Cefuroxime sodium compound and new preparation method thereof

A technology for ceftizoxime sodium and ceftizoxime acid, which is applied in the field of medicine, can solve the problems of difficult-to-high-purity and high-yield compounds, excessive consumption of activated carbon, poor reproducibility, etc., and achieves improved purity and content, low cost, The effect of mild reaction conditions

Inactive Publication Date: 2011-06-01
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] CN101348492A discloses a method for preparing high-purity ceftizoxime or its salt, which comprises the steps of: (1) converting the aqueous solution of ceftizoxime or its salt crude product into ceftizoxime acid under acidic conditions; (2) using Organic solvent extraction step (1) obtains ceftizoxime acid crude product; (3) uses aluminum oxide as the filler of chromatographic column, with the mixed solution of hydrocarbon solvent and chlorinated solvent as eluent, to step (2) gained ceftizole Carrying out chromatographic separation of the crude product of oxamic acid, collecting fractions with a ceftizoxime acid content of not less than 80%; (4) removing the solvent in the fraction of ceftizoxamic acid obtained in step (3), and then adding a lower alkyl alcohol solvent Dissolving, adding alkali to precipitation; (5) recrystallizing the precipitate obtained in step (4) with a lower alkyl alcohol solvent to obtain high-purity ceftizoxime or its salt. This method is relatively complicated, and the yield is not high. poor performance
[0011] CN101606910A discloses a method for synthesizing t

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  • Cefuroxime sodium compound and new preparation method thereof
  • Cefuroxime sodium compound and new preparation method thereof
  • Cefuroxime sodium compound and new preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Example 1 Purification of Ceftizoxime Sodium Compound

[0033] (1) Dissolve 100 g of ceftizoxime sodium crude product with a purity of 95.8% in 1000 ml of purified water, slowly add 3% acetic acid solution until the pH of the solution is 3, stir, leave to cool, produce precipitation, filter to obtain ceftizoxime acid ;

[0034] (2) Dissolve ceftizoxime acid in 800ml of isopropanol and isopropyl ether in a mixed solvent of 1:3, add 0.8g of activated carbon, stir at 50°C for 20min, filter for decarburization, and collect the filtrate;

[0035] (3) The filtrate obtained in the previous step is evaporated under reduced pressure, and the preparation chromatographic column is utilized to carry out separation and purification, and the mixed solvent of water and acetonitrile with a volume ratio of 1: 3 is the mobile phase, and the stationary phase filler is silica gel, and the flow rate is 2.8ml / min , the column temperature is 40°C; the fractions are collected in sections, ...

Embodiment 2

[0037] Example 2 Purification of Ceftizoxime Sodium Compound

[0038] (1) Dissolve 100 g of ceftizoxime sodium crude product with a purity of 95.8% in 1000 ml of purified water, slowly add 5% citric acid solution until the pH of the solution is 2.0, stir, leave to cool, produce precipitation, filter to obtain ceftizoxime acid;

[0039] (2) Dissolve ceftizoxime acid in 800ml of isopropanol and isopropyl ether 1:3 mixed solvent, add 2.4g of activated carbon, stir at 40°C for 30min, filter for decarburization, and collect the filtrate;

[0040] (3) The filtrate obtained in the previous step is evaporated under reduced pressure, and the preparation chromatographic column is utilized to carry out separation and purification, and the mixed solvent of water and acetonitrile with a volume ratio of 1: 3 is the mobile phase, and the stationary phase filler is silica gel, and the flow rate is 4.5ml / min , the column temperature is 30°C; the fractions are collected in sections, and th...

Embodiment 3

[0042] Example 3 Purification of Ceftizoxime Sodium Compound

[0043] (1) 100g of 95.8% pure ceftizoxime sodium crude product is dissolved in 1200ml of purified water, slowly add 7% oxalic acid solution until the pH of the solution is 4.0, stir, leave to cool, produce precipitation, filter to obtain ceftizole oxime acid;

[0044] (2) Dissolve ceftizoxime acid in 800ml of isopropanol and isopropyl ether in a 1:3 mixed solvent, add 1.6g of activated carbon, stir at 40°C for 20min, filter for decarburization, and collect the filtrate;

[0045] (3) The filtrate obtained in the previous step is evaporated under reduced pressure, and the preparation chromatographic column is utilized to carry out separation and purification, and the mixed solvent of water and acetonitrile with a volume ratio of 1: 3 is the mobile phase, and the stationary phase filler is silica gel, and the flow rate is 3.5ml / min , the column temperature is 30°C; the fractions are collected in sections, and the...

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Abstract

The invention provides a cefuroxime sodium compound and a new preparation method thereof. The method comprises the following steps: performing acid-base reaction, absorbing with activated carbon, and separating and purifying with a chromatographic column. By adopting the method, the purity and content of cefuroxime sodium can be greatly increased, the product quality of the preparation can be increased, the toxic or side effects can be reduced and the safety of the preparations of the medicines for curing respiratory tract infection and urinary tract infection can be ensured; and compared with the prior art, the method has the advantages of simple and practical technology, mild reaction conditions, low cost, high yield and high product purity and is suitable for industrial production.

Description

technical field [0001] The invention relates to a ceftizoxime sodium compound and a new method thereof, belonging to the technical field of medicine. Background technique [0002] Ceftizoxime sodium belongs to the third-generation cephalosporins, which has a spectrum antibacterial effect and is stable to the spectrum β-lactamase (including penicillinase and cephalosporinase) produced by various Gram-positive and Gram-negative bacteria. Ceftizoxime sodium has a strong antibacterial effect on Escherichia coli, Klebsiella pneumoniae, Proteus mirabilis and other enterobacteria, and has a good antibacterial effect on Haemophilus influenzae and Neisseria gonorrhoeae. Ceftizoxime sodium achieves bactericidal effect by inhibiting the biosynthesis of bacterial cell wall mucopeptides. At present, ceftizoxime sodium is mainly used clinically for the treatment of lower respiratory tract infection, urinary tract infection, abdominal infection, pelvic infection, sepsis, skin and soft tis...

Claims

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Application Information

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IPC IPC(8): C07D501/20C07D501/04C07D501/12A61P31/04A61P11/00A61P13/02
Inventor 郝志艳
Owner HAINAN LINGKANG PHARMA CO LTD
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