Nakamura J, Shiota H, Sasaki H, Shibasaki J
Faculty of Pharmaceutical Sciences, Nagasaki University, Japan.
J Pharmacobiodyn. 1988 Sep;11(9):625-9. doi: 10.1248/bpb1978.11.625.
The blood concentrations of salicyluric acid and salicylic acid following oral, intravenous, intracecal and rectal administration of salicyluric acid were determined in rats. After oral administration of salicyluric acid, salicyluric acid was rapidly absorbed. Salicylic acid was detected at low concentration. Following intravenous administration of salicyluric acid, salicyluric acid was detected in the blood and was rapidly eliminated. A trace amount of salicylic acid was detected, suggesting that systemic deconjugation of glycine was involved. Furthermore, in vitro incubation of salicyluric acid with contents of the gut showed that the major source of the hydrolysis was the hind gut. Immediate and very extensive salicylic acid formation in the cecum was found following intracecal administration of salicyluric acid. The blood concentration of salicylic acid was maintained at 2.6-4.0 micrograms/ml from 4 to 12 h following rectal administration of salicyluric acid (10 mg/kg: salicylic acid equivalent). Species difference in the metabolic fate of salicyluric acid in rats and rabbits reported previously is discussed.
测定了大鼠口服、静脉注射、盲肠内和直肠给予水杨尿酸后水杨尿酸和水杨酸的血药浓度。口服水杨尿酸后，水杨尿酸迅速吸收。检测到低浓度的水杨酸。静脉注射水杨尿酸后，在血液中检测到水杨尿酸并迅速消除。检测到微量水杨酸，提示涉及甘氨酸的全身去结合作用。此外，水杨尿酸与肠道内容物的体外孵育表明，水解的主要来源是后肠。盲肠内给予水杨尿酸后，在盲肠中立即发现非常大量的水杨酸形成。直肠给予水杨尿酸（10mg/kg：水杨酸当量）后4至12小时，水杨酸血药浓度维持在2.6 - 4.0微克/毫升。讨论了先前报道的大鼠和兔子中水杨尿酸代谢命运的种属差异。
