Formation of a Thiol–Ene Addition Product of Asthma Medication Montelukast Caused by a Widespread Tin-Based Thermal Stabilizer,Chemical Research in Toxicology

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Formation of a Thiol–Ene Addition Product of Asthma Medication Montelukast Caused by a Widespread Tin-Based Thermal Stabilizer
Chemical Research in Toxicology ( IF 3.7 ) Pub Date : 2020-11-11 , DOI: 10.1021/acs.chemrestox.0c00261
Philipp Schmidt ₁ , Christine Kolb ₂ , Andreas Reiser ₂ , Markus Philipp ₂ , Markus Godejohann ₃ , Hannes Helmboldt ₄ , Hans-Christian Müller ₂ , Konstantin Karaghiosoff ₁

Affiliation

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.

中文翻译：

由广泛使用的锡基热稳定剂引起的哮喘药物孟鲁司特的硫醇-烯加成产物的形成

我们报告了咀嚼片中哮喘药物孟鲁司特的两种非对映异构硫醇-烯加成产物的形成和表征。广泛使用的锡基热稳定剂二辛基锡双（2-乙基己基巯基乙酸盐）和单辛基锡三（2-乙基己基巯基乙酸盐），用于药物成型箔的制造过程，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功能类似于孟鲁司特的 API 的降解中发挥作用，在药物开发过程中应考虑到这一点。这些杂质的分离和分析是通过 HPLC 和 UV-vis 光谱进行的。收集 HRMS 和 NMR 数据以表征和确定这些化合物的结构。

更新日期：2020-12-21

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