发明名称 METHOD FOR PREPARING N4-PROPYLAJMALINIUM SALTS WITH CARBOXYLIC ACIDS, STABLE SOLUTION OF N4-PROPYLAJMALINIUM HYDROMALONATE AND METHOD FOR ITS PREPARING
摘要 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
申请公布号 RU2296765(C1) 申请公布日期 2007.04.10
申请号 RU20050131778 申请日期 2005.10.13
申请人 GOSUDARSTVENNOE OBRAZOVATEL'NOE UCHREZHDENIE VYSSHEGO PROFESSIONAL'NOGO OBRAZOVANIJA SANKT-PETERBURGSKAJA GOSUDARSTVENNAJA KHIMIKO-FARMATSEVTICHESKAJA AKADEMIJA (GOU VPO SPKHFA ROSZDRAVA) 发明人 SEVBO DMITRIJ PETROVICH;GROMOVA LIDIJA IVANOVNA;SHEBATIN RUSLAN VLADIMIROVICH;ERMAKOVA MARINA VLADIMIROVNA
分类号 C07D471/18;A61K9/08;A61K31/475;A61P9/06;C07D459/00 主分类号 C07D471/18
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