Liss E, Robertson A
Arzneimittelforschung. 1975 Nov;25(11):1792-3.
Following oral administration of 4-acetamido-phenyl-2-acetoxybenzoate (carboxyl-14C) (benorylate) to rats, no gross differences were detected 7.5 h after administration with respect to the distribution of 14C in various tissues, including the upper sections of the small intestine. A high concentration of 14C was found in the lower sections of the intestine 4 h after administration. The 14C in the intestine was present as unchanged benorylate, as detected by thin-layer chromatography, suggesting that benorylate absorption was slow. Intravenous injection of 14C-benorylate to rats showed that the drug had a relatively high elimination rate from the blood with a half-life of 1.9 h. In blood benorylate must be rapidly hydrolysed enzymatically since no 14C-metabolites, other than salicylic acid, could be detected.
给大鼠口服4-乙酰氨基苯基-2-乙酰氧基苯甲酸酯(羧基-14C)(贝诺酯)后,给药7.5小时后,在包括小肠上段在内的各种组织中,未检测到14C分布存在明显差异。给药4小时后,在小肠下段发现高浓度的14C。通过薄层色谱法检测发现,肠道中的14C以未变化的贝诺酯形式存在,这表明贝诺酯的吸收缓慢。给大鼠静脉注射14C-贝诺酯表明,该药物从血液中的消除率相对较高,半衰期为1.9小时。在血液中,贝诺酯必须迅速被酶水解,因为除了水杨酸外,未检测到其他14C代谢物。