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哮喘药物孟鲁司特与广泛使用的锡基热稳定剂发生硫醇-烯加成产物的形成。

Formation of a Thiol-Ene Addition Product of Asthma Medication Montelukast Caused by a Widespread Tin-Based Thermal Stabilizer.

机构信息

Department Chemie, Ludwig-Maximillians-Universität München, Butenandtstraße 5-13, Haus D, 81377 Munich, Germany.

Analytical Development, Hexal AG, Industriestraße 25, 83607 Holzkirchen, Germany.

出版信息

Chem Res Toxicol. 2020 Dec 21;33(12):2963-2971. doi: 10.1021/acs.chemrestox.0c00261. Epub 2020 Nov 11.

Abstract

We report the formation and characterization of two diastereomeric thiol-ene addition products of the asthma medication Montelukast within chewing tablets. Widespread tin-based thermal stabilizers dioctyltin bis(2-ethylhexyl thioglycolate) and monooctyltin tris(2-ethylhexyl thioglycolate), used in the manufacturing process of the medication's forming foil, were identified as the source of the thiol reactant, showing that these stabilizers may play a part in the degradation of Montelukast and APIs with functionalities similar to those of Montelukast, which should be considered during development of medication. The isolation and analysis of these impurities was performed by HPLC and UV-vis spectroscopy. HRMS and NMR data were collected to characterize and determine the structures of these compounds.

摘要

我们报告了哮喘药物孟鲁司特在咀嚼片中两种非对映异构体硫醇-烯加成产物的形成和特性。在药物成型箔的制造过程中使用的广泛的基于锡的热稳定剂二辛基锡双(2-乙基己基硫代甘醇酸酯)和单辛基锡三(2-乙基己基硫代甘醇酸酯)被确定为硫醇反应物的来源,表明这些稳定剂可能在孟鲁司特和具有与孟鲁司特类似官能团的 API 的降解中发挥作用,这在药物开发过程中应加以考虑。这些杂质的分离和分析通过 HPLC 和 UV-vis 光谱法进行。收集了 HRMS 和 NMR 数据以对这些化合物进行表征和确定其结构。

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