Soluble derivatives of silybin, a method of preparing them, and

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Phosphorus containing other than solely as part of an...

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549220, A61K 31335, C07D31920

Patent

active

048867918

ABSTRACT:
Novel water-soluble derivatives of silybin of enhanced activity are provided as well as methods of preparing the derivatives and pharmaceutical compositions containing them. The novel derivatives according to the invention have the following general formula (I); ##STR1## where: R=H or PO(OH).sub.2 and R'=PO(OH).sub.2 The compounds of the invention are useful inter alia in therapy of liver disorders and other applications where an anti-radical effect is required. They have the advantages of high hydrophilicity and are soluble at approximately pH 4, compared to prior art compounds which are water-soluble only at higher pH and enhanced stability.

REFERENCES:
The Merck Index, 10th edition, Merck & Co., Inc., Rahway, N.J., U.S.A., 1983, p. 1224, No. 8372.

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