Temperature and eluent composition effects on enantiomer separation of carvedilol by high-performance liquid chromatography on immobilized amylose-based chiral stationary phases  

作　　者：Cristina Panella Rosella Ferretti Adriano Casulli Roberto Cirilli 

机构地区：[1]Centro Nazionale peril Controllo e la Valutazione dei Farmaci, Istituto Superiore di Sanita, Viale Regina Elena 299, 00161 Rome, Italy [2]European Union Reference Laboratory for the Parasites, Istituto Superiore di Sanita, Viale Regina Elena 299, 00161 Rome, Italy [3]World Health Organization Collaborating Centre for the Epidemiology, Detection and Control of Cystic and Alveolar Echinococcosis (in Animals and Humans), Istituto Superiore di Sanita, Viale Regina Elena 299, 00161 Rome, Italy

出　　处：《Journal of Pharmaceutical Analysis》2019年第5期324-331,共8页药物分析学报（英文版）

摘　　要：Carvedilol is a chiral drug with potent antihypertensive and antianginal activities. Although it is clinically used as a racemic mixture, its enantiomers show different pharmacokinetic and pharmacodynamic profiles. Here, the direct chiral separation of racemic drug by high performance liquid chromatography using two immobilized-type amylose-based chiral stationary phases is presented. Some chromatographic parameters, such as retention and selectivity, were determined under multimodal eluent conditions and different temperatures. A temperature-dependent inversion of the elution order of enantiomers was observed in the operative temperature range of chiral chromatographic support. Finally, an effective direct enantioselective method was successfully applied to the separation of the enantiomers of carvedilol on a semipreparative scale.Carvedilol is a chiral drug with potent antihypertensive and antianginal activities.Although it is clinically used as a racemic mixture,its enantiomers show different pharmacokinetic and pharmacodynamic profiles.Here,the direct chiral separation of racemic drug by high performance liquid chromatography using two immobilized-type amylose-based chiral stationary phases is presented.Some chromatographic parameters,such as retention and selectivity,were determined under multimodal eluent conditions and different temperatures.A temperature-dependent inversion of the elution order of enantiomers was observed in the operative temperature range of chiral chromatographic support.Finally,an effective direct enantioselective method was successfully applied to the separation of the enantiomers of carvedilol on a semipreparative scale.

关 键 词：Chiralpak^(■) IG-3 Enantioselective HPLC CARVEDILOL Column temperature Isoenantioselective temperature Semipreparative enantioseparation 

分 类 号：R[医药卫生]