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Cefodizime sodium crystal form and preparation method thereof as well as drug compound comprising crystal form

A technology of cefodizime sodium and a composition is applied in the field of preparation of pharmaceutical compounds, can solve the problems of high ethanol residue, high organic residue, low specific density and the like, and achieves the effects of easy operation, equipment saving and good fluidity

Inactive Publication Date: 2010-06-30
SHENZHEN SALUBRIS PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The currently commercially available cefodizime sodium product is in the form of dust, resulting in a very low specific density, which generates a huge amount of static electricity during the packaging process. When it is applied to preparations, manual packaging is required, which increases equipment, power and manpower. cost
In addition, the ethanol residue in this product is very high, and it is extremely difficult to remove
Patent EP391393 protects a method of preparing crystalline cefodizime sodium with cefodizime in aqueous ethanol with alkaline organic amine and sodium donor, but the cefodizime sodium crystals made according to this method are in the form of powder , after vacuum drying, its organic residue is higher

Method used

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  • Cefodizime sodium crystal form and preparation method thereof as well as drug compound comprising crystal form
  • Cefodizime sodium crystal form and preparation method thereof as well as drug compound comprising crystal form
  • Cefodizime sodium crystal form and preparation method thereof as well as drug compound comprising crystal form

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Take 5 g of cefodizime crude sodium salt sample, add it to 12.5 ml of purified water, and stir at room temperature until it dissolves completely. The solution was then placed in an ice bath and cooled to about 0 °C. Slowly drop 200ml of absolute ethanol into the above solution, and at the same time stir at a stirring speed of 250rpm until the solids are completely precipitated, filter with suction, wash the filter cake with acetone, and then vacuum-dry to constant weight to obtain 3.7g of granular cefodizime sodium crystals product. The resulting product X-ray diffraction pattern is as figure 1 As shown, its differential thermal analysis spectrum is shown as figure 2 As shown, its infrared spectrum is shown as image 3 shown.

[0033] The obtained cefodizime sodium crystal form product and the commercially available cefodizime sodium sample are carried out organic residue test, and gas chromatography analysis result shows that ethanol and acetone residual content a...

Embodiment 2

[0035] Take 5 g of cefodizime sodium salt sample, add it to 20 ml of methanol purified aqueous solution with a volume fraction of 50% (V / V), and stir at room temperature until completely dissolved. The solution was then placed in an ice bath and cooled to about 10°C. Slowly drop 300ml of ethanol into the above solution, and at the same time stir at a stirring speed of 200rpm until the solid is completely precipitated, filter with suction, wash the filter cake with acetone and vacuum dry to constant weight to obtain 3.6g of granular cefodizime sodium crystal form product. The X-ray diffraction pattern, differential thermal analysis pattern, and infrared spectrogram of the obtained product are basically consistent with Example 1; the residual content of methanol is less than 0.3%, and the residual content of ethanol and acetone is less than 0.5%, which meets the technical guidance of the national chemical drug residual solvent research. Standards established in principle (methan...

Embodiment 3

[0037] Take 5 g of cefodizime sodium salt sample, add 15 ml of 25% (V / V) methanol purified aqueous solution, and stir at room temperature until completely dissolved. The solution was then placed in an ice bath and cooled to about 5 °C. Slowly drop 200ml of acetone into the above solution, and at the same time stir at a stirring speed of 300rpm until the solid is completely precipitated, filter with suction, wash the filter cake with acetone and vacuum dry to constant weight to obtain 3.8g of granular cefodizime sodium crystal form product. Gained product X-ray diffraction pattern, differential thermal analysis pattern, infrared spectrogram are basically consistent with embodiment 1; Residual content of methanol is less than 0.3%, and residual content of acetone is less than 0.5%, conforms to the technical guideline of national chemical drug residual solvent research and formulates standard.

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Abstract

The invention provides a cefodizime sodium crystal form. In the X-ray diffraction pattern of the crystal form, a 2 theta angle is expressed to have peaks at the locations of 3.8 degrees and 6.8 degrees as well as 10.2 degrees and 21.7 degrees; the error is between plus or minus 0.2 degree; in a differential thermogram, an endothermic peak is located at 66-72 DEG C and an exothermic peak is located at 252-256 DEG C. The invention also provides a method for preparing the cefodizime sodium crystal form and a drug compound comprising the cefodizime sodium crystal form. The cefodizime sodium crystal form product of the invention is granulated and has good flowability, is not needed to be crushed when being applied to preparation, has small static electricity, and saves equipment, power and human resource costs for industrial production. The crystal form cannot be caked during drying, is easy to be operated, has low organic residue and meets relevant national standards.

Description

technical field [0001] The invention belongs to the field of preparation of pharmaceutical compounds, in particular to a crystal form of cefodizime sodium, a preparation method thereof and a pharmaceutical composition containing the crystal form. Background technique [0002] Cefodizime was invented by Hoechst, Germany, and it is the world's first third-generation cephalosporin with immune enhancing function. Cefodizime can enhance the immune response, and animal models and human studies in vitro and in vivo have shown that the drug can activate macrophages and increase their phagocytic activity and bactericidal rate. Cefodizime has high affinity to proteins involved in cell wall synthesis in sensitive bacteria. Cefodizime has a broad antibacterial spectrum, including most clinically relevant Gram-positive bacteria, Gram-negative bacteria, aerobic bacteria and anaerobic bacteria. [0003] The currently commercially available cefodizime sodium product is in the form of dust...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/36A61K31/546A61P31/04
Inventor 郑加林邵记
Owner SHENZHEN SALUBRIS PHARMA CO LTD
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