Nakamura J, Shiota H, Haraguchi Y, Sasaki H, Shibasaki J
Faculty of Pharmaceutical Sciences, Nagasaki University, Japan.
J Pharmacobiodyn. 1988 Jan;11(1):53-7. doi: 10.1248/bpb1978.11.53.
The blood concentrations of salicyluric acid and salicylic acid following intracecal and rectal administration of salicyluric acid were determined in rabbits. Immediate and very extensive salicylic acid formation in the cecum was found following intracecal administration. After rectal administration, a small amount of salicyluric acid was absorbed in intact form. The rest was rapidly hydrolyzed to salicylic acid, which was subsequently absorbed. The blood concentration of salicylic acid was maintained at 1.3-1.8 micrograms/ml from 2 to 12 h. Three doses of salicyluric acid were administered rectally. The peak level of salicyluric acid increased with dose. However, salicylic acid concentration in the blood following administration of salicyluric acid at 10.0 mg/kg (salicylic acid equivalent) was not double that observed following administration of salicyluric acid at 5.0 mg/kg (salicylic acid equivalent). It appears that a larger amount of salicyluric acid in the rectal lumen may have saturated the glycine deconjugation system.
测定了兔经盲肠内和直肠给予水杨尿酸后血液中水杨尿酸和水杨酸的浓度。盲肠内给药后，在盲肠中发现立即且大量地形成了水杨酸。直肠给药后，少量水杨尿酸以完整形式被吸收。其余部分迅速水解为水杨酸，随后被吸收。水杨酸的血药浓度在2至12小时内维持在1.3 - 1.8微克/毫升。经直肠给予了三剂水杨尿酸。水杨尿酸的峰值水平随剂量增加而升高。然而，给予10.0毫克/千克（水杨酸当量）水杨尿酸后血液中的水杨酸浓度并非给予5.0毫克/千克（水杨酸当量）水杨尿酸后观察到浓度的两倍。似乎直肠腔内大量的水杨尿酸可能使甘氨酸去结合系统饱和了。
