製剤学的研究 第9報

ビタミンA, Dの水溶化 その5 Sucrose Monoesterによる可溶化

抄録

Solubilization of vitamins A and D in water has heretofore been effected by surfaceactive agents of polyethylene glycol system. In order to improve the defects of such agents, solubilization was attempted with sucrose monoester. Sucrose ester was prepared by the method of Osipow and others, using straight-chain saturated fatty acids from caproic to stearic acid, and 10 kinds of esters of C₁₈-unsaturated acid. Esters of fatty acids below C₁₄ and those of linolic and linolenic acids have bitter taste. Solubilization of vitamin A palmitate was well effected by linoleate, that of vitamin A acetate by laurate, caproate, and myristate, and that of vitamin A alcohol and D₂ by caprate, caprylate, and laurate. The aqueous solution in which solubilization had been effected perfectly does not undergo clouding on heating. The mechanism of solubilization is assumed to be the same as in other surface-active agents, that of micelle formation. Oral toxicity of sucrose esters is very small and it seems possible to use it for solubilization in foodstuffs, but its toxicity by intravenous injection is stronger than that of the Tweens. This latter is thought to be due to their hemolytic action and their use in injections requires caution.