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类风湿关节炎中托美丁的动力学及滑液中前列腺素E水平

Tolmetin kinetics and synovial fluid prostaglandin E levels in rheumatoid arthritis.

作者信息

Dromgoole S H, Furst D E, Desiraju R K, Nayak R K, Kirschenbaum M A, Paulus H E

出版信息

Clin Pharmacol Ther. 1982 Sep;32(3):371-7. doi: 10.1038/clpt.1982.174.

DOI:10.1038/clpt.1982.174
PMID:7105628
Abstract

Tolmetin kinetics were determined in the plasma and synovial fluid of five rheumatoid arthritis patients after they had ingested tolmetin (400 mg every 6 hr) for 7 days. Tolmetin was rapidly absorbed, with average peak levels in plasma and synovial fluid occurring at 45 min and 2 hr. The drug concentration in synovial fluid was higher than that in plasma for prolonged periods, while the rates of elimination from both plasma and synovial fluid were similar. The average half-lives of tolmetin in plasma and synovial fluid were 6.77 +/- 1.47 hr and 6.90 +/- 2.3 hr. Total prostaglandin E levels in synovial fluid of these patients were suppressed for at least 24 hr after the last dose of tolmetin, suggesting that PGE synthesis continues to be suppressed even by the very low concentrations of tolmetin remaining after 24 hr.

摘要

在五名类风湿性关节炎患者连续7天服用托美汀(每6小时400毫克)后,测定了其血浆和滑液中的托美汀动力学。托美汀吸收迅速,血浆和滑液中的平均峰值水平分别出现在45分钟和2小时。滑液中的药物浓度在较长时间内高于血浆中的浓度,而血浆和滑液的消除速率相似。托美汀在血浆和滑液中的平均半衰期分别为6.77±1.47小时和6.90±2.3小时。在最后一剂托美汀后,这些患者滑液中的总前列腺素E水平至少被抑制了24小时,这表明即使在24小时后残留的托美汀浓度非常低,PGE合成仍持续受到抑制。

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