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采用毛细管气相色谱法对夸西泮及其2-氧代和N-去甲基代谢物进行血浆定量分析。

Plasma quantification of quazepam and its 2-oxo and N-desmethyl metabolites by capillary gas chromatography.

作者信息

Bun H, Coassolo P, Ba B, Aubert C, Cano J P

出版信息

J Chromatogr. 1986 May 28;378(1):137-45. doi: 10.1016/s0378-4347(00)80706-9.

DOI:10.1016/s0378-4347(00)80706-9
PMID:3733966
Abstract

The authors have developed a gas chromatographic method for the simultaneous quantification of quazepam in plasma and its two main metabolites, 2-oxoquazepam and N-desmethylquazepam. This method involves an extraction from plasma using butyl acetate, and an analysis by electron-capture detection on a CP-Sil 5 WSCOT capillary column. Intra- and inter-day precision and accuracy were better than 10% for each of these three compounds, even near their detection limit estimated at 0.2 ng/ml. Linearity proved satisfactory between 0.2 and 60-70 ng/ml. For endogenous plasma components, adequate specificity was achieved. Despite some inconveniences, a long analysis time, a progressive saturation of the column owing to a low oven temperature, and a relatively short life-span of the CP-Sil 5 columns, this method was the only one available in the literature for the quantification of quazepam and its metabolites from the same plasma sample. It was successfully applied to phase I studies in healthy volunteers.

摘要

作者开发了一种气相色谱法,用于同时定量血浆中夸西泮及其两种主要代谢物2-氧代夸西泮和N-去甲基夸西泮。该方法包括用乙酸丁酯从血浆中萃取,并在CP-Sil 5 WSCOT毛细管柱上通过电子捕获检测进行分析。这三种化合物各自的日内和日间精密度及准确度均优于10%,即使在估计为0.2 ng/ml的检测限附近也是如此。在0.2至60 - 70 ng/ml之间线性证明令人满意。对于内源性血浆成分,实现了足够的特异性。尽管存在一些不便之处,如分析时间长、由于柱温低导致柱逐渐饱和以及CP-Sil 5柱的使用寿命相对较短,但该方法是文献中唯一可用于从同一血浆样品中定量夸西泮及其代谢物的方法。它已成功应用于健康志愿者的I期研究。

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Plasma quantification of quazepam and its 2-oxo and N-desmethyl metabolites by capillary gas chromatography.采用毛细管气相色谱法对夸西泮及其2-氧代和N-去甲基代谢物进行血浆定量分析。
J Chromatogr. 1986 May 28;378(1):137-45. doi: 10.1016/s0378-4347(00)80706-9.
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引用本文的文献

1
Liquid chromatographic assay and pharmacokinetics of quazepam and its metabolites following sublingual administration of quazepam.夸西泮舌下给药后夸西泮及其代谢产物的液相色谱分析及药代动力学
Pharm Res. 1988 Jun;5(6):365-8. doi: 10.1023/a:1015907611170.
2
Quazepam. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in insomnia.夸西泮。对其药效学和药代动力学特性以及在失眠治疗中的疗效的初步综述。
Drugs. 1988 Jan;35(1):42-62. doi: 10.2165/00003495-198835010-00003.