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Ceftizoxime sodium novel crystal form capable of reducing anaphylactic reactions and preparation thereof

A technology of ceftizoxime sodium and crystal, which is applied in the field of injection powder for injection comprising a new crystal form of ceftizoxime sodium and its preparation, and can solve the problems that affect the application of ceftizoxime or its salt, are not suitable for industrialized production, and are complicated to operate. problems, to achieve the effect of improving product stability and drug safety, improving bioavailability, and low residues

Active Publication Date: 2016-06-01
福安药业集团庆余堂制药有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Most ceftizoxime sodium raw materials have problems such as low purity, poor clarity after dissolution, poor stability in aqueous solution, and relatively large side effects.
Thereby, have had a strong impact on the application of ceftizoxime or its salt
[0005] Chinese patent CN101348492A discloses a method for preparing high-purity ceftizoxime sodium. It is intended to convert ceftizoxime sodium into ceftizoxime acid in water, extract the crude product of ceftizoxime acid with an organic reagent, and use an aluminum peroxide chromatography column to remove the resulting The solvent in the mobile phase is dissolved by adding a lower alcohol, and the product is extracted by adding alkali. This method uses an alumina chromatography column, and a large amount of eluent is used, which is costly, pollutes the environment, and is complicated to operate. It is not suitable for industrial production.
The ceftizoxime sodium crystalline hydrate has good storage stability, but the method uses chloroform, dichloromethane and other solvents

Method used

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  • Ceftizoxime sodium novel crystal form capable of reducing anaphylactic reactions and preparation thereof
  • Ceftizoxime sodium novel crystal form capable of reducing anaphylactic reactions and preparation thereof
  • Ceftizoxime sodium novel crystal form capable of reducing anaphylactic reactions and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Dissolve 100 g of the crude product of ceftizoxime sodium in water, control the pH value of the solution to 6.5, and the temperature at 25 ° C, and add dropwise a mixed solvent of isopropanol and tetrahydrofuran (volume ratio 2:1) to the solution under stirring until the solution is cloudy, and the stirring speed is 250 rev / min, the rate of addition is 300ml / h; the temperature is raised to 50°C, and the crystal is left to grow for 3 hours; absolute ethanol is added dropwise under stirring, the stirring speed is 100 rev / min, and the temperature is slowly cooled to 25°C; the rate of addition is 80ml / h, after the dropwise addition, let stand for 2 hours; continue to lower the temperature to 10°C under stirring, let stand for 1 hour; filter, wash with absolute ethanol 3 times, and vacuum-dry at 30°C to obtain ceftizoxime sodium crystals. The particle size is 50-70 μm, the yield is 96.4%, and the HPLC content is 99.95%. The X-ray powder diffraction spectrum obtained by Cu-Kα...

Embodiment 2

[0024] Dissolve 100 g of ceftizoxime sodium crude product in water, control the pH value of the solution to 6.8 and the temperature at 30°C, and add a mixed solvent of isopropanol and tetrahydrofuran (volume ratio 1:1) to the solution dropwise under stirring until the solution is cloudy, and the stirring speed is 250 rpm, the rate of addition is 350ml / h; the temperature is raised to 50°C, and the crystal is left to grow for 3 hours; absolute ethanol is added dropwise under stirring, the stirring speed is 100 rpm, and the temperature is slowly cooled to 25°C; the rate of addition is 80ml / h, after the dropwise addition, let stand for 2 hours; continue to lower the temperature to 10°C under stirring, let stand for 1 hour; filter, wash with absolute ethanol 3 times, and vacuum-dry at 30°C to obtain ceftizoxime sodium crystals. The particle size is 50-70 μm, the yield is 95.9%, and the HPLC content is 99.96%. The X-ray powder diffraction pattern measured by Cu-Kα rays is consistent...

Embodiment 3

[0026] Dissolve 100 g of the crude product of ceftizoxime sodium in water, control the pH value of the solution to 6.3, and the temperature at 25 ° C, and add a mixed solvent of isopropanol and tetrahydrofuran (volume ratio 3:1) to the solution dropwise under stirring until the solution is cloudy, and the stirring speed is 250 rev / min, the rate of addition is 400ml / h; the temperature is raised to 50°C, and the crystal is left to grow for 4 hours; absolute ethanol is added dropwise under stirring, the stirring speed is 100 rev / min, and the temperature is slowly cooled to 25°C; the rate of addition is 80ml / h, after the dropwise addition, let stand for 2 hours; continue to cool down to 10°C under stirring, let stand for 1 hour; filter, wash with absolute ethanol 3 times, and vacuum-dry at 30°C to obtain ceftizoxime sodium crystals. The particle size is 50-70 μm, the yield is 94.6%, and the HPLC content is 99.95%. The X-ray powder diffraction pattern measured by Cu-Kα rays is cons...

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Abstract

The invention discloses a ceftizoxime sodium novel crystal form capable of reducing anaphylactic reactions, a preparation method and a pharmaceutic preparation of the ceftizoxime sodium novel crystal form. Ceftizoxime sodium is measured through an X-ray powder diffraction method, and feature diffraction peaks are displayed at the 6.8-degree position, the 11.5-degree position, the 14.6-degree position, the 15.8-degree position, the 19.4-degree position, the 20.2-degree position, the 21.8-degree position, the 24.0-degree position, the 27.4-degree position and the 30.5-degree position of an X ray powder diffraction pattern expressed by a 2 theta + / -0.2-degree diffraction angle. The content of ceftizoxime sodium compound impurities is obviously reduced compared with the prior art, and the ceftizoxime sodium novel crystal form has the advantages of being good in stability and fluidity, not prone to absorb moisture, high in dissolution speed, good in clinical effect, low in occurrence rate of adverse reactions and very suitable for clinical application.

Description

technical field [0001] The invention relates to the field of antibiotic drugs, in particular to a powder for injection containing a new crystal form of ceftizoxime sodium and a preparation method thereof. Background technique [0002] Ceftizoxime sodium, chemical name: [6R-[6a,7b(Z)]]-7[[2,3-dihydro-2-imino-4-thiazolyl)(methoxyimino)acetyl ]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid sodium salt, molecular formula C13H12N5NaO5S2, molecular weight 405.38. [0003] Ceftizoxime sodium is a third-generation cephalosporin with broad-spectrum antibacterial effect and is stable to broad-spectrum lactamase (including penicillinase and cephalosporinase) produced by various Gram-positive and Gram-negative bacteria. Enterobacteriaceae such as Escherichia coli, Klebsiella pneumoniae, and Proteus mirabilis have strong antibacterial effects, while Pseudomonas such as Pseudomonas aeruginosa and Acinetobacter are less sensitive to this product. The effect of ceftizo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/20C07D501/12A61K31/546A61P31/04A61P11/00A61P1/16A61P13/00A61P7/00A61P17/00A61P25/00A61P15/00A61P19/00
CPCA61K9/0019A61K9/19C07B2200/13C07D501/12C07D501/20
Inventor 蒋晨胡昌勤周晓东
Owner 福安药业集团庆余堂制药有限公司
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