Krstulović A M, Fouchet M H, Burke J T, Gillet G, Durand A
L.E.R.S.-SYNTHELABO, Recherche Analytique et Contrôle Pharmaceutique,Meudon la Forêt, France.
J Chromatogr. 1988 Oct 28;452:477-83. doi: 10.1016/s0021-9673(01)81470-9.
A direct method is described for the resolution of the enantiomers of betaxolol, a novel cardioselective beta-adrenergic blocking agent, using a tris(3,5-dimethylphenylcarbamate)cellulose chiral column. An excellent resolution of the two antipodes is obtained (Rs greater than 2) with high peak symmetries. The method is simple and ideally suited to the routine control of the enantiomeric excess in the bulk drug and the analysis of the enantiomers of betaxolol in hepatocyte suspensions. With modification of the polar modifier in a hexane-based mobile phase, most commercially available beta-blockers can be baseline resolved.
描述了一种直接方法，使用三（3,5-二甲基苯基氨基甲酸酯）纤维素手性柱拆分新型心脏选择性β-肾上腺素能阻滞剂倍他洛尔的对映体。两种对映体获得了出色的分离度（Rs大于2），峰对称性高。该方法简单，非常适合原料药对映体过量的常规控制以及肝细胞悬浮液中倍他洛尔对映体的分析。通过改变基于己烷的流动相中的极性改性剂，大多数市售的β-阻滞剂都可以实现基线分离。
