Water-soluble antibiotic comprising an amino sugar, in the form of a polysaccharide conjugate

Abstract

The invention relates to novel pharmaceutical forms for antibiotics containing amino sugar, amphotericin B, daunorubicin and doxorubicin, in which the known side effects are reduced and which can be used in a simple manner. The antimycotic agent B is nephrotoxic. The cytostatic agents daunorubicin and doxorubicin are highly cardiotoxic. The novel pharmaceutical forms are antibiotic-starch conjugates, wherein the antibiotic is combined with the polysaccharide at the reducing end thereof by means of a peptide bond. According to the invention, said bond is carried out by means of J2 oxidation of the starch derivative at the reducing end thereof in an aqueous alkaline solution, and by coupling the starch derivative oxidised thereby to the antibiotic in an organic solution. The conjugates obtained are less toxic. The polysaccharide part can be decomposed by serum-α-amylase and the peptide bond can be accessed by an enzymatic attack.

Dependencies are inferred from the claim text.