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核心技术专利：CN118964589B侵权必究

核心技术专利：CN118964589B侵权必究

Zhang A Q, Mitchell S C, Barrett T, Ayesh R, Smith R L

Department of Pharmacology and Toxicology, St Mary's Hospital Medical School, Imperial College of Science, Technology and Medicine, London, UK.

Xenobiotica. 1994 Apr;24(4):379-87. doi: 10.3109/00498259409045901.

The fate of [14C]-dimethylamine was investigated following oral administration to four male volunteers. 2. The major route of excretion was urine, with 94% of the administered radioactivity being voided over 3 days (87% during the first 24 h). Small amounts (1-3%) of radioactivity were found in the faeces and expired air. 3. Metabolism was limited with only 5% being demethylated to methylamine. The remainder of the dose was excreted unchanged. 4. Pharmacokinetic studies indicated rapid (t1/2ab = 8 min) and extensive absorption (bioavailability = 82%) from the gastrointestinal tract followed by widespread distribution and a fairly prompt excretion (t1/2el = 6-7 h) with a plasma clearance of 190 ml/min.

对四名男性志愿者口服给予[14C]-二甲胺后，研究了其代谢情况。2. 排泄的主要途径是尿液，给药放射性的94%在3天内排出（头24小时内排出87%）。在粪便和呼出气体中发现少量（1 - 3%）放射性。3. 代谢有限，仅有5%被脱甲基生成甲胺。其余剂量以原形排出。4. 药代动力学研究表明，胃肠道吸收迅速（吸收半衰期t1/2ab = 8分钟）且广泛（生物利用度 = 82%），随后广泛分布，并相当迅速地排泄（消除半衰期t1/2el = 6 - 7小时），血浆清除率为190毫升/分钟。

Zhang A Q, Mitchell S C, Barrett T, Ayesh R, Smith R L

Department of Pharmacology and Toxicology, St Mary's Hospital Medical School, Imperial College of Science, Technology and Medicine, London, UK.

Xenobiotica. 1994 Apr;24(4):379-87. doi: 10.3109/00498259409045901.

The fate of [14C]-dimethylamine was investigated following oral administration to four male volunteers. 2. The major route of excretion was urine, with 94% of the administered radioactivity being voided over 3 days (87% during the first 24 h). Small amounts (1-3%) of radioactivity were found in the faeces and expired air. 3. Metabolism was limited with only 5% being demethylated to methylamine. The remainder of the dose was excreted unchanged. 4. Pharmacokinetic studies indicated rapid (t1/2ab = 8 min) and extensive absorption (bioavailability = 82%) from the gastrointestinal tract followed by widespread distribution and a fairly prompt excretion (t1/2el = 6-7 h) with a plasma clearance of 190 ml/min.

对四名男性志愿者口服给予[14C]-二甲胺后，研究了其代谢情况。2. 排泄的主要途径是尿液，给药放射性的94%在3天内排出（头24小时内排出87%）。在粪便和呼出气体中发现少量（1 - 3%）放射性。3. 代谢有限，仅有5%被脱甲基生成甲胺。其余剂量以原形排出。4. 药代动力学研究表明，胃肠道吸收迅速（吸收半衰期t1/2ab = 8分钟）且广泛（生物利用度 = 82%），随后广泛分布，并相当迅速地排泄（消除半衰期t1/2el = 6 - 7小时），血浆清除率为190毫升/分钟。