Abstract
Ilaprazole is a proton pump inhibitor used to treat digestive diseases. In this study, blood samples were collected after oral administration of ilaprazole and prepared by liquid–liquid extraction. The metabolites of ilaprazole were detected by liquid chromatography–high-resolution mass spectrometry (LC-HRMS) and LC-MSn. A total of twelve in vivo metabolites were detected in rat plasma and six new metabolites of ilaprazole, including one reductive metabolite with sulfide (M3), two hydroxylated metabolites with sulfoxide (M7 and M8), and three oxidative metabolites with sulfone (M9, M11, and M12), were identified. The possible metabolic pathways of ilaprazole and the fragmentation behaviors of its metabolites were elucidated. The result of the in silico prediction indicates that all the new metabolites showed the potential ability to inhibit H+/K+-ATPase activity.
Highlights
Ilaprazole is a proton pump inhibitor (PPI) that was approved for the treatment of digestive diseases such as gastroesophageal reflux disease, peptic ulcers, and helicobacter pylori infections [1,2,3,4,5,6]
The present study aims to identify in vivo metabolites of ilaprazole in rat plasma by liquid chromatography coupled with mass spectrometry (LC-MS)
After being prepared by liquid–liquid extraction, the samples were detected via liquid chromatography–tandem high-resolution mass spectrometry (LC-HRMS/MS).The fragmentation behaviors of ilaprazole and its metabolites have been elucidated by LC-MSn and liquid chromatography–high-resolution mass spectrometry (LC-HRMS)/MS
Summary
Ilaprazole is a proton pump inhibitor (PPI) that was approved for the treatment of digestive diseases such as gastroesophageal reflux disease, peptic ulcers, and helicobacter pylori infections [1,2,3,4,5,6]. The [M + H]+, fragment ions, and the retention time of M1 were the same as the reference standards of ilaprazole sulfide. Retention time of M2 were the same as the reference standards of ilaprazole sulfone These proposed fragment ions can be supported by MSn (Supplementary Material Figure S1C). The [M + H]+, fragment ions, and the retention time of M2 were the same as the reference standards of ilaprazole sulfone.
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