Daneels R, Loew D, Pütter J
Arzneimittelforschung. 1975 Jul;25(7):1073-7.
Quantitative Determination of the Main Metabolites of Acetylsalicylic Acid / 2nd Communication: The concentrations of salicylic acid and its metabolies in patients with renal insufficiency 9 patients suffering from renal insufficiencies of varing degrees and treated regularly by hemodialysis were given 1.5 g Colfarit (microcapsulated acetyl salicylic acid) as a single dose. The concentrations of salicylic acid (SA), salicyluric acid (SU), further salicylic acid conjugates (SAC) and salicyluric acid conjugates (SUC) were determined in the blood plasma. Likewise urea and creatinine were determined. SA concentration decreased continually and, at the end of the trial (72 h after application), had vanished almost completely from the plasma of most patients. SU increased at first and decreased afterwards. With the exception of the dailysis time SAC and SUC increased during the trial. After 3 days the SUC level was more than 50% of total salicylate (SSS) in most patients. SSS (the sum of SA + SU + SAC + SUC) did not change very much before dialysis, but showed a rather high decrease during the first hours of dialysis. tafter dialysis the SSS levels rose again, apparently as a consequence of a redistribution and of the synthesis of conjugates with decreased tissue affinity. It could be shown that SSS in the blood plasma does not parallel SSS in the whole body. The interindividual variation of SA metabolism as well as the variation of the biological blank values was rather high. The results are discussed with regard to salicylate pharmacokinetics in renal insufficiency and to normal salicylate metabolism.
乙酰水杨酸主要代谢产物的定量测定/第二篇通讯:肾功能不全患者体内水杨酸及其代谢产物的浓度 9名不同程度肾功能不全且定期接受血液透析治疗的患者单次服用1.5g可力菲(微囊化乙酰水杨酸)。测定血浆中水杨酸(SA)、水杨尿酸(SU)、其他水杨酸结合物(SAC)和水杨尿酸结合物(SUC)的浓度。同样也测定了尿素和肌酐。SA浓度持续下降,在试验结束时(用药后72小时),大多数患者血浆中SA几乎完全消失。SU起初升高,之后下降。除透析时间外,试验期间SAC和SUC升高。3天后,大多数患者的SUC水平超过总水杨酸酯(SSS)的50%。透析前SSS(SA+SU+SAC+SUC之和)变化不大,但在透析的最初几个小时内显著下降。透析后SSS水平再次升高,显然是由于重新分布以及与组织亲和力降低的结合物合成所致。可以看出,血浆中的SSS与全身的SSS并不平行。SA代谢的个体间差异以及生物空白值的差异相当大。结合肾功能不全时水杨酸酯的药代动力学以及正常水杨酸酯代谢对结果进行了讨论。