烟苄丙酮香豆素的立体特异性测定：在人体药代动力学研究中的应用。
Stereospecific assay of nicoumalone: application to pharmacokinetic studies in man.
作者信息
Gill T S, Hopkins K J, Rowland M
机构信息
Department of Pharmacy, Medeval Ltd, University of Manchester, UK.
出版信息
Br J Clin Pharmacol. 1988 May;25(5):591-8. doi: 10.1111/j.1365-2125.1988.tb03350.x.
Abstract
- A stereospecific h.p.l.c. assay of nicoumalone in plasma has been developed. 2. The assay was applied to a study in which 20 mg racemic nicoumalone was given orally to three volunteers and blood samples taken for 168 h. 3. The mean pharmacokinetic parameters of the individual enantiomers were: clearance/bioavailability 1.28 1 h-1, R-enantiomer; 17.5 1 h-1, S-enantiomer: volume of distribution/bioavailability 12.5 1, R-enantiomer; 22.6 1, S-enantiomer: terminal half-life 6.8 h, R-enantiomer; 0.91 h, S-enantiomer. 4. The data are consistent with a substantial first-pass hepatic loss of S-nicoumalone.
摘要
- 已开发出一种血浆中尼可马隆的立体特异性高效液相色谱分析方法。2. 该分析方法应用于一项研究，给三名志愿者口服20毫克外消旋尼可马隆，并采集168小时的血样。3. 各对映体的平均药代动力学参数为：清除率/生物利用度1.28升/小时，R-对映体；17.5升/小时，S-对映体：分布容积/生物利用度12.5升，R-对映体；22.6升，S-对映体：末端半衰期6.8小时，R-对映体；0.91小时，S-对映体。4. 数据表明S-尼可马隆存在显著的首过肝损失。
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