Day R O, Shen D D, Azarnoff D L
Clin Pharmacokinet. 1983 May-Jun;8(3):263-71. doi: 10.2165/00003088-198308030-00005.
Average steady-state serum salicylate concentrations and salicyluric acid (SU) formation rates were measured in 4 subjects with rheumatoid arthritis. After a salicylate washout period (1 month), the mean observed maximum formation rate of SU was determined by collecting frequent urine samples after a single oral dose of salicylate (35 mg/kg). The patients were then commenced on appropriate high dose salicylate therapy. Two and 5 weeks later, the mean observed maximum rates of SU formation were re-determined along with the average steady-state serum salicylate concentrations. Mean observed maximum SU excretion rates increased significantly between the single-dose study (0.96 +/- 0.22 mg/kg/h) and the last dose of the high dose therapy at 2 weeks (1.65 +/- 0.30 mg/kg/h; p less than 0.01); however, there was no further increase at week 5. Similar increases in the theoretical maximum rate of SU formation (Vmax) were observed between the single-dose study and after 2 weeks of high dose salicylate therapy. Average steady-state serum salicylate concentrations showed no decline between weeks 2 and 5. High dose salicylate therapy leads to acceleration of the rate of SU formation in patients with rheumatoid arthritis and this occurs largely during the first 2 weeks of therapy.
对4名类风湿性关节炎患者测定了平均稳态血清水杨酸浓度和水杨尿酸(SU)生成率。在水杨酸洗脱期(1个月)后,通过在单次口服水杨酸(35mg/kg)后收集频繁的尿液样本,确定了SU的平均观察到的最大生成率。然后患者开始接受适当的高剂量水杨酸治疗。2周和5周后,重新测定了SU生成的平均观察到的最大速率以及平均稳态血清水杨酸浓度。在单剂量研究(0.96±0.22mg/kg/h)和高剂量治疗2周时的最后一剂之间,平均观察到的最大SU排泄率显著增加(1.65±0.30mg/kg/h;p<0.01);然而,在第5周时没有进一步增加。在单剂量研究和高剂量水杨酸治疗2周后,观察到SU生成的理论最大速率(Vmax)有类似的增加。平均稳态血清水杨酸浓度在第2周和第5周之间没有下降。高剂量水杨酸治疗导致类风湿性关节炎患者SU生成速率加快,这主要发生在治疗的前2周。