Naringin has been documented to possess multiple pharmacological activities. Reported pharmacokinetic studies revealed that oral bioavailability of naringin was low, in contrast to its significant pharmacological effects. The in vivo distribution of naringin and derived metabolites might partly explain this discrepancy. In this study, an ultra-fast liquid chromatography-quadrupole-time-of-flight tandem mass spectrometry system (UFLC-Q-TOF-MS/MS) was used for profiling the distribution of naringin and its metabolites in rat plasma and fourteen tissues after oral administration. Naringin was widely distributed and its concentrations in certain tissues were much higher than that in plasma, especially in trachea and lung. Moreover, a total of 23 flavonoid metabolites and 15 phenolic catabolites were screened. Naringenin glucuronides were principal metabolites in plasma, while free naringenin and naringenin-7-O-sulfate were the major molecular forms in most tissues. Meanwhile, phenolic catabolites derived from naringin were found to be abundant in liver and kidney. These pharmacokinetic results would be useful to explain the pharmacodynamics of naringin.
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