Cefuroxime sodium compound containing 1/2 of water

A technology of cefuroxime sodium and furoxin sodium, which is applied in organic chemistry, antibacterial drugs, organic active ingredients, etc., can solve the problems of low thermal decomposition temperature, poor fluidity, and unclearness, and achieve wide application prospects and thermal stability Good performance and fast drying effect

Inactive Publication Date: 2019-01-04
陕西顿斯制药有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Cefuroxime sodium has poor stability and needs to be sealed and refrigerated at 2-8°C. Improper storage or transportation is prone to solid color deepening. When tested according to pharmacopoeia standards, the color of the solution often fails.
[0006] The cefuroxime sodium product currently used clinically is an anhydrous substance. Due to the influence o

Method used

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  • Cefuroxime sodium compound containing 1/2 of water
  • Cefuroxime sodium compound containing 1/2 of water
  • Cefuroxime sodium compound containing 1/2 of water

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The preparation of embodiment 1 1 / 2 cefuroxime sodium compound

[0033] (1) At room temperature, 848.8 g of cefuroxime acid and 272.2 g of sodium acetate were added to a mixed solution of water (2 L) and ethanol (2 L), stirred at 150 rpm, and reacted for 2 hours to obtain cefuroxime sodium solution;

[0034] (2) Add 10 g of seed crystals to the above cefuroxime sodium solution, lower the temperature to -5°C, slowly add ethanol, stir and crystallize at 150 rpm, and filter;

[0035] (3) Dissolve the above filtrate in 2L of water, add 1g of activated carbon, stir and adsorb for 30min, filter, slowly add 3L of ethanol to the filtrate, lower the temperature to -5°C, stir and crystallize at 150rpm for 1h, filter; wash the filtrate with ethanol, Vacuum drying at 40°C for 1 hour yielded 846.3 g of the 1 / 2 water cefuroxime sodium compound.

[0036] Test results:

[0037] The X-ray powder diffraction pattern has characteristic diffraction peaks at the diffraction angle 2θ of 10...

Embodiment 2

[0040] The preparation of embodiment 2 1 / 2 cefuroxime sodium compound

[0041] (1) At room temperature, 849.6 g of cefuroxime acid and 274.1 g of sodium acetate were added to a mixed solution of water (2 L) and methanol (2.5 L), stirred at 500 rpm, and reacted for 2 hours to obtain cefuroxime sodium solution;

[0042] (2) Add 10 g of seed crystals to the above-mentioned cefuroxime sodium solution, lower the temperature to 0° C., slowly add 2 L of methanol, stir and crystallize at 500 rpm, and filter;

[0043] (3) Dissolve the above filtrate in 3L of water, add 1.5g of activated carbon, stir and adsorb for 30min, filter, slowly add 3L of methanol to the filtrate, lower the temperature to 0°C, stir and crystallize at 500rpm for 1h, filter; wash the filtrate with methanol, Vacuum drying at 40°C for 1 hour gave 851.1 g of the 1 / 2 water cefuroxime sodium compound.

[0044] Test results:

[0045] The X-ray powder diffraction pattern has characteristic peaks at diffraction angles 2...

Embodiment 3

[0048] Example 3 Preparation of 1 / 2 cefuroxime sodium compound

[0049] (1) At room temperature, add 906.2 g of cefuroxime acid and 285.3 g of sodium acetate into a mixed solution of water (2 L) and ethyl acetate (2 L), stir at 300 rpm, and react for 1 hour to obtain cefuroxime sodium solution;

[0050] (2) Add 10 g of seed crystals to the above-mentioned cefuroxime sodium solution, lower the temperature to -1 ° C, slowly add 2 L of ethyl acetate, stir and crystallize at 300 rpm, and filter;

[0051] (3) Dissolve the above filtrate in 2L of water, add 2g of activated carbon, stir and absorb for 30min, filter, slowly add 3L of ethyl acetate to the filtrate, lower the temperature to -1°C, stir and crystallize at 300rpm for 1h, and filter; The filtrate was washed and vacuum-dried at 40° C. for 1 hour to obtain 877.5 g of 1 / 2 cefuroxime sodium compound.

[0052] Test results:

[0053] The X-ray powder diffraction pattern has characteristic peaks at the diffraction angle 2θ of 10...

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PUM

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Abstract

The invention discloses a cefuroxime sodium compound containing 1/2 of water. Each mole of cefuroxime sodium contains 1/2 mole of water. The cefuroxime sodium compound containing 1/2 of water preparedby the method has the significant advantages of having good thermal stability and good mobility and not absorbing moisture easily, and meets the requirements for serving as a preparation raw material.

Description

technical field [0001] The invention belongs to the technical field of crystallization of chemical engineering medicines, and in particular relates to a 1 / 2 cefuroxime sodium compound and a preparation method thereof. Background technique [0002] Cefuroxime sodium, English name Cefuroxime Sodium, also known as cefuroxime, cefuroxime, Chinese nickname: (6R, 7R)-7-[2-furyl (methoxyimino) acetamido]-3-aminomethyl Sodium acyloxymethyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate, molecular weight: 446.37, molecular formula: C 16 h 15 N 4 NaO 8 S. [0003] Cefuroxime sodium is white, off-white or light yellow powder or crystalline powder; odorless, bitter taste; hygroscopic, easily soluble in water, slightly soluble in methanol, insoluble in ethanol or chloroform, and contains in every 1ml In a 10 mg solution, the specific rotation is +55° to +65°; the absorbance is measured at a wavelength of 274nm by spectrophotometry, and the absorption coefficient (E1cm1%) is...

Claims

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Application Information

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IPC IPC(8): C07D501/34C07D501/12C07D501/04A61K31/546A61P31/04
Inventor 黄奋
Owner 陕西顿斯制药有限公司
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