Water-Soluble polyene conjugate

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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514 54, 514 59, 536 65, 536 111, 536112, 536123, 5361231, 536124, 536127, A61K 3170, C07H 106, C07G 1100, C08B 3702

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active

055676855

ABSTRACT:
A method for producing a substantially stable water-soluble polysaccharide conjugate of a polyene antibiotic is described. The method comprises the following steps: (a) activating the polysaccharide to a dialdehyde by periodate oxidation; (b) purifying the dialdehyde from interfering anions and by-products; (c) coupling the polyene to the purified dialdehyde by Schiff base formation to form the conjugate; and (d) purifying the conjugate. In a preferred embodiment, the conjugate of step (c) is reduced to an amine conjugate by a reducing agent prior to purification. Also described are imine and amine polysaccaride conjugates of the polyene Nystatin.

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