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Cefepime dihydrochloride compound and pharmaceutical composition thereof

A technology of cefepime hydrochloride and compounds, which is applied in antibacterial drugs, organic chemistry, and pharmaceutical formulations, can solve the problems of low product purity, increased impurities, and decreased content, and achieve high yield, simple process, and low cost. Effect

Active Publication Date: 2015-05-13
YOUCARE PHARMA GROUP
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Cefepime is a thermally unstable and highly water-soluble neutral internal salt. Cefepime has carboxyl negative ions, which combine with protons in the aqueous solution to promote the ionization balance of water to generate more alkaline ions and make the solution It is weakly alkaline, but it is prone to degradation and ring-opening reactions under weakly alkaline conditions, resulting in a decrease in content, increased impurities, low yield, and low product purity

Method used

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  • Cefepime dihydrochloride compound and pharmaceutical composition thereof
  • Cefepime dihydrochloride compound and pharmaceutical composition thereof
  • Cefepime dihydrochloride compound and pharmaceutical composition thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] A cefepime hydrochloride compound prepared by the following method:

[0027] (1), 100g of cefepime hydrochloride crude product (purity 83.2%) was dissolved in 1500ml of water, and a separation membrane with a molecular weight cut-off of 500-3000 was selected, and the aromatic polyamide membrane was separated and removed under the operating pressure condition of 0.3MPa;

[0028] (2), the cefepime hydrochloride solution of step (1) was added to 1000ml of a mixed solvent of cyclohexane and acetonitrile with a volume ratio of 1:2, 7.5g of activated carbon was added to the resulting solution, and the temperature was kept at 45°C and stirred for 30min , filter and decarbonize, and collect the filtrate;

[0029] (3), the filtrate of step (2) is carried out chromatographic column separation and purification; The condition of described chromatographic column separation and purification is: mobile phase is the mixed solvent of isopropanol and acetonitrile of volume ratio 1: 3, an...

Embodiment 2

[0040] A cefepime hydrochloride compound prepared by the following method:

[0041] (1), 100g of cefepime hydrochloride crude product (purity 82.4%) was dissolved in 1500ml of water, and a separation membrane with a molecular weight cut-off of 500-3000 was selected, and the sulfonated polysulfone membrane was separated and removed under the operating pressure condition of 0.1MPa;

[0042] (2), the cefepime hydrochloride solution of step (1) was added to 1000ml of a mixed solvent of cyclohexane and acetonitrile with a volume ratio of 1:2, 2.5g of activated carbon was added to the resulting solution, and the temperature was kept at 40°C and stirred for 20min , filter and decarbonize, and collect the filtrate;

[0043] (3), the filtrate of step (2) is carried out chromatographic column separation and purification; The condition of described chromatographic column separation and purification is: mobile phase is the mixed solvent of isopropanol and acetonitrile of volume ratio 2:5,...

Embodiment 3

[0054] A cefepime hydrochloride compound prepared by the following method:

[0055] (1), 100g cefepime hydrochloride crude product (purity 81.7%) is dissolved in 1500ml water, select the separation membrane that molecular weight cut off is 500~3000 for use, under 0.5MPa operating pressure condition, polysulfone membrane separates and removes impurities;

[0056] (2), the cefepime hydrochloride solution of step (1) is added to 1000ml volume ratio is in the mixed solvent of cyclohexane and acetonitrile of 1:2, the gac of 10g is added in the gained solution, is incubated at 50 ℃ and stirred for 25min, Filter and decarbonize, collect the filtrate;

[0057] (3), the filtrate of step (2) is carried out chromatographic column separation and purification; The condition of described chromatographic column separation and purification is: mobile phase is the mixed solvent of isopropanol and acetonitrile of volume ratio 1: 4, and stationary phase filler is aluminum oxide , the flow rate ...

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Abstract

The invention discloses a cefepime dihydrochloride compound. The cefepime dihydrochloride compound is prepared by a following method comprising the following steps: (1) dissolving a cefepime dihydrochloride crude product into water and performing membrane separation and impurity removal by selecting a separating membrane with the molecular weight cut off of 500-3000; (2) adding the impurity-removed solution into an organic solvent, then adding active carbon into the obtained solution, stirring, filtering the solution to remove charcoal, and collecting the filter solution; (3) separating and purifying the filter solution with a chromatographic column, wherein a mobile phase is a mixed solvent of isopropanol and acetonitrile, and a stationary phase filler is silica gel or aluminum oxide; and (4) concentrating the separated and purified filter solution, and performing spray-drying to obtain the cefepime dihydrochloride compound. The invention also discloses a pharmaceutical composition containing the cefepime dihydrochloride compound, wherein the pharmaceutical composition is sterile powder for injection. The cefepime dihydrochloride compound and the pharmaceutical composition disclosed by the invention have low impurity content and few toxic and side effects, so that the medication safety of the patient is greatly improved.

Description

technical field [0001] The invention relates to a cefepime hydrochloride compound and a pharmaceutical composition thereof, belonging to the technical field of medicinal chemistry. Background technique [0002] Cefepime is a broad-spectrum fourth-generation cephalosporin that achieves bactericidal effect by inhibiting the biosynthesis of bacterial cell walls. In vitro tests have shown that it has effects on both Gram-positive and Gram-negative bacteria. This product has a low affinity to the β-lactamase encoded by the bacterial chromosome, can be highly resistant to the hydrolysis of most β-lactamases, and can quickly penetrate into the cells of Gram-negative bacteria. In bacterial cells, its target molecule is penicillin-binding protein (PBP). Molecular formula: C 19 h 25 ClN 6 o 5 S 2 ·HCl·H 2 O, white or off-white powder; slightly smelly, tasteless. [0003] Cefepime is a thermally unstable and highly water-soluble neutral internal salt. Cefepime has carboxyl neg...

Claims

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Application Information

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IPC IPC(8): C07D501/46C07D501/12A61K31/546A61P31/04
Inventor 李琦杨磊
Owner YOUCARE PHARMA GROUP
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