Castro-Puyana María, Crego Antonio L, Marina M Luisa
Departamento de Química Analítica, Facultad de Química, Universidad de Alcalá, Alcalá de Henares, Madrid, Spain.
Electrophoresis. 2005 Oct;26(20):3960-8. doi: 10.1002/elps.200500100.
EKC using a neutral CD as chiral selector was applied in this work to the development of a method enabling the enantiomeric separation of ketoconazole and terconazole antifungals. The influence of different experimental conditions such as temperature, CD concentration, pH, and nature and concentration of the buffer on the enantiomeric resolution of the compounds studied was investigated. The use of 10 mM heptakis-(2,3,6-tri-O-methyl)-beta-CD in a 100 mM phosphate buffer (pH 3.5) with a temperature of 15 degrees C allowed the separation of the enantiomers of ketoconazole and terconazole with high resolution (R(s) > 2.0). The rapid separation of ketoconazole enantiomers with an analysis time less than 3 min was carried out after fitting some experimental parameters. The developed method was applied to the determination of ketoconazole in different pharmaceutical formulations.
本研究采用以中性环糊精（CD）作为手性选择剂的毛细管电泳法（EKC）来开发一种能够对酮康唑和特康唑这两种抗真菌药物进行对映体分离的方法。研究了不同实验条件，如温度、CD浓度、pH值以及缓冲液的性质和浓度对所研究化合物对映体拆分的影响。在100 mM磷酸盐缓冲液（pH 3.5）中使用10 mM七（2,3,6 - 三 - O - 甲基）-β - 环糊精，温度为15℃时，可实现酮康唑和特康唑对映体的高分辨率分离（R(s) > 2.0）。在优化了一些实验参数后，实现了酮康唑对映体的快速分离，分析时间不到3分钟。所开发的方法应用于不同药物制剂中酮康唑的测定。
