KR880002530A - Injectable Compositions with Cephalosporins - Google Patents

Abstract

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Description

Injectable Compositions with Cephalosporins

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Figure 1 shows Form 7- [, determined by dilution with KBr. -(2-aminothiazol-4-yl)- Infrared absorption spectrum of-(Z) -methoxyimino acetamido] -3-[(1-methyl-1-pyrrolidinio) methyl] -3-cephem-4-carboxylate sulfate is shown in graphs.

2 shows 7- [as measured by dilution with KRr. -(2-Aminothiazol-4-yl) -X- (Z) -methoxy-imino acetamido] -3-[(1-methyl-1-pyrrolidinio) -methyl] -3- Infrared absorption spectra of crystalline cesky phosphate of cefem-4-carboxylate are shown in graphs.

3 shows 7- [as measured by dilution with KBr. -(2-Aminothiazol-4-yl) -X- (Z) -methoxy-imino acetamido] -3-[(1-methyl-1-pyrrolidino) -methyl] -3-cepem The infrared absorption spectrum of the crystalline diphosphate of 4-carboxylic acid salt is shown in graph.

Claims (15)

Orthophosphoric acid addition salts containing sulfuric acid, 2-nitric acid, mono-hydrochloric acid and di-hydrochloric acid addition salts and 1.5-2 molar equivalents of H ₃ PO ₄ , or solvates thereof 7- [ -(2-aminothiazol-4-yl)- -(Z) -methoxyiminoacet amido] -3-[(1-methyl-1-pyrrolidinio) -methyl] -3-cefem-4- carboxylate salt of crystalline phase stable. The crystalline salt of claim 1 selected from the group consisting of sulfuric acid, mono-hydrochloric acid, dihydrochloric acid and orthophosphoric acid addition salts, or solvates thereof. A physical mixture of pharmaceutically acceptable non-toxic organic or inorganic bases and salts of claim 1 in a proportion of about 3.5 to about 7 by diluting the mixture with water to an injectable concentration. The physical mixtures recited in claim 3, wherein the salts and bases are present in proportions such that the mixture is diluted with water to an injectable concentration to a pH of about 4 to about 6. The physical mixture recited in claim 4, wherein the base is L (+) lysine. The physical mixture recited in claim 4, wherein the base is L (+) arginine. (a) forming an aqueous solution of a mixture of (i) at least one molar equivalent of sulfuric acid and (ii) a zwitterion corresponding to the base, and (b) the zwitterion is present in the mixture at a concentration of 25 mg / ml or less, The crystallization of sulfuric acid addition salts is carried out under the condition that the crystallization is carried out in the presence of an organic solvent, and (c) a process for producing sulfate addition salts comprising the steps of separating the sulfuric acid addition salts in the crystal phase. The process as recited in claim 7, wherein step (b) is carried out in an organic solvent-free aqueous medium. The process recited in claim 8, wherein the zwitterion is used in step (a) in an amount sufficient to be present in the mixture at a concentration of up to 500 mg / ml. The method recited in claim 7 wherein the amount of zwitterion used in step (a) is present in the mixture at a concentration of at least 25 mg / ml. The method recited in claim 8, wherein the zwitterion is used in step (a) in an amount such that the zwitterion is present in the mixture at a concentration ranging from about 100 mg / ml to about 200 mg / ml. Sulfuric acid addition salt of the crystalline phase of claim 1. Next 7- [of crystalline phase with X-ray powder diffraction model -(2-aminothiazol-4-yl)- Sulfate of-(Z) -methoxy-imino acetamido] -3-[(1-methyl-1-pyrrolidinio) methyl] -3-cepem-4-carboxylic acid salt. The crystalline orthophosphate addition salt of claim 1 and a hydrate thereof. Next 7- [of crystalline phase with X-ray powder diffraction model -(2-aminothiazol-4-yl)- Phosphate of-(Z) -methoxyimino acetamido] -3-[(1-methylpyrrolidinio) -methyl] -3-cepem-4-carboxylic acid salt. ※ Note: The disclosure is based on the initial application.