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阿司匹林对小鼠亚中毒剂量14C - 对乙酰氨基酚的影响。

Effect of aspirin on a subtoxic dose of 14C-acetaminophen in mice.

作者信息

Whitehouse L W, Paul C J, Wong L T, Thomas B H

出版信息

J Pharm Sci. 1977 Oct;66(10):1399-403. doi: 10.1002/jps.2600661012.

Abstract

The interaction of 14C-acetaminophen, 150 mg/kg (20 muCi/kg), and aspirin, 200 mg/kg po, was studied in male mice. The radiolabel was rapidly absorbed from the GI tract, achieving maximum blood levels 0.25 hr after oral dosing. Radioactivity in the blood equilibrated rapidly with the tissues and was concentrated in the liver and kidney. At 14 hr, most of the dose was eliminated in urine as the glucuronide, cysteine, sulfate, free drug, and mercapturate. Pretreatment with aspirin tended to reduce the rate and extent of acetaminophen absorption and altered the percentage of the dose excreted in the urine as sulfate, mercapturate, glucuronide, and cysteine. Interpretation of these data toxicologically as an indication of the potentiation of either toxicity or protection was not possible.

摘要

研究了150毫克/千克(20微居里/千克)的14C - 对乙酰氨基酚与200毫克/千克口服阿司匹林在雄性小鼠体内的相互作用。放射性标记物从胃肠道迅速吸收,口服给药后0.25小时达到最高血药浓度。血液中的放射性与组织迅速达到平衡,并在肝脏和肾脏中富集。14小时时,大部分剂量以葡萄糖醛酸苷、半胱氨酸、硫酸盐、游离药物和硫醚氨酸的形式经尿液排出。阿司匹林预处理倾向于降低对乙酰氨基酚的吸收速率和程度,并改变以硫酸盐、硫醚氨酸、葡萄糖醛酸苷和半胱氨酸形式经尿液排泄的剂量百分比。从毒理学角度解释这些数据以表明毒性增强或保护作用是不可能的。

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