Politechnika Gdanska

Instytut Przemyslu Farmaceutycznego

Jan Zielinski

Edward Borowski

Leonard S Falkowski

Jerzy J Golik

Pawel Kolodziejczyk

Barbara J Stefanska

Elzbieta Troka

Andrzej B Jarzebski

Halina Dahlig

Elzbieta Bylec

Zofia Plociennik

Wladyslawa Wagner

Danuta Roslik-Kaminska

Emilia Cybulska

Zuzanna Kowszyk-Gindifer

Ewa Jakobs

Jan Pawlak

Inorganic salts of trimethylammonium derivatives of polyene macrolides, particularly the inorganic salts of methyl esters of these derivatives having the general formula: ##STR1## wherein R is the residue of a polyene macrolide and X is an anion of a salt selected from the group consisting of methylsulphate, sulphate, chloride, phosphate and acetate. The preparation of salts of formula (I) or formula (II) is also disclosed.

Water-soluble salts of trimethylammonium derivatives of polyene

The new compounds, N-methylglucamine salts of N-glycosyl derivatives of polyene macrolides particularly N-methylglucamine salts of N-glycosyl derivatives of amphotericin B, polifungin and nystatin are described herein. These compounds exhibit high pharamacological activity in some topical and sistemic fungal infections. The product is prepared by reaction of an amino group containing polyene macrolide with an aldose or ketose mono- or oligosaccharide, in an organic solvent medium or in the mixture of solvents characterized in that the formed N-glycosyl derivatives is precipitated from the reaction medium by water or with an aqueous solution of inorganic salt, preferably ammonium sulphate, and after crystallization from a higher alkanol of C.sub.3-6 atoms, preferably n-butanol transformed into a salt, preferably an N-methylglucamine salt and then crystallized from higher alkanol, preferably n-butanol.

Salts of N-glycosyl derivatives of polyene macrolides, especially

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Gdansk, Poland

Jan Zielinski