Water-soluble polyene conjugate

摘要

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.