Developing Validated Method to Analyze Canagliflozin and Determine its Metabolites in Rat Plasma by LC-UV/MS


Rawa Akasha, Abdul Wahab Allaf and Mohammad Amer Al-Mardini

Published in

Arab Journal of Pharmaceutical Sciences, Journal of the Society of Arab Universities, Volume 6, Issue 3, May 2020.


Canagliflozin is a novel, orally selective inhibitor of sodium-dependent glucose co-transporter-2 (SGLT2) for the treatment of patients with type 2 diabetes mellitus.

In this study, a sensitive method for the separation and quantification of canagliflozin and its metabolites in rat plasma were established and validated.

Chromatographic separation of canagliflozin and its metabolites was carried out on C18 column (250×4.6 mm, i.d. 5μm) using acetonitrile–formic acid 0.1% in a gradient mode as mobile phase at a flow rate of 0.5 mL/ min. Canagliflozin and its metabolites were extracted from rat’s plasma by protein precipitation method using methanol. The mass spectrometric detection was performed using electrospray ionization source in negative mode ESI-.

The method was validated according to USP 35 guideline recommendations and to the ICH guidelines for validation. The method is suitable to apply in the characterization of oral pharmacokinetic profiles of canagliflozin in rats.

Keywords: Canagliflozin, metabolites, LC-MS, Plasma, validation.

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