METABOLIC CONVERSION OF CYCLOCARBO-THIAMINE INTO THIAMINE

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  • SHIOBARA YUICHI
    Central Research Laboratory, Yamanouchi Pharmaceutical Company
  • SATO NOBORU
    Central Research Laboratory, Yamanouchi Pharmaceutical Company
  • YOGI KEIKO
    Central Research Laboratory, Yamanouchi Pharmaceutical Company
  • MURAKAMI MASUO
    Central Research Laboratory, Yamanouchi Pharmaceutical Company

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Abstract

Metabolic conversion of cyclocarbothiamine into thiamine was studied in vivo as well as in vitro.<br>1. The compound was easily transformed into thiamine when incubated with rabbit blood.<br>The supernatant obtained from liver and kidney homogenate of rats also changed cyclocarbothiamine into thiamine. No such conversion occurred with heated supernatant.<br>2. Manometric measurement of carbon dioxide liberated during the conversion showed that it was produced in an amount equimolar to thiamine.<br>3. Bioautography with Lactobacillus fermenti revealed that not a trace of cyclocarbothiamine remained unchanged in blood samples taken 30 minutes after oral or intravenous administration to rabbits. Nor was it detected as such in urine.<br>However, a trace amount of the compound was detected unaltered in threehour urine samples following oral administration of 50mg to human subjects.<br>4. The following metabolic schema has been established.<br>Cyclocarbothiamine → Thiamine+CO2

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