METHOD FOR PREPARING N-PROPYLAJMALINIUM SALTS WITH CARBOXYLIC ACIDS, STABLE SOLUTION OF N-PROPYLAJMALINIUM HYDROMALONATE AND METHOD FOR ITS PREPARING Russian patent published in 2007 - IPC C07D471/18 A61K31/475 A61K9/08 C07D459/00 A61P9/06 

FIELD: medicine, chemical-pharmaceutical industry, chemical technology.

SUBSTANCE: invention relates to using biologically active derivatives of ajmaline possessing anti-arrhythmic effect. Method for synthesis of N₄-propylajmalinium salts with carboxylic acids is carried out by neutralization of N₄-propylajmalinium hydroxide with equivalent amount of carboxylic acid in homogenous phase. The end substance is isolated by distillation of solvent with the yield of salts 97-99%. Method provides preparing acetate, l-lactate, hydrooxalate, hydromalonate, hydrosuccinate, hydroglutarate, l-hydrotartrate, hydrocitrate, salicylate and p-aminobenzoate. Stable solution of N₄-propylajmalinium hydromalonate in water for injection of a medicinal agent comprises sodium metabisulfite as antioxidant, 5-30 mg/ml of N₄-propylajmalinium hydromalonate, ascorbic acid as antioxidant taken in the effective amounts. Preferably, stable solution of N₄-propylajmalinium hydromalonate comprises 10 mg of N₄-propylajmalinium hydromalonate/ml of solution, 0.20 wt.-% of sodium metabisulfite and 0.05 wt.-% of ascorbic acid as measured for solution of N₄-propylajmalinium hydromalonate. Invention provides the development stable aqueous compositions of N₄-propylajmalinium salts for injection of medicinal agent by selection of antioxidants.

EFFECT: improved preparing method.

7 cl, 5 tbl, 5 ex