Bisulfite stabilization of 5-azacytidine

Drug – bio-affecting and body treating compositions – Conjugate or complex of monoclonal or polyclonal antibody,... – Conjugated via claimed linking group – bond – chelating agent,...

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536 23, A61K 3170

Patent

active

044056117

ABSTRACT:
A bisulfite addition product of 5-azacytidine and method wherein bisulfite is added to the azacytidine molecule at the 5-6 protonated imine bond. It is significant and advantageous to maintain the compound in this pro-drug form. At a pH above 6 and including higher physiological pH in animals, the bisulfite form reverts to the parent compound, rendering it readily available for utilization in the body. This product is produced as the bisulfite addition product at preferably a pH of 2.5.

REFERENCES:
patent: 4058602 (1977-11-01), Beisler et al.
Chatteyi et al., Journal of Pharmaceutical Sciences, vol. 68, pp. 822-826, 1979.
Notari et al., J. Pharm. Science, vol. 64, pp. 1148-1157, 1975.

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