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采用高效液相色谱法测定血浆中布呋洛尔及其主要代谢产物。

Determination of bufuralol and its major metabolites in plasma by high-performance liquid chromatography.

作者信息

Haefelfinger P

出版信息

J Chromatogr. 1980 Dec 12;221(2):327-35. doi: 10.1016/s0378-4347(00)84318-2.

DOI:10.1016/s0378-4347(00)84318-2
PMID:7217302
Abstract

A high-performance liquid chromatographic method for the determination of bufuralol, a benzofuran analogue, in plasma is described. The unchanged drug, the major metabolites and an internal standard are extracted from plasma, purified by back-extraction steps and thereafter separated using a reversed-phase liquid chromatographic system. The detection is carried out by means of a fluorescence detector and an UV detector connected in series. The sensitivity of the assay for the unchanged drug and the major metabolite is about 1 ng/ml plasma using a 0.5 ml specimen per analysis and the relative standard deviation of the whole assay lies in the range +/- 4-5%. The procedure was successfully used to determine plasma levels in volunteers following a single oral dose of 40 mg of bufuralol. The results obtained using the new high-performance liquid chromatographic method were compared with those determined by another method which combines gas chromatography with mass fragmentography, and it was found that these two sets of results coincided quite well.

摘要

本文描述了一种用于测定血浆中苯并呋喃类似物布呋洛尔的高效液相色谱法。将未变化的药物、主要代谢物及内标从血浆中提取出来,经反萃取步骤纯化,然后使用反相液相色谱系统进行分离。检测通过串联的荧光检测器和紫外检测器进行。使用每份分析0.5 ml样本时,该方法对未变化药物和主要代谢物的检测灵敏度约为1 ng/ml血浆,整个分析的相对标准偏差在±4 - 5%范围内。该方法成功用于测定志愿者单次口服40 mg布呋洛尔后的血浆浓度。将使用新的高效液相色谱法获得的结果与通过气相色谱 - 质谱碎片分析法相结合的另一种方法所测定的结果进行比较,发现这两组结果相当吻合。

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引用本文的文献

1
Contribution of the genetic status of oxidative metabolism to variability in the plasma concentrations of beta-adrenoceptor blocking agents.
Eur J Clin Pharmacol. 1983;24(6):797-9. doi: 10.1007/BF00607090.
2
Relationship between pharmacokinetic and pharmacodynamic behaviour of bufuralol and its metabolite Ro 3-7410 in hypertensive patients.布呋洛尔及其代谢产物Ro 3-7410在高血压患者体内的药代动力学与药效学行为之间的关系。
Eur J Clin Pharmacol. 1983;24(4):479-84. doi: 10.1007/BF00609890.
3
Defective hydroxylation of bufuralol associated with side-effects of the drug in poor metabolisers.布呋洛尔羟化缺陷与药物在代谢缓慢者中的副作用相关。
Br J Clin Pharmacol. 1982 May;13(5):750-2. doi: 10.1111/j.1365-2125.1982.tb01453.x.
4
The genetic control of bufuralol metabolism in man.
Eur J Drug Metab Pharmacokinet. 1982 Jan-Mar;7(1):73-7. doi: 10.1007/BF03189547.
5
Effect of oxidative polymorphism (debrisoquine/sparteine type) on hepatic first-pass metabolism of bufuralol.氧化多态性(异喹胍/鹰爪豆碱型)对布呋洛尔肝首过代谢的影响。
Eur J Clin Pharmacol. 1985;28(3):317-20. doi: 10.1007/BF00543330.