Stability, Bactericidal Activity, Vitamin B6 Activity and Gastrointestinal Absorption of Benzoic Acid Esters of Pyridoxine

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α4-O-Benzoyl-pyridoxine (PN-4MB) and α5-O-benzoyl-pyridoxine (PN-5MB) were hydrolyzed in 10% aqueous solution of acetone at pH 1-4. They were hydrolyzed obeying apparent first-order kinetics. In the pH range of 1-7, PN-4MB was hydrolyzed 10 times faster than PN-5MB. At pH 7-12, an interconversion between the two derivatives was observed. They were bactericidal against Escherichia coli and Bacillus subtilis and prevented severe convulsions induced in mouse by 4-methoxypyridoxine, a potent antagonist of vitamin B6. PN-4MB was hydrolyzed with the homogenate of rat liver more easily than PN-5MB. The metabolite of PN-MBs in man was identified as 4-pyridoxic acid, i.e., a principal metabolite of PN, using high-performance liquid chromatography. The amount of urinary excretion of 4-pyridoxic acid in 10 hr after oral administration of PN-4MB or PN-5MB was as large as that of PN.
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