Trnavská Z, Trnavský K
Eur J Clin Pharmacol. 1980 Nov;18(5):403-6. doi: 10.1007/BF00636793.
Protein binding of salicylate in synovial fluid and plasma from patients with rheumatoid arthritis was studied by equilibrium dialysis. Protein binding in the synovial fluid was considerably lower at all salicylate concentrations studied (0.07 - 2.2 mM). Scatchard plots of the data were analyzed assuming binding to two classes of binding sites, each plasma sample being diluted to an albumin concentration equal to that in synovial fluid from the same patient. Binding to the primary binding sites was considerably decreased in synovial fluid in comparison with plasma. The affinity of the secondary binding sites was slightly lower. Thus, at a low therapeutic drug concentration, the decreased binding of salicylate to synovial fluid protein in patients with rheumatoid arthritis could mainly be accounted for by decreasing affinity of binding to the primary binding sites.
通过平衡透析研究了类风湿性关节炎患者滑液和血浆中水杨酸盐的蛋白质结合情况。在所研究的所有水杨酸盐浓度(0.07 - 2.2 mM)下,滑液中的蛋白质结合率均显著较低。假设与两类结合位点结合,对数据进行Scatchard作图分析,每个血浆样本都稀释至与同一患者滑液中白蛋白浓度相同。与血浆相比,滑液中与主要结合位点的结合显著减少。次要结合位点的亲和力略低。因此,在低治疗药物浓度下,类风湿性关节炎患者滑液蛋白中水杨酸盐结合率降低主要是由于与主要结合位点结合的亲和力降低所致。