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Preparation method of low-moisture and high-stability sterile cefuroxime sodium

A cefuroxime sodium and high stability technology, which is applied in the field of drug synthesis, can solve the problems of long drying time, unstable quality, and difficult to achieve, and achieve the effects of improving equipment production capacity, reducing production costs, and improving stability

Inactive Publication Date: 2013-04-17
潘行远
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] Due to the addition of water in the above original process, there is residual water in the crystals of cefuroxime sodium, causing the crystals of cefuroxime sodium to be soft and easy to stick. Do not stir when drying in the tank (because stirring can cause the crystal form to break and stick), only when the solvent is dried under static reduced pressure and the water is low, can intermittent and slow stirring be performed. The drying time is very long, about 15-25 hours
The obtained cefuroxime sodium product has many hard lumps, is not easy to crush, and is easy to generate heat when crushed, causing burning powder, affecting product color, clarity, color point and other quality problems
The moisture of the obtained cefuroxime sodium is 2.5-3.0%, and the residual solvent is more than 0.3%. No matter how long the drying time is, the moisture is difficult to reach below 2.5%, and the residual solvent is difficult to be less than 0.3%, resulting in unsatisfactory product stability.
The moisture content of amorphous cefuroxime sodium obtained by freeze-drying is difficult to reach below 2.0%. Due to the large surface area of ​​amorphous cefuroxime sodium, the quality is extremely unstable, and there is no freeze-dried cefuroxime sodium product on the market so far
The cefuroxime sodium produced by the existing technology must be stored in cold storage, which causes troubles in the circulation and use of the product

Method used

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  • Preparation method of low-moisture and high-stability sterile cefuroxime sodium

Examples

Experimental program
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Effect test

Embodiment 1

[0030] 1. Add 100Kg of cefuroxime acid, 900L of anhydrous acetone, and 800L of absolute ethanol into a 1500L dissolving tank, stir and dissolve at a temperature of 20 degrees, then add 10Kg of activated carbon, decolorize for 30 minutes, decarbonize, filter aseptically, and filter to no Bacteria crystallization tank.

[0031] 2. In the sodium-alkali solution decolorization tank, add 120L absolute ethanol, 40Kg sodium isooctanoate, and 5Kg activated carbon at a temperature of 20 degrees and stir for 20 minutes to decolorize. After decarburization and sterile filtration, filter the liquid into a sterile metering tank.

[0032] 3. Stir at a slow speed at a temperature of 28-30 degrees, and control the stirring speed at 20-40r / min. Add the sodium-alkali solution dropwise into the crystallization tank. After about 50 minutes, the crystallization precipitates, and then slowly add 300L sterile-filtered Anhydrous acetone, stirred for 30min.

[0033] 4. The crystallization is hydrauli...

Embodiment 2

[0036] 1. Add 100Kg of cefuroxime acid, 1000L of anhydrous acetone, and 300L of anhydrous methanol into a 1500L dissolving tank, stir and dissolve at a temperature of 20 degrees, then add 10Kg of activated carbon, decolorize for 30 minutes, decarbonize, filter aseptically, and filter to no Bacteria crystallization tank.

[0037] 2. Add 80L of anhydrous methanol, 25Kg of sodium acetate trihydrate, and 5Kg of activated carbon to the sodium-alkali solution decolorization tank at a temperature of 20 degrees and stir for 20 minutes to decolorize. After decarburization and sterile filtration, filter the liquid into a sterile metering tank.

[0038] 3. With temperature controlled at 23-25°C and stirring at a slow speed, add the sodium-alkali solution dropwise into the crystallization tank for about 20 minutes, and then crystallize, then slowly add 700L sterile-filtered anhydrous acetone and stir for 30 minutes.

[0039] 4. The crystallization is hydraulically filtered into a three-in...

Embodiment 3

[0042] 1. Add 100Kg of cefuroxime acid, 800L of anhydrous acetone, and 700L of absolute ethanol into a 1500L dissolving tank, stir and dissolve at a temperature of 20 degrees, then add 10Kg of activated carbon, decolorize for 30 minutes, and decarbonize and filter aseptically until the liquid pressure reaches zero. Bacteria crystallization tank.

[0043] 2. In the sodium-alkali solution decolorization tank, add 120L absolute ethanol, 35Kg sodium isooctanoate, 5Kg activated carbon at a temperature of 20°C and stir for 20 minutes to decolorize. After decarburization and sterile filtration, filter the liquid into a sterile metering tank.

[0044] 3. With temperature controlled at 25-30°C and stirring at a slow speed, add the sodium-alkali solution dropwise into the crystallization tank for about 30 minutes, and then crystallize, then slowly add 900L sterile-filtered anhydrous acetone and stir for 30 minutes.

[0045] 4. The crystallization is hydraulically filtered into a three-i...

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Abstract

The invention discloses a preparation method of low-moisture and high-stability sterile cefuroxime sodium, which comprises the steps of (a) dissolving cefuroxime acid in an anhydrous mixed solvent, decolorizing, conducting sterile filtration, collecting filter liquor to a crystallizing tank, (b) dissolving soda in an organic solvent, decolorizing, conducting the sterile filtration, collecting filter liquor to a sodium solution metering tank, (c) controlling temperature for 10-50min, adding a soda solution into the crystallizing tank dropwise, controlling a stirring rate at 20-60r / min, crystallizing, adding acetone after the sterile filtration to ensure full crystallizing; (d) pressing crystallized liquid in a three-in-one multifunctional tank for filtration, washing with the mixed solvent, drying at 30-60 DEG C, obtaining the sterile cefuroxime sodium, and (e) transferring materials in a sterile bicone at 30-70 DEG C, continuing to dry under reduced pressure for 2-5h, and obtaining the sterile cefuroxime sodium with better stability and the moisture less than 1%. The preparation method is short in drying time and simple and practicable, the sterile cefuroxime sodium is easy to smash, low in moisture, less in solvent residual and stable in quality, the color, clarity and color points of the sterile cefuroxime sodium are not affected, and the production cost is lowered.

Description

[0001] Technical field: [0002] The invention relates to a method for preparing sterile cephalosporin antibiotics, in particular to a method for preparing sterile cefuroxime sodium with low water content and high stability, and belongs to the technical field of drug synthesis. Background technique: [0003] Cefuroxime sodium is a second-generation cephalosporin antibiotic drug, and its broad-spectrum antibacterial effect on Gram-positive bacteria is lower than or close to that of the first-generation cephalosporins. Gram-negative Haemophilus influenzae, Neisseria gonorrhoeae, Meningococcus, Escherichia coli, Klebsiella, Proteus mirabilis, Enterobacter, Citrobacter, Salmonella, Shigella, and certain indoles Positive Proteus bacteria were sensitive to cefuroxime sodium. Cefuroxime sodium has good resistance to the β-lactamase of Gram-negative bacteria, and it is also effective against ampicillin-resistant or first-generation cephalosporin-resistant strains of the above-m...

Claims

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Application Information

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IPC IPC(8): C07D501/34C07D501/04
Inventor 潘行远
Owner 潘行远
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