Institute for Pharmacy and Food Chemistry, Julius-Maximilians University Würzburg, Am Hubland, D-97074, Würzburg, Germany.
IBMP - Institute for Biomedical and Pharmaceutical Research, Paul-Ehrlich-Straße 19, D-90562, Nürnberg-Heroldsberg, Germany.
J Pharm Biomed Anal. 2019 Aug 5;172:278-284. doi: 10.1016/j.jpba.2019.04.035. Epub 2019 Apr 16.
The recent incidences of contaminated valsartan drug products gave rise to review the suitability of current impurity profiling workflows implemented at authorities and pharmaceutical companies. The major drawback of targeted impurity profiling, where a considerable amount of prior knowledge about possible contaminants is necessary, is the fact that unexpected impurities are overlooked easily. Here, a generic untargeted approach was applied on sartan containing drug products. The untargeted workflow allowed for the discrimination of different batches, different production sites, and differences after changes in the production process. The presented universal workflow makes use of LC-HRMS/MS and multivariate analysis for the interpretation of the data. Sartan samples contaminated with N-nitrosodimethylamine could be very well discriminated from N-nitrosodimethylamine-free samples using the procedure. Furthermore, untargeted approaches revealed two new impurities in various sartans drug products: valeramide and N,N-dimethylvaleramide.
最近发生的缬沙坦药物污染事件促使人们重新审视当前监管机构和制药公司实施的杂质分析工作流程的适用性。有针对性的杂质分析方法(需要对可能的污染物有大量的先验知识)存在一个主要缺陷,即容易忽略意想不到的杂质。在这里,我们应用了一种通用的非靶向方法对含有沙坦的药物进行分析。非靶向工作流程能够区分不同批次、不同生产地点以及生产工艺变化后的差异。所提出的通用工作流程利用 LC-HRMS/MS 和多元分析来解释数据。使用该方法可以很好地区分含有 N-亚硝基二甲胺和不含 N-亚硝基二甲胺的缬沙坦样品。此外,非靶向方法还在各种沙坦类药物中发现了两种新的杂质:缬氨酰胺和 N,N-二甲基缬氨酰胺。