Kurowski M, Dunky A, Geddawi M
Curr Med Res Opin. 1987;10(7):494-501. doi: 10.1185/03007998709112409.
Six patients suffering from rheumatoid arthritis with massive knee joint effusions were treated with single daily doses of 600 mg pirazolac, a novel non-steroidal anti-inflammatory drug, for 3 days. Before the first dose, 3 hours after the second and the third dose, specimens of plasma and synovial fluid were drawn simultaneously. Plasma and synovial fluid concentrations of pirazolac, as determined by HPLC, amounted to 47.9 micrograms/ml and 19.8 micrograms/ml (Day 2) and 55.5 micrograms/ml and 18.7 micrograms/ml (Day 3), respectively. The samples were analyzed for PGE2, LTB4, LTC4 and LTD4 applying various extraction procedures and subsequent radioimmunoassays. PGE2 levels decreased during treatment from 928 pg/ml to 443 pg/ml after the third dose of pirazolac. LTB4 levels were slightly but insignificantly augmented. LTC4 and LTD4 concentrations were below the detection limit prior to and after administration of the drug.
六名患有类风湿性关节炎且膝关节大量积液的患者,每日单次服用600毫克吡唑酸(一种新型非甾体抗炎药),持续治疗3天。在首次给药前、第二次和第三次给药后3小时,同时采集血浆和滑液样本。通过高效液相色谱法测定,吡唑酸的血浆和滑液浓度在第2天分别为47.9微克/毫升和19.8微克/毫升,在第3天分别为55.5微克/毫升和18.7微克/毫升。采用各种提取程序及后续放射免疫分析法对样本进行PGE2、LTB4、LTC4和LTD4分析。治疗期间,吡唑酸第三次给药后,PGE2水平从928皮克/毫升降至443皮克/毫升。LTB4水平略有升高,但无显著差异。给药前后,LTC4和LTD4浓度均低于检测限。