骨关节炎患者滑液中萘普生的动力学
Naproxen kinetics in synovial fluid of patients with osteoarthritis.
作者信息
Bruno R, Iliadis A, Jullien I, Guego M, Pinhas H, Cunci S, Cano J P
机构信息
Recherche Syntex France, Leuville-sur-Orge.
出版信息
Br J Clin Pharmacol. 1988 Jul;26(1):41-4. doi: 10.1111/j.1365-2125.1988.tb03361.x.
Abstract
- The kinetics of naproxen in synovial fluid were studied in 407 osteoarthritic outpatients with knee effusion requiring aspiration, following a single 1100 mg oral dose of naproxen sodium. 2. The drug concentration-time profiles were described by a biexponential function. Naproxen entered synovial fluid rapidly, reaching a maximum concentration of 36 mg l-1 (Cmax) at 7.5 h. The first order input rate constant (kOs) was 0.41 +/- 0.15 h-1 with a lag time (tlag) of 0.24 +/- 0.36 h. 3. Elimination from the fluid was slow (t1/2 = 31 +/- 12 h) and appreciable drug concentrations were still measurable (27 mg l-1) after 24 h. 4. During once daily dosing of naproxen sodium, naproxen should accumulate in synovial fluid, a steady-state being achieved within a week of treatment. The predicted accumulation ratio based on trough concentration was 2.4.
摘要
- 在407例需要进行膝关节积液抽吸的骨关节炎门诊患者中，口服单次1100毫克萘普生钠后，研究了萘普生在滑液中的动力学。2. 药物浓度-时间曲线用双指数函数描述。萘普生迅速进入滑液，在7.5小时时达到最大浓度36毫克/升（Cmax）。一级输入速率常数（kOs）为0.41±0.15小时-1，滞后时间（tlag）为0.24±0.36小时。3. 从滑液中消除缓慢（t1/2 = 31±12小时），24小时后仍可测得相当可观的药物浓度（27毫克/升）。4. 在每日一次服用萘普生钠期间，萘普生应在滑液中蓄积，治疗一周内达到稳态。基于谷浓度预测的蓄积比为2.4。
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