Identification of the absorbed components and their metabolites of Tianma‐Gouteng granule in rat plasma and bile using ultra‐high‐performance liquid chromatography combined with quadrupole time‐of‐flight mass spectrometry

Zhang H, Duan S, Wang L, Liu J, Qi W, Yuan D · Biomedical Chromatography · 2019 February

Objective

To investigate the absorbed prototype components and related metabolites of Tianma-Gouteng granule in rat plasma and bile after oral administration at high and normal clinical dosages using ultra-performance liquid chromatography coupled with quadrupole time-of-flight mass spectrometry.

Conclusions

The study identified 68 components in rat plasma and bile, showing that Tianma-Gouteng granule components undergo phase I reactions including isomerization, hydrolysis and reduction and predominantly phase II biotransformation involving glucuronidation and sulfation.

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Insights

The intake of Tianma-Gouteng granule, a Chinese herbal formula, results in absorption and metabolising of numerous identified compounds, with the phase II biotransformation pathway as the main metabolic process.

The study used a novel method of Ultra Performance Liquid Chromatography-Quadrupole Time of Flight Mass Spectrometry (UPLC-Q/TOF MS) to detect and identify absorbed components of Tianma-Gouteng granule (TGG) and related metabolites in rat plasma and bile, after the oral administration of TGG at normal and high clinical dosages. In total, 68 components were recognized in the plasma and bile samples which included both absorbed prototypes and their metabolites. The key observation was that the major absorbed components underwent significant phase I (isomerization, hydrolysis and reduction) and phase II (glucuronidation and sulfation) reactions, with the phase II biotransformation pathway being predominantly involved. This data provides substantive information on the absorption and metabolism of TGG in a live organism, marking an important step in the analysis of TGG's pharmacokinetics and pharmacodynamics.