Abstract
Rise of blood thiamine levels by the intravenous injection of various O-acylthiamine disulfides into rabbit were investigated. Applying kinetics, the elimination constants and biological half-lives of thiamine were determined for each derivative and precise and reliable comparison of the each was made possible. It was found that the derivative of 4-carbon aliphatic acyl groups was the most excellent one giving the highest thiamine lebel and its sustention. Both increase and decrease of the acyl carbon numbers resulted the lower blood level and higher elimination rate. These values were found to be correlated with in vitro penetrating abilities into erythrocytes of each derivative. Solubility, stability and other properties of the 4-carbon acyl derivative, O-butyroylthiamine disulfide, were tested and it was concluded that the new compound may be of value for pharmaceutical and clinical use.
