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类风湿关节炎患者体内吲哚美辛的经滑膜动力学及体外环氧合酶抑制作用

Transsynovial kinetics of indoprofen in patients with rheumatoid arthritis and cyclooxygenase-inhibition in vitro.

作者信息

Kurowski M, Schiemann A, Siebler D

机构信息

Institute of Pharmacy, Free University of Berlin West, Federal Republic of Germany.

出版信息

Int J Clin Pharmacol Res. 1988;8(4):287-93.

PMID:3141302
Abstract

Twenty-four patients suffering from rheumatoid arthritis and requiring articular punctures were treated with 200 mg of indoprofen thrice daily for four days. The subjects were divided into four groups each of six patients. Following the last dose, blood and synovial fluid samples were taken simultaneously according to different time schedules. Maximum plasma levels of 17.5 micrograms/ml were observed after 2.5 h. Peak synovial fluid concentrations amounted to 8.1 micrograms/ml 4 h following the last dose. Elimination from synovial fluid occurred at 10.6 h compared to 9.3 h from plasma. Free synovial fluid levels of approximately 50 ng/ml are in the range of concentrations necessary for cyclooxygenase inhibition in mouse peritoneal macrophages.

摘要

24名患有类风湿性关节炎且需要进行关节穿刺的患者,接受每日三次、每次200毫克吲哚美辛的治疗,为期四天。受试者被分为四组,每组6名患者。在最后一剂药物服用后,根据不同的时间表同时采集血液和滑液样本。服药2.5小时后观察到血浆最高水平为17.5微克/毫升。最后一剂药物服用4小时后,滑液中的峰值浓度达到8.1微克/毫升。滑液中的消除时间为10.6小时,而血浆中的消除时间为9.3小时。滑液中约50纳克/毫升的游离水平处于抑制小鼠腹腔巨噬细胞中环氧化酶所需的浓度范围内。

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