Enantioselective Analysis and Separation of Two β-Blockers via Derivatization Approach

IF 2.8 4区 化学 Q2 CHEMISTRY, ANALYTICAL Chirality Pub Date : 2025-01-06 DOI:10.1002/chir.70010
Vinod, Shubham Sharma, Rajasekhar V. S. R. Pullabhotla, Ankit Mittal
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Abstract

Enantiomeric analysis of chiral drugs is very significant, as their enantiomers display different pharmacological or toxicological behavior towards living systems. Among these drugs, β-blockers are available as racemates, where their enantiomers display different pharmacological effects. Herein, we report enantioselective separation of two β-blockers, namely, atenolol and sotalol, using a derivatization approach. The analytes were derivatized with “(S)-1-[1H-benzo(d)(1,2,3)triazol-1-yl]-2-[6-methoxynaphthalen-2-yl-propan-1-one]” {(S)-BTMNP} in a straightforward derivatization step. The resulting diastereomers were separated on a reverse-phase HPLC C18 column with a mobile phase composed of acetonitrile and TEAP buffer (75:25, v/v, pH = 3.5) and detection at 230 nm. This method achieved successful enantiomer separation for both drugs within 20 min, yielding resolution values greater than 3.8. The detection limits were determined to be 6.4 and 4.6 ng mL−1 for atenolol and sotalol, respectively, which indicated sensitivity and effectiveness of the method for the analysis of two β-blockers from their dosage formulations.

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衍生化法分离两种β受体阻滞剂的对映选择性分析。
手性药物的对映体分析是非常重要的,因为它们的对映体对生命系统表现出不同的药理或毒理学行为。在这些药物中,β受体阻滞剂以外消旋体的形式存在,它们的对映体表现出不同的药理作用。在此,我们报告了两种β受体阻滞剂,即阿替洛尔和索他洛尔,使用衍生化方法的对映选择性分离。在直接的衍生化步骤中,分析物被“(S)-1-[1h -苯并(d)(1,2,3)三唑-1-基]-2-[6-甲氧基萘-2-基丙烷-1- 1]”{(S)- btmnp}衍生化。分离得到的非对映体采用C18反相高效液相色谱柱进行分离,流动相为乙腈和TEAP缓冲液(75:25,v/v, pH = 3.5),检测波长为230 nm。该方法在20 min内成功分离了两种药物的对映体,分离值大于3.8。阿替洛尔和索他洛尔的检出限分别为6.4和4.6 ng mL-1,表明该方法对两种β受体阻滞剂的剂量分析具有敏感性和有效性。
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来源期刊
Chirality
Chirality 医学-分析化学
CiteScore
4.40
自引率
5.00%
发文量
124
审稿时长
1 months
期刊介绍: The main aim of the journal is to publish original contributions of scientific work on the role of chirality in chemistry and biochemistry in respect to biological, chemical, materials, pharmacological, spectroscopic and physical properties. Papers on the chemistry (physiochemical, preparative synthetic, and analytical), physics, pharmacology, clinical pharmacology, toxicology, and other biological aspects of chiral molecules will be published.
期刊最新文献
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