2. Academic Validation
  3. Characterisation of degradation products of tegoprazan by LC-MS and GC-MS

Characterisation of degradation products of tegoprazan by LC-MS and GC-MS

  • J Pharm Biomed Anal. 2023 May 10:228:115323. doi: 10.1016/j.jpba.2023.115323.
Kaijing Guo 1,  Xiao He 1,  Hongyi Zhao 1,  Chen Ma 2
Affiliations

Affiliations

  • 1 Institute of Materia Medica, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China.
  • 2 Institute of Materia Medica, Chinese Academy of Medical Science and Peking Union Medical College, Beijing 100050, China. Electronic address: [email protected].
PMID: 36921447 DOI: 10.1016/j.jpba.2023.115323
Abstract

Tegoprazan is a novel orally active potassium-competitive acid blocker (P-CAB), capable of binding to the K+ binding site of H+/K+-ATPase in a reversible way to inhibit gastric acid secretion. Tegoprazan has been approved for treating acid-related diseases. In this study, stress testings of tegoprazan were performed under various conditions, including hydrolysis (acidic, alkaline, and neutral), oxidation, photolysis, and thermal stress. Tegoprazan showed instability in acidic, alkaline, and oxidative conditions. Eight degradation products (DPs) were identified. The DPs were characterized by LC-HRMS, LC-MSn, or GC-Q-TOF-MS. Meanwhile, DP-1, DP-2 and DP-3 were successfully synthesized and confirmed by NMR. The degradation pathway of tegoprazan was summarized. To the best of our knowledge, this is the first study on the forced degradation of tegoprazan.

Keywords

GC-Q-TOF-MS; LC-HRMS; LC-MS(n); NMR; Stress testing; Tegoprazan.

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