Bird H A, Allen J G, Dixon J S, Wright V
Br J Rheumatol. 1985 Nov;24(4):351-6. doi: 10.1093/rheumatology/24.4.351.
In view of the paucity of information on the synovial-fluid pharmacokinetics of nonsteroidal anti-inflammatory drugs with a long half-life, we have compared the pharmacokinetics of tenoxicam (Tilcotil, Mobiflex) in plasma and synovial fluid in six patients with polyarthritis causing knee effusion. Plasma and synovial-fluid concentrations of tenoxicam were measured up to 96 h after an oral dose of a single 40 mg tablet. A full pharmacokinetic analysis was performed. Tenoxicam passed into synovial fluid attaining a peak concentration significantly later than that for plasma. However, the mean half-life for synovial fluid (45 h) was not significantly different from that for plasma (42 h). Comparison of area under the curve (AUC) indicated the total exposure of the synovial fluid to tenoxicam was consistent in different patients, comprising 50-60% of the corresponding plasma levels in every case. In the case of tenoxicam, synovial fluid exhibits the pharmacokinetic properties of a peripheral 'tissue' compartment.
鉴于关于半衰期较长的非甾体抗炎药在滑液中的药代动力学信息匮乏,我们比较了6例因多关节炎导致膝关节积液患者血浆和滑液中替诺昔康(替诺昔康片,莫比可)的药代动力学。口服单剂量40mg片剂后,测定长达96小时的血浆和滑液中替诺昔康的浓度,并进行完整的药代动力学分析。替诺昔康进入滑液,其达到峰值浓度的时间明显晚于血浆。然而,滑液的平均半衰期(45小时)与血浆的平均半衰期(42小时)无显著差异。曲线下面积(AUC)比较表明,不同患者滑液中替诺昔康的总暴露量一致,每种情况下均占相应血浆水平的50-60%。就替诺昔康而言,滑液表现出外周“组织”隔室的药代动力学特性。