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治疗剂量摄入后人体尿液中甲非酰胺及其主要降解产物去甲基甲非酰胺的定量测定(作者译)

[Quantitative determination of mefexamide and its main degradation product desmethyl-mefexamide in human urine after ingestion of therapeutic doses (author's transl)].

作者信息

Gielsdorf W, Herper M

出版信息

Z Rechtsmed. 1981;87(4):297-303. doi: 10.1007/BF00200645.

Abstract

After oral ingestion of 400 mg Mefexamidehydrochloride for Mefexamide (I) and its main degradation product Desmethyl-Mefexamide (II) the following pharmakokinetic parameters have been determined: 1. Elimination of I and II follows 1st order kinetics. 2. Biological half-life t 1/2 for I is 4-6, for II 4.5-6.5 H. 3. Elimination rate constant for I and II is between 0.10 to 0.20 h-1. 4. 5-10% of the administered drug are excreted unchanged, 10-16% as Desmethyl-Mefexamide within 72 h after ingestion. 5. The described thinlayer chromatographic and gas chromatographic/mass spectrometric methods allow detection of I and II for at least 72 h after application. 6. II is excreted free and conjugated in nearly equal amounts.

摘要

口服400毫克盐酸美非沙胺(用于美非沙胺(I)及其主要降解产物去甲基美非沙胺(II))后,已测定以下药代动力学参数:1. I和II的消除遵循一级动力学。2. I的生物半衰期t 1/2为4 - 6小时,II为4.5 - 6.5小时。3. I和II的消除速率常数在0.10至0.20 h-1之间。4. 给药药物的5 - 10%以原形排泄,10 - 16%在摄入后72小时内以去甲基美非沙胺形式排泄。5. 所述的薄层色谱和气相色谱/质谱方法可在应用后至少72小时检测到I和II。6. II以游离和结合形式排泄的量几乎相等。

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