Cefamandole nafate compound and pharmaceutical composition thereof

A technology of cefamandole sodium and its compounds, applied in the field of medicine, can solve the problems of unstable crystal water, many insoluble particles, and decreased stability, and achieve the effect of reducing insoluble particles, less insoluble particles, and high stability

Active Publication Date: 2013-04-17
HUNAN KELUN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0004] In the above-mentioned technical scheme, Chinese patent ZL201010257886.X and Chinese patent ZL201010199235.X are both prepared into hydrates of cefamandole sodium, but substances containing crystal water often have the defect that the crystal water is unstable during the preparation process, such as The stability of the long-term test and accelerated test of Chinese patent ZL201010257886.X decreased significantly, and sodium benzoate was added to the preparation claimed by Chinese patent ZL201010199235.X, and sodium benzoate, as a preservative, has potential safety hazards and has been banned in some countries
Although the compound of cefamandole sodium disclosed in Chinese application 201210284600.6 has higher stability, because it does not solve the problem of solubility, there are many insoluble particles, and a large amount of sodium carbonate (100g cefamandole) is still added in the preparation Add 18~20g sodium carbonate to sodium ester), or add lidocaine, reduced glutathione and sodium glutamate, and both lidocaine and reduced glutathione are active drugs, together There are uncertain security risks in the use of

Method used

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  • Cefamandole nafate compound and pharmaceutical composition thereof
  • Cefamandole nafate compound and pharmaceutical composition thereof
  • Cefamandole nafate compound and pharmaceutical composition thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0024] The preparation of embodiment 1 cefamandole sodium compound

[0025] At 20°C, dissolve 200 g of cefamandole sodium in a mixed solution of 1000 g of water and methanol (volume ratio 10:1), add 8 g of activated carbon, stir for 20 minutes, filter to remove carbon, and filter the filtrate through a 0.22 μm filter membrane; 28 ℃, at a stirring speed of 200 rpm, slowly (20ml / min) add 100g methanol to the filtrate while stirring, and stir for 30 minutes; at 20℃, at a stirring speed of 100 rpm, slowly (10ml / min) while stirring min) Add 12,000g of a mixed solution of ethanol and isopropanol (volume ratio 5:1), cool down to 0°C at a constant rate of 1°C / min, let stand for 12 hours, filter, and use 3 times the weight of the filter cake with a volume ratio of 5: Wash twice with a mixed solution of ethanol and isopropanol in 1, and dry in vacuum at 35°C for 6 hours to obtain the cefamandole sodium compound with a melting point of 205-210°C. X-ray powder diffraction pattern see at...

Embodiment 2

[0026] The preparation of embodiment 2 cefamandole sodium compound

[0027] At 25°C, dissolve 200 g of cefamandole sodium in a mixed solution of 1600 g of water and methanol (volume ratio 10:1), add 8 g of activated carbon, stir for 20 minutes, filter to remove carbon, and filter the filtrate through a 0.22 μm filter membrane; 30 ℃, at a stirring speed of 250 rpm, slowly (30ml / min) add 160g methanol to the filtrate while stirring, and stir for 30 minutes; at 22℃, at a stirring speed of 150 rpm, slowly (20ml / min) min) Add 24,000g of a mixed solution of ethanol and isopropanol (volume ratio 5:1), cool down to 2°C at a constant speed of 0.8°C / min, let stand for 12 hours, filter, and use 3 times the weight of the filter cake with a volume ratio of 5: Wash twice with a mixed solution of ethanol and isopropanol in 1, and dry in vacuum at 40°C for 6 hours to obtain the cefamandole sodium compound with a melting point of 205-210°C. The X-ray powder diffraction pattern is consistent w...

Embodiment 3

[0028] Example 3 Preparation of Cefamandole Sodium Powder for Injection

[0029] Precisely weigh 80g of the cefamandole sodium compound under 100-grade aseptic conditions, pass through a 120-mesh sieve, and carry out aseptic sub-packaging according to the loading requirements, and the loading volume of each bottle is 0.5g.

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Abstract

The invention relates to a cefamandole nafate compound and a pharmaceutical composition of the cefamandole nafate compound. The cefamandole nafate compound is crystal, and is determined by X-ray powder diffraction, and the characteristic peak in an atlas is shown as 8.8 degrees, 9.5 degrees, 10.2 degrees, 11.3 degrees, 12.0 degrees, 14.4 degrees, 16.8 degrees, 17.3 degrees, 20.6 degrees, 25.0 degrees, 27.8 degrees, 28.1 degrees and 30.2 degrees in a range of 20+/0.2 degrees. The pharmaceutical composition of the cefamandole nafate compound is a preparation and a pharmaceutical composition preparation containing the above cefamandole nafate compound and the preparation is powder-injection. The cefamandole nafate crystalline compound is high in stability and few in insoluble particles; a cosolvent is not needed, so that the compound can be directly and aseptically sub-packaged to obtain cefamandole nafate powder injection for injection. The cefamandole nafate crystalline compound is also fully mixed with aseptic sodium carbonate powder to be aseptically sub-packaged. The number of insoluble particles added with the powder injection of sodium carbonate is few on the basis of reaching standard request.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to a cefamandole sodium compound and a pharmaceutical composition thereof. Background technique [0002] Cefamandole sodium chemical name 7-D-(2-formyloxyphenylacetamide)-3-[(1-methyl-1H-tetrazol-5-yl)thiomethyl]-8-oxo- 5-Thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid sodium salt, is a second-generation cephalosporin, in addition to having the same effect as cefazolin, it is also effective against some Gram-negative bacteria Has antibacterial effect. The antibacterial spectrum is similar to that of cefotaxime, but it is not as good as cefotaxime against Gram-positive cocci. The main feature of this product is that it has a strong effect on Gram-negative bacteria, which is better than cefazolin. It has a strong effect on anaerobic Clostridium, meningococcus, Neisseria gonorrhoeae, Escherichia coli, Klebsiella pneumoniae, influenza bacillus and indole-positive proteus, especial...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/36C07D501/12A61K31/546A61K9/14A61P31/04
Inventor 胡成忠李美林
Owner HUNAN KELUN PHARMA
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