手性固定相法和手性衍生化法拆分β-受体阻断剂类药物及其结构类似物  

Enatiomeric separation of β-blocking agents and analogs

作　　者：余露山[1] 姚彤炜[1] 王向军[1] 曾苏[1] 

机构地区：[1]浙江大学药学院,浙江杭州310031

出　　处：《浙江大学学报（医学版）》2002年第6期414-418,428,共6页Journal of Zhejiang University(Medical Sciences)

基　　金：国家自然科学基金 (C39770 868);浙江省青年科技人才培养专项基金资助项目 (RC970 1 6)

摘　　要：目的 :建立一些 β-受体阻断剂类药物及其结构类似物的手性高效液相色谱拆分方法。方法 :利用 Chiral-cel OD和 Chiralpak AD两种手性固定相及 GITC手性衍生化试剂 ,对 11种药物进行手性拆分研究。结果 :普萘洛尔、阿替洛尔、比索洛尔、美托洛尔、塞利洛尔、卡维地洛、索他洛尔、普罗帕酮、麻黄碱和佐米曲普坦都在一种或几种色谱条件下得到了较好的分离。柱温对 Chiralcel OD的拆分因子影响较大 ,相同条件下柱温越低 ,药物拆分因子越大。结论 :用 OD和 AD两种手性固定相和 GITC手性衍生化法拆分 β-受体阻断剂等Objective: To evaluate enantiomeric separation methods for β blocking agents and analogs. Me thods : Enantiomeric separation of racemates of 11β blocking agents and their analogs was performed using chiral stationary phases and 2,3,4,6 tetra O acetyl β D glucopyranosyl isothiocyanate (GITC). Results: These β blocker racemates were separated into enantiomers in one or several chormatographic states such as propranolol, bisoprolol, metoprolol, celiprolol, carvedilol, sotalol, propafenone, ephedrine, and zomitriptan. Temperature had a significant effect on the resolution of the drugs when using chiralcel OD. Lower temperatures were associated with higher resolutions. Conclusion: When separating β blocking agents and their analogs, Chiralcel OD, Chiralpak AD, Chiral stationary phases and GITC chiral derivative reagents have complementary functions.

关 键 词：立体异构现象 高压液相色谱法 肾上腺素能β-受体拮抗剂 手性固定相 手性衍生化 GITC 

分 类 号：O658[理学—分析化学]