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高效液相色谱法测定人血浆中卡托普利和人体药动学的研究

杨丽*, 许爱霞, 赵荣生, 严宝霞   

  1. 北京大学第三医院药剂科, 北京 100083
  • 收稿日期:2002-01-26 修回日期:2003-02-10 出版日期:2003-03-15 发布日期:2003-03-15
  • 通讯作者: 杨丽*

Determination of Captopril in Human Plasma by High-Performance Liquid Chromatography and Study on the Pharmacokinetics after a Single Oral Dose

YANG Li*, XU Ai-xia, ZHAO Rong-sheng, YAN Bao-xia   

  1. Department of Pharmacy, Peking University Third Hospital, Beijing 100083, China
  • Received:2002-01-26 Revised:2003-02-10 Online:2003-03-15 Published:2003-03-15
  • Contact: YANG Li*

摘要: 目的 建立简便的测定人血浆中卡托普利血药浓度的高效液相色谱法, 研究卡托普利在健康人体中的药动学参数. 方法 以对溴苯乙酰基溴为紫外衍生化试剂, 采用高效液相色谱紫外检测法测定18名健康志愿受试者口服单剂量卡托普利受试制剂和参比制剂(50 mg)后血药浓度.结果卡托普利的血药浓度标准曲线的线性范围为25~1200ng·mL-1, 其最低定量限为25 ng·mL-1, 日内及日间BSD均小于8%.应用所建立的血药浓度检测方法测定18名健康志愿受试者口服单剂量卡托普利受试制剂和参比制剂(50 mg)后血药浓度, 并计算药动学参数. 结果 表明口服受试制剂或参比制剂后的tmax分别为(0.64±0.18)h(0.82±0.41)h; Cmax分别为(600.2±194.3)ng·mL-1(582.7±175.3)ng·mL-1; AUC0→8h分别为(1448.5±483.7)ng·h·mL-1(1389.9±392.5)ng·h·mL-1; AUC0→∞分别为(1869.4±701.6)ng·h·mL-1(1781.8±615.5)ng·h·mL-1. 结论 本方法操作便捷, 灵敏度高, 为血药浓度监测及药代动力学研究提供了方法学基础.

关键词: 卡托普利, 药代动力学, 高效液相色谱法, 紫外检测法

Abstract: Aim To establish a simple high-performance liquid chromatography method for the determination of captopril in human plasma and study the pharmacokinetics of captopril in healthy volunteers. Methods Captopril was stabilizedby forming an adduct with p-bromophenacyl bromide and this adduct in plasma was measured by high-performance liquidchromatography with UV detection following a single oral dose 50 mg of captopril test and reference preparations respectivelygiven to 18 healthy volunteers. Results The standard curve was liner over a range of 25-1200 ng·mL-1. The quantitativelimit of detection was 25 ng·mL-1. The RSD of inter- and intra- assay were below 8%. On the basis of elaborated method,single-dose pharmacokinetics in 18 healthy volunteers have been investigated. The comparison of the pharmacokinetic parameters was performed. The pharmacokinetic parameters of test and reference tablets were calculated as follows: tmax were(0.64± 0.18)h and (0.82±0.41)h; Cmax were(600.2+194.3)ng·mL-1 and (582.7+175.3)ng·mL-1; AUC0→8h were (1448.5+483.7)ng·h·mL-1 and (1389.9±392.5)ng·h·mL-1; AUC0→∞ were (1869.4+701.6)ng·h·mL-1 and (1781.8 +615.5)ng·h·mL-1, respectively. Conclusion The improved analytical method for captopril was found to be sensitive,simple and rapid, suitable for application in pharmacokinetic studies and routine determination of numerous samples.

Key words: captopril, captopril, pharmacokinetics, pharmacokinetics, high performance liquid chromatography, high performance liquid chromatography, UV detection, UV detection

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Supporting: *Corresponding author. Tel.: 86-010-62017961-2740