薬物動態試験,血球移行性試験およびB_1復元試験よりみたビタミンB_1誘導体の評価

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To evaluate the merits of commercially available leading thiamin derivatives, thiamin tetrahydrofurfuryl disulfide (TTFD), O-benzoylthiamin disulfide (BTDS), and S-benzoylthiamin O-monophosphate (BTMP), were studied in the following 3 experiments. The requirements of commercially available thiamin derivatives are also discussed from the point of view of effectiveness and safety. 1. Bioavailability Study in Human Subjects: Commercial tablets containing 100 mg of TTFD, or BTDS and a powder formulation containing 100 mg of thiamin were administered to healthy subjects and their bioavailability was evaluated by determining the blood concentration and urinary excretion of thiamin. It was found that the bioavailability of TTFD was better than that of BTDS or thiamin, according to the indices of C_<max>, T_<max>, AUC, and the 48-hour urinary excretion of thiamin. 2. Uptake into Human Blood Cells: An in vitro test was carried out to compare the uptake of TTFD, BTDS, BTMP, and thiamin into human blood cells. Most of the TTFD was incorporated by blood cells and converted into thiamin, but BTDS and thiamin largely remained in the supernatant. Most of the BTMP was not converted into thiamin under these experimental conditions. 3. Conversion to Thiamin by Rat Liver Homogenate: An in vitro test of the conversion of thiamin derivatives to thiamin by rat liver homogenate showed that TTFD was readily converted to thiamin by either fresh or boiled liver homogenate. BTDS was rapidly converted to O-benzoylthiamin (OBT), an intermediate metabolite, but conversion from O-benzoylthiamin to thiamin was very slow. BTMP was converted to thiamin fairly readily by fresh liver homogenate, but conversion was negligible when boiled liver homogenate was used.
日本ビタミン学会の論文
1992-01-25

薬物動態試験,血球移行性試験およびB_1復元試験よりみたビタミンB_1誘導体の評価

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