1963 年 83 巻 7 号 p. 663-671
Various O-acyithiamines were prepared by the oxidation of O-acrylate, O-methacrylate, O-crotonate, and O-undecylenate of thiothiamine and high-molecular derivatives of thiamine were obtained by their polymerization. Copolymer of these with vinyl compounds was also prepared.
Oral administration of these high-molecular derivatives in man and measurement of the amount of thiamine excreted in the urine showed that the total amount excreted during 24 hours was 1/2 to 1/4 of that after administration of thiamine hydrochloride. The peak of excretion appeared much later, 7-12 hours later than that of thiamine, and indicated the lasting effect of high-molecular derivatives. Of these derivatives, those with smaller molecular weight were excreted in larger amount, and copolymers were excreted in larger amount than homopolymers. Greater urinary excretion was found in basic comonomers than acid comonomers among these copolymers.
These experimental results showed the same tendency as that shown by hydrolysis of high molecular derivatives with alkali or diastase. O-Methacryloyl derivative was not hydrolyzed by alkali or diastase but was hydrolyzed in vivo to be excreted into urine in a similar manner as the other derivatives.