Urinary excretion profiles of two major triazolam metabolites, α-hydroxytriazolam and 4-hydroxytriazolam
Urinary excretion profiles of two major triazolam metabolites, α-hydroxytriazolam and 4-hydroxytriazolam
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DOI：
10.1093/jat/29.4.240
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发表时间：
2005-05-01
影响因子：
2.5
通讯作者：
Kishi, T
中科院分区：
文献类型：
--
作者：
Tsujikawa, K;Kuwayama, K;Kishi, T
本研究的目的是检查人体中两种主要三唑仑代谢物 α-羟基三唑仑 (α-OHTRZ) 和 4-羟基三唑仑 (4-OHTRZ) 的尿液排泄情况。尿液样本采集自三名健康男性志愿者，他们在样本采集前 24 小时和 48 小时分别服用过单次 0.25 毫克和 0.5 毫克剂量的三唑仑。经过酶解提取后，对每个样品进行液相色谱-质谱联用分析，α-OHTRZ迅速排泄，最大浓度出现在摄入后收集的第一个或第二个样品中，大部分药物在12小时内排出。同时，4-OHTRZ的排泄速度比α-OHTRZ慢。 α-OHTRZ/4-OHTRZ 比率最初大于 19.7，然后迅速下降，在超过 12 小时内达到几乎恒定的值。
The objective of this study was to examine urinary excretion profiles of two major triazolam metabolites, α-hydroxytriazolam (α-OHTRZ) and 4-hydroxytriazolam (4-OHTRZ) in humans. Urine samples were collected from three healthy male volunteers who had been previously administered single 0.25- and 0.5-mg doses of triazolam 24 h and 48 h, respectively, before sample collection. After enzymatic hydrolysis and extraction, each sample was analyzed by liquid chromatography-mass spectrometry, α-OHTRZ was rapidly excreted, with the maximum concentrations appearing in the first or second sample collected after ingestion, with the majority of the drug being excreted within 12 h. Meanwhile, 4-OHTRZ was excreted more slowly than α-OHTRZ. The α-OHTRZ/4-OHTRZ ratios were initially greater than 19.7, then decreased rapidly, reaching a nearly constant value for times in excess of 12 h.