高效液相色谱法测定大鼠血浆、尿和肝匀浆中的2',3'-二脱氢-2',3'-二脱氧核糖-2-氨基-6-环丙胺基嘌呤核苷

高效液相色谱法测定大鼠血浆、尿和肝匀浆中的2',3'-二脱氢-2',3'-二脱氧核糖-2-氨基-6-环丙胺基嘌呤核苷

刘薏, 杨振军^*, Boudinot F Douglas, CHU Chang kuang, 张礼和

1.北京信诺康达医药信息技术有限公司, 北京, 100083;
2.北京大学药学院, 北京, 100083;
3.College of Pharmacy, The University of Georgia，Athens, Georgia 30602-2352, USA

收稿日期:2003-02-03 修回日期:2003-05-10 出版日期:2003-06-15 发布日期:2003-06-15
通讯作者: 杨振军*

Determination of 2-Amino-6-Cyclopropylamino-9-(2,3-Dideoxy-β-D-glyceropent-2-enofuranosyl)purine in Rat Plasma, Urine and Liver Homogenates by High Performance Liquid Chromatography

LIU Yi, YANG Zhen-jun^*, Boudinot F Douglas, CHU Chang kuang, ZHANG Li-he

1.School of Pharmaceutical Sciences, Peking University, Beijing 100083, China;
2.Beijing Sinopm Medical Information Co. Ltd.,Beijing 100083, China;
3.College of Pharmacy, The University of Georgia, Athens, Georgia 30602-2352, USA

Received:2003-02-03 Revised:2003-05-10 Online:2003-06-15 Published:2003-06-15
Contact: YANG Zhen-jun*

摘要/Abstract

摘要： 目的建立高效液相法测定大鼠血浆、尿和肝匀浆中2', 3'-二脱氢-2', 3'-二脱氧核糖-2-氨基-6-环丙胺嘌呤核苷(Cyclo-D4G, D4G前药)的简单而特异、适合于研究其体内药物代谢动力学的方法. 方法采用高效液相色谱法, C-18 Hypersil ODS柱, 流动相为7%(v/v)乙腈的磷酸盐缓冲液 (pH7.40), 紫外检测波长为283 nm. 结果该方法的线性范围为0.5-80 μg·mL^-1, 提取平均回收率100.1%, 精确度为99.4%, 日内和日间差均小于9.0%. 结论 Cyclo-D4G在大鼠血浆中稳定, 在肝匀浆中4小时后即有明显的分解.

关键词: 药物分析, 高效液相色谱分析, D4G前药, 稳定性

Abstract: Aim To develop a simple and specific high-performance liquid chromatographic (HPLC) method, suitable for the pharmacokinetic studies in Vivo, to determine the concentrations of 2-amino-6-cyclopropylamino-9-(2,3-dideoxy-β-D-glyceropent-2-enofuranosyl) purine (Cyclo-D4G, D4G prodrug) in rat plasma, urine and liver homogenates. Methods Chromatography was performed with C-18 Hypersil ODS column and a mobile phase of 7% (v/v) acetonitrile in phosphate buffer, pH7.40, with UV detection at 283 nm. Results The average extraction recovery of Cyclo-D4G in rat plasma and urine was 100.1% over its linear range of 0.5-80 μg·mL^-1. The accuracy of the assay was 99.4%. The intra-and interday RSDs were less than 9.0%. Conclusion The analytical method was found to be applicable, reliable and suitable for pharmacokinetic studies.

Key words: Pharmaceutical analysis, Pharmaceutical analysis, HPLC analysis, HPLC analysis, D4G prodrug, D4G prodrug, Stability, Stability

中图分类号:

R917

Supporting: ^*Corresponding author. Tel.: 010-62091570; fax: 010-62092724

刘薏, 杨振军^*, Boudinot F Douglas, CHU Chang kuang, 张礼和. 高效液相色谱法测定大鼠血浆、尿和肝匀浆中的2',3'-二脱氢-2',3'-二脱氧核糖-2-氨基-6-环丙胺基嘌呤核苷[J]. .

LIU Yi, YANG Zhen-jun^*, Boudinot F Douglas, CHU Chang kuang, ZHANG Li-he . Determination of 2-Amino-6-Cyclopropylamino-9-(2,3-Dideoxy-β-D-glyceropent-2-enofuranosyl)purine in Rat Plasma, Urine and Liver Homogenates by High Performance Liquid Chromatography[J]. .

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