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健康志愿者中[3H]-哌替噻吨的药代动力学与代谢

Pharmacokinetics and metabolism of [3H]-pipethiaden in healthy volunteers.

作者信息

Plecitá Z, Spanĕl M, Ulc I, Rejŏlec V, Lapka R

机构信息

Research Institute for Pharmacy and Biochemistry, Prague, Czechoslovakia.

出版信息

Eur J Drug Metab Pharmacokinet. 1992 Apr-Jun;17(2):89-92. doi: 10.1007/BF03188776.

DOI:10.1007/BF03188776
PMID:1425816
Abstract

Six healthy volunteers participated in a single-dose study of pharmacokinetics and metabolism of oral administration of [3H]-pipethiaden (1 mg). Plasma levels of total radioactivity, urinary excretion and metabolism were analyzed by liquid scintillation counting and radio-TLC. The mean peak plasma concentration of radioactive metabolites was 4.9 ng eq/ml, and the mean elimination half life was 11.5 h. 34% of radioactivity was recovered in 4 days in urine, with only 0.4% present as unchanged drug. Pipethiaden was extensively metabolized by S-oxidation, N-demethylation, and N-oxidation.

摘要

六名健康志愿者参与了口服[3H]-哌替噻吨(1毫克)的单剂量药代动力学和代谢研究。通过液体闪烁计数和放射性薄层色谱法分析了总放射性的血浆水平、尿排泄和代谢情况。放射性代谢物的平均血浆峰浓度为4.9纳克当量/毫升,平均消除半衰期为11.5小时。34%的放射性在4天内从尿液中回收,仅0.4%以未变化的药物形式存在。哌替噻吨通过S-氧化、N-去甲基化和N-氧化进行广泛代谢。

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本文引用的文献

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