Preparation method of cefuroxime sodium

A technology of cefuroxime sodium and cefuroxime acid, which is applied in the fields of organic chemistry and antibacterial drugs, can solve the problems of slow dissolving speed of cefuroxime sodium, increase of impurities and side reactions, increase of stirring time, etc., and achieve clinical benefit The effect of safe medication, convenient clinical use, and mild reaction conditions

Inactive Publication Date: 2011-01-26
上海新先锋药业有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0007] But, the synthetic method of various cefuroxime sodium disclosed at present, although the synthetic method is not complicated, the yield of product is higher; But, according to conventional method, the dissolving speed of synthetic cefuroxime sodium is slow
For cefuroxime sodium with a slow dissolution rate, during the production process, it is necessary to increase the dissolution temperature or increase the stirring time, thereby increasing the probability of impurities and side reactions; in addition, the powder made of cefuroxime sodium with a slow dissolution rate Injection preparations, in clinical application, a longer dissolution time will increase the labor of medical staff, and also increase the possibility of oxidation, impurities and adverse reactions in the prepared injection

Method used

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  • Preparation method of cefuroxime sodium

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Effect test

Embodiment 1

[0027] A preparation method of cefuroxime sodium, comprising the steps of:

[0028] In the first step, add 250ml of methanol, 39.5g of sodium isooctanoate and 50% sodium lactate aqueous solution containing 0.27g of sodium lactate into a three-necked bottle, and stir until the sodium isooctanoate is completely dissolved to obtain a sodium solution.

[0029] In the second step, add 400ml of acetone, 50ml of purified water and 50.9g of cefuroxime acid to another three-necked bottle, raise the temperature to 25-26°C, stir to completely dissolve the cefuroxime acid; then add 5g of activated carbon, stir to decolorize, Filter to obtain cefuroxime acid filtrate.

[0030] In the third step, slowly add the cefuroxime acid filtrate into the sodium solution at room temperature, stir to form a precipitate, stir for 30 minutes, and filter to obtain a wet product of cefuroxime sodium.

[0031] In the fourth step, the wet product of cefuroxime sodium was washed twice with a mixture of 200ml...

Embodiment 2

[0034] A preparation method of cefuroxime sodium, comprising the steps of:

[0035] In the first step, add 200ml of absolute ethanol, 0.53g of sodium isooctanoate and 70% sodium lactate aqueous solution containing 35.5g of sodium lactate into a three-necked bottle, and stir until the sodium isooctanoate is completely dissolved to obtain a sodium solution.

[0036] In the second step, add 270ml of acetone, 30ml of purified water and 135.8g of cefuroxime acid to another three-necked bottle, raise the temperature to 34-35°C, and stir to completely dissolve the cefuroxime acid; then add 8g of activated carbon, stir to decolorize, Filter to obtain cefuroxime acid filtrate.

[0037] In the third step, the temperature of the sodium solution is controlled at 28-30° C., and the cefuroxime acid filtrate is slowly added to the sodium solution, stirred to form a precipitate, stirred for 45 minutes, and filtered to obtain a wet product of cefuroxime sodium.

[0038] In the fourth step, th...

Embodiment 3

[0041] A preparation method of cefuroxime sodium, comprising the steps of:

[0042] In the first step, add 180ml of absolute ethanol, 14g of sodium isooctanoate and 70% sodium lactate aqueous solution containing 27g of sodium lactate into a three-necked bottle, and stir until the sodium isooctanoate is completely dissolved to obtain a sodium solution.

[0043] In the second step, add 240ml of acetone, 35ml of purified water and 38g of cefuroxime acid to another three-necked bottle, raise the temperature to 30-31°C, and stir to completely dissolve the cefuroxime acid; then add 5g of activated carbon, stir to decolorize, and filter , to obtain cefuroxime acid filtrate.

[0044] In the third step, the temperature of the sodium solution is controlled at 39-40°C, and the cefuroxime acid filtrate is slowly added to the sodium solution, stirred to form a precipitate, cooled to room temperature while stirring, and filtered to obtain a wet product of cefuroxime sodium.

[0045] In the...

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Abstract

The invention discloses a preparation method of cefuroxime sodium, comprising the following steps of: 1, adding anhydrous methanol or alcohol, an aqueous solution of sodium lactate and sodium iso-octoate to a vessel to obtain sodium liquid; 2, adding acetone, water and cefuroxime acid to the other vessel, and then adding active carbon for stirring, decoloring and filtering to obtain filtrate of cefuroxime acid; 3, adding the filtrate of cefuroxime acid to the sodium liquid, wherein the amount of the sodium liquid is not less than that of the cefuroxime acid, stirring the mixture of the filtrate and the sodium liquid to generate sedimentation, and filtering to obtain a wet product of cefuroxime sodium; 4, washing the wet product with a methanol / acetone mixed liquid or anhydrous alcohol / acetone mixed liquid, and then washing the wet product with a solution of acetone, and drying to obtain the product of the cefuroxime sodium. In the invention, the prepared product of the cefuroxime sodium has high purity; the operation is simple and convenient; the reaction condition is gentle; in addition, the invention is suitable for industrial production, and can be carried out under the aseptic condition and can be used for preparing the aseptic product of the cefuroxime sodium.

Description

technical field [0001] The invention relates to a preparation method of cefuroxime sodium, belonging to the field of drug synthesis. Background technique [0002] Cefuroxime sodium, the molecular formula is C 16 h 15 N 4 NaO 8 S, chemical name (6R, 7R)-7-[2-furyl(methoxyimino)acetamido]-3-carbamoyloxymethyl-8-oxo-5-thia-1-aza Bicyclo[4.2.0]oct-2-ene-2-carboxylic acid sodium salt. The structural formula is as follows: [0003] [0004] Cefuroxime sodium is a second-generation cephalosporin antibiotic. The antibacterial activity against Gram-positive cocci is similar to or slightly worse than that of the first-generation cephalosporins, but it is quite stable against β-lactamases produced by Staphylococci and Gram-negative bacilli. Methicillin-resistant Staphylococcus, Enterococcus and Listeria are drug-resistant, and other positive cocci (including anaerobic cocci) are sensitive to this product. It can be used for respiratory tract infection caused by sensitive bac...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/34C07D501/04A61P31/04
Inventor 郑玉林李建文管海英薛明辉秦健
Owner 上海新先锋药业有限公司
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