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在α1-酸性糖蛋白柱和卵类粘蛋白柱上进行钙拮抗剂手性液相色谱分离的设计。

Design of chiral LC separations for calcium antagonists on alpha 1-acid glycoprotein and ovomucoid columns.

作者信息

De Lorenzi E, Fell A F, Caccialanza G, Massolini G, Kitsos M

机构信息

Department of Pharmaceutical Chemistry, University of Pavia, Italy.

出版信息

J Pharm Biomed Anal. 1992 Oct-Dec;10(10-12):909-15. doi: 10.1016/0731-7085(91)80098-t.

DOI:10.1016/0731-7085(91)80098-t
PMID:1298397
Abstract

Three chiral calcium antagonist drugs, gallopamil and two dihydropyridine derivatives, have been successfully separated within short retention times using both the alpha 1-acid glycoprotein chiral stationary phase (Chiral-AGP) and the ovomucoid column (Ultron ES-OVM). Aqueous buffer at defined pH is modified by the addition of an organic component, in order to modulate the retention properties of each system. Optimization of pH and organic modifier is carried out using the modified simplex method, with Kaiser's peak separation function as a criterion. The influence of pH and percentage of organic modifier on retention, selectivity, resolution and column performance are discussed for the two dihydropyridines analysed on Chiral-AGP and Ultron ES-OVM stationary phases. A new method is proposed as a new chiral system suitability test for these protein-based phases, utilizing a racemic mixture of closely eluting verapamil enantiomers as a probe.

摘要

使用α1-酸性糖蛋白手性固定相(Chiral-AGP)和卵类粘蛋白柱(Ultron ES-OVM),在较短的保留时间内成功分离了三种手性钙拮抗剂药物,即加洛帕米和两种二氢吡啶衍生物。通过添加有机成分来调节特定pH值的水性缓冲液,以调节每个系统的保留特性。使用改进的单纯形法,以Kaiser峰分离函数为标准,对pH值和有机改性剂进行优化。讨论了在Chiral-AGP和Ultron ES-OVM固定相上分析的两种二氢吡啶的pH值和有机改性剂百分比对保留、选择性、分离度和柱性能的影响。提出了一种新方法,以紧密洗脱的维拉帕米对映体的外消旋混合物作为探针,作为这些基于蛋白质的固定相的新手性系统适用性试验。

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引用本文的文献

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Gallopamil. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic potential in ischaemic heart disease.加洛帕米。对其药效学和药代动力学特性以及在缺血性心脏病中的治疗潜力的综述。
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