Ott H, Meier J
Scand J Rheumatol Suppl. 1978(21):12-4. doi: 10.3109/03009747809095667.
In 13 patients with hydrarthrosis of the knee, samples of synovial fluid and blood were drawn at regular intervals, following a single oral dose of 600 mg proquazone. The concentrations of the unchanged drug were measured fluorimetrically and those of its three principal, active metabolites by high pressure liquid chromatography. The absorption and distribution of proquazone and its metabolites were rapid. Measurable--in some cases considerable--concentrations were to be found in both the synovial fluid and serum as early as 30 minutes after intake. High concentrations were still present up to 7 hours after intake. Considerable variations were observed, both between patients and over time for each patient, so that only qualitative rather than quantitative kinetic conclusions could be drawn from the results. The concentrations were generally lower in the synovial fluid than in the serum, which may be ascribed to the drug's high protein binding.
在13例膝关节积水患者中,单次口服600毫克丙氧苯唑后,定期采集滑液和血液样本。采用荧光法测定原形药物的浓度,用高压液相色谱法测定其三种主要活性代谢物的浓度。丙氧苯唑及其代谢物的吸收和分布迅速。摄入后30分钟,在滑液和血清中即可检测到——在某些情况下浓度相当可观——的药物浓度。摄入后7小时仍存在高浓度。观察到患者之间以及每位患者不同时间的浓度存在相当大的差异,因此从结果中只能得出定性而非定量的动力学结论。滑液中的浓度通常低于血清中的浓度,这可能归因于该药物的高蛋白结合率。