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A Rapid and Sensitive Liquid Chromatography–Tandem Mass Spectrometry Method for the Quantification of Nitrosamine Impurities in an Anticoagulant Drug: Application to Drug Substance and Pharmaceutical Dosage Forms

Abhishek Sharma, Narayana Reddy Pedavenkatagari, Santhosh Kumar Ettaboina, Srinivas Nakka

2025Separation Science Plus9 citationsDOIOpen Access PDF

Abstract

ABSTRACT Nitrosamine impurities are formed when amines react with nitrosating agents under acidic or high‐temperature conditions. Since many nitrosamines are known carcinogens, strict regulatory limits have been established to control their presence in pharmaceuticals. Detecting such impurities requires highly sensitive and reliable analytical methods. In this study, a liquid chromatography–tandem mass spectrometry (LC–MS/MS) method was developed and validated for the trace‐level quantification of N ‐nitroso‐ N ‐desmethyl‐edoxaban in both the drug substance and pharmaceutical dosage forms. Separation was achieved on an ACE Excel‐3 C18 column using gradient elution, with 0.01 M ammonium formate in water as Phase A and a 10:90 (v/v) water–acetonitrile mixture as Phase B. The method employed electro spray ionization in multiple reaction monitoring mode, with a flow rate of 0.4 mL/min at 30°C. The monitored mass transition was 563.00 → 533.15 m/z . Validation followed International Council for Harmonization guidelines (ICH) and United States Pharmacopeia (USP) <1225> requirements. The method demonstrated high sensitivity, with a limit of detection (0.03 µg/mL) and limit of quantification (0.08 µg/mL). Linearity was excellent, with correlation coefficients ( R 2 ) greater than 0.99. Accuracy and recovery results were within the acceptable range of 80%–120%. This validated LC–MS/MS method is suitable for routine quality control and effective monitoring of nitrosamine impurities in edoxaban‐based pharmaceutical products, ensuring compliance with regulatory standards.

Topics & Concepts

ChemistryChromatographyDetection limitAmmonium formateDosage formMass spectrometryImpurityPharmaceutical formulationBioanalysisAtmospheric-pressure chemical ionizationAnalytical Chemistry (journal)Liquid chromatography–mass spectrometryActive ingredientOrbitrapSolid phase extractionResolution (logic)Quantitative analysis (chemistry)Liquid–liquid extractionChemical ionizationVolumetric flow rateExtraction (chemistry)Pharmaceutical drugReagentAccuracy and precisionPhase (matter)High-performance liquid chromatographySelected reaction monitoringWater Treatment and DisinfectionEnvironmental Chemistry and AnalysisPer- and polyfluoroalkyl substances research
A Rapid and Sensitive Liquid Chromatography–Tandem Mass Spectrometry Method for the Quantification of Nitrosamine Impurities in an Anticoagulant Drug: Application to Drug Substance and Pharmaceutical Dosage Forms | Litcius