新型环糊精衍生物对手性药物的立体选择性研究  

Three Enantiomers Separation with Mono -6 - O - phenylcarbamoyl - β - CD and a Study on the Binding of Cyclodextrins with These Enantiomers

作　　者：林秀丽[1] 主沉浮[2] 魏云鹤[2] 李剑[2] 王明峰[2] 

机构地区：[1]山东大学药学院,济南250012 [2]山东大学化学与化学工程学院,济南250061

出　　处：《药物分析杂志》2004年第5期489-493,共5页Chinese Journal of Pharmaceutical Analysis

摘　　要：目的:用实验证明新型环糊精衍生物单-6-O-苯基氨甲酰基-B-CD(单-6-O-P-B-CD)对普萘洛尔、妥洛特罗以及氯丙那林3种手性药物的手性识别作用要强于β-CD。方法:用一定浓度的单-6-O-P-β-CD和β-CD为手性选择剂,以60 mmol·L-1硼砂(pH 9.25)为运行缓冲液,在分离电压为9.0 kV,检测波长为214nm的条件下,考察了单6-O—P—β—CD和β-CD对3种手性药物对映体的毛细管电泳分离;并用毛细管区带电泳法分别求解了单-6-O—P—β—CD与β—CD和所研究的手性药物形成的配合物的稳定常数。结果:单-6-O—P—β—CD能使所研究的3种手性药物达基线分离,β—CD仅能使上述药物中的普萘洛尔达部分分离(R=0.67)。结论:理论计算和实验结果均表明单-6-O-P—β—CD对所研究的手性药物的手性识别作用要强于β—CD。Objective: To demonstrate that the chiral separating ability of mono - 6 - O - phenylcarbamoyl - β - CD for propranolol, tulobuterol and clorprenaline is stronger than β - CD. Method; Certain concentration of mono - 6 -O - phenylcarbamoyl - β - CD and β - CD were used as chiral selector. Borate( pH 9. 25 ) was used as running buffer. Under the conditions of voltage being 9. 0 kV, detection wavelength 214 nm,the separating of the three chiral drugs was carried out. The equilibrium constants of host - guest complexation of propranolol, tulobuterol and clorprenaline enantiomers with β - CD and mono - 6 - O - phenylcarbamoyl - ? - CD were calculated using electropho-resis method. Results:The three chiral drugs (propranolol, tulobuterol and clorprenaline) were baseline separated by mono -6 - O - phenylcarbamoyl - β - CD. Only one chiral drug( Propranolol) was partial separated by β - CD. Conclusion: We have demonstrated from theory that the chiral separating ability of mono - 6 - O- phenylcarbamoyl - β - CD is stronger than β - CD for the three chiral drugs.

关 键 词：手性药物 普萘洛尔 环糊精衍生物 毛细管区带电泳法 分离 研究 作用 新型 并用 苯基 

分 类 号：R914[医药卫生—药物化学] R917[医药卫生—药学]