Key result
Stress degradation of apixaban yields five distinct products including novel positional isomers.
Why the study?
Previous reports tentatively identified apixaban degradation products using mass analysis alone without confirmation from nuclear magnetic resonance spectroscopy.
The study identified and structurally characterized five degradation products of apixaban under stress conditions, including two novel positional isomers, using advanced analytical techniques.
May guide apixaban stability testing; leaves open clinical or regulatory relevance pending validation.
The current research explains the stress degradation behavior of Apixaban, which is an anticoagulant or blood thinner. The degradation was conducted using hydrolytic, oxidative, thermal, and photolytic conditions. Apixaban is relatively stable in oxidative, thermal, and photolytic conditions; however, considerable degradation was observed in acid and base hydrolysis. Degradation products were identified using ultra-high performance liquid chromatography-mass spectrometry, isolated using semi-preparative high-performance liquid chromatography, and structural characterization by high-resolution mass spectrometry and nuclear magnetic resonance spectroscopy. A total of five degradation products were identified and isolated in acid and base degradation. Degradation products 1, 2, and 3 were observed in acid conditions, whereas in base conditions, along with those three, two more degradation products 4 and 5 were identified. The representative thing was that among the five degradation products, two sets of positional isomers 1, 4, and 2, 5 were observed; out of which 2 and 5 are novel. The remaining degradation products 1, 3, and 4 are already reported tentatively using a single analytical technique of mass analysis without any evidence from nuclear magnetic resonance spectroscopy. Hence, the present study focused on using high-resolution mass, and nuclear magnetic resonance spectroscopy data for concrete confirmation of structures for degradation products.
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Salakolusu et al. (2022) studied this question. Apixaban was evaluated on Identification and structural characterization of degradation products. Stress degradation of apixaban under acid and base hydrolysis yielded five degradation products, including two novel positional isomers, structurally confirmed by high-resolution mass and NMR.
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