| 摘要 |
PURPOSE:An antitumor agent showing high water-solubility, comprising 5,6-O- benzylidene-L-ascorbic acid or its salt as an active ingredient. CONSTITUTION:An antitumor agent containing 0.1-20wt% 5,6-O-benzylidene-L- ascorbic acid shown by the formula or its salt as an active ingredient in the case of oral or mucosa absorption, and 0.01-10wt% 5,6-benzyl-O-ascorbic acid or its salt in the case of parenteral absorption. The compound shown by the formula as an active ingredient is obtained by reacting L-ascorbic acid with alpha,alpha- dimethoxytoluene in dimethyl sulfoxide, etc. in the presence of an acid catalyst (e.g., p-toluenesulfonic acid, etc.) under heating. The antitumor agent can be administered orally or parenterally, and as dosage form, capsule, tablet, fine granule, powder, injection, ophthalmic solution, suppository, etc. may be cited. A dose is 500-1,000g/day/person.
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