Analysis of gastrointestinal behavior and the prediction of the absorption rate of orally administered drugs using PET molecular imaging technology

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In this study, we investigated the gastrointestinal (GI) behavior of PET probes derived from drugs and its analog with the different physicochemical properties. The GI behavior of our original PET probes, [^<11>C]dehydropravastatin, an organic anion PET probe, and [^<11>C]metformin, an organic cation PET probe, were compared by the PET image analysis. In addition, PET image analysis was performed using [^<18>F]deoxyfluoropoly (ethyleneglycol)s ([^<18>F]FPEG), as a non-absorbable marker to elaborate on more detail of the GI physiology, such as a segmental transition of the administered water and fluid volume and distribution in the intestine. The rate constant of the intestinal transition of radioactivity in each intestinal segment was calculated by the kinetic model analysis, which revealed that PET analysis allows to determine the GI transit from the same individuals and that it is applicable to determine the site specific intestinal absorption. In conclusion, we demonstrated the high potency of PET imaging technique to elucidate the distribution of orally administered solution in the GI tract in experimental animal study.