沈阳药科大学学报

2018, v.35;No.274(11) 943-946

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HPLC手性固定相法分离5种H_1-受体阻断剂药物对映体
Separation of five H_1-receptor blocker enantiomers with chiral HPLC

李泽众;李晨;朱子豪;自汝捷;郭兴杰;姜珍;
LI Zezhong;LI Chen;ZHU Zihao;ZI Rujie;GUO Xingjie;JIANG Zhen;School of Pharmacy,Shenyang Pharmaceutical University;

摘要(Abstract):

目的建立手性固定相HPLC法拆分氯苯那敏、非尼拉敏、多西拉敏、特非那定和非索非那定5种H_1-受体阻断剂药物对映体,并探讨其分离机制。方法使用Chiralpak ID手性色谱柱,在正相系统下进行拆分,考察了酸碱添加剂的种类,有机改性剂种类与浓度对5种药物对映体分离的影响。结果在优化条件下,氯苯那敏、非尼拉敏、多西拉敏、特非那定和非索非那定的对映体分离度分别为2. 51、2. 94、1. 34、5. 53和2. 48。结论除多西拉敏外,其余4种药物对映体均达到了基线分离。
Objective To develop a chiral HPLC method for the enantioseparation of five H_1-receptor antagonists,including chlorpheniramine,pheniramine,doxylamine,terfenadine and fexofenadine,and then to discuss the chiral resolution mechanisms. Methods Using Chiralpak ID column with normal mobile phase,the factors influencing separation process,such as types of acidic or basic addictives,organic modifiers,and the volume ratio of isopropanol in mobile phase were investigated. Results Under the optimized condition,the resolutions of the enantiomers of chlorpheniramine,pheniramine,doxylamine,terfenadine and fexofenadine were 2. 51,2. 94,1. 34,5. 53 and 2. 48,respectively. Conclusion All the analyte enantiomers except doxylamine obtain good baseline separation.

关键词(KeyWords): 高效液相色谱法;Chiralpak ID;对映体分离;H1-受体阻断剂
HPLC;Chiralpak ID;enantioseparation;H1-receptor blocker

Abstract:

Keywords:

基金项目(Foundation): 国家基础科学人才培养基金资助项目(J1103606)

作者(Authors): 李泽众;李晨;朱子豪;自汝捷;郭兴杰;姜珍;
LI Zezhong;LI Chen;ZHU Zihao;ZI Rujie;GUO Xingjie;JIANG Zhen;School of Pharmacy,Shenyang Pharmaceutical University;

DOI: 10.14066/j.cnki.cn21-1349/r.2018.11.006

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