而尿排泄量为50.41%。给予双氯芬酸或吲哚美辛时，胆汁中分别发现给药剂量的4.62%和6.40%，而尿液中的回收率分别为34.73%和32.22%（均值）。以原形药物和活性II期代谢物形式经胆汁排泄的平均百分比，布洛芬为0.15%，双氯芬酸为1.09%，吲哚美辛为5.02%。
