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Crystal form of flomoxef sodium, preparation method, pharmaceutical composition and application

A technology of sodium fluoxefaclor and a composition, applied in the field of drug crystals, can solve the problems of inability to be removed by drying, no clear disclosure of the crystal form of sodium fluoxefate, and organic solvents affecting medicinal value, etc., and achieve the advantage of good stability Effect

Active Publication Date: 2020-05-22
泊诺(天津)创新医药研究有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, fluoxetal sodium is easy to form solvated crystals with organic solvents such as dichloromethane, ethyl acetate, methanol, etc., which cannot be removed by drying, and the residue of organic solvents seriously affects its medicinal value.
[0008] At present, there is no clear and public information about the crystal form of fluoxetal sodium

Method used

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  • Crystal form of flomoxef sodium, preparation method, pharmaceutical composition and application
  • Crystal form of flomoxef sodium, preparation method, pharmaceutical composition and application
  • Crystal form of flomoxef sodium, preparation method, pharmaceutical composition and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Add 40 grams of fluoxetal acid to a mixed solvent of 400 milliliters of ethylene glycol and 400 milliliters of isobutanol, and stir to dissolve. 5% (W / W) sodium bicarbonate aqueous solution was added dropwise under stirring to adjust the pH to 4.5-6.0. Afterwards, stirring and cooling down to -10°C, continued stirring and crystallization for 5 hours, the suspension was filtered, and the obtained crystals were washed with isobutanol, and vacuum-dried at 25°C to constant weight to obtain 26.6 grams of white granular crystals of fluoxetal sodium, The purity of the crystal form obtained in this example was determined to be 98.4% by high performance liquid chromatography (HPLC).

Embodiment 2

[0053] Add 20 grams of fluoxetal acid to a mixed solvent of 150 milliliters of ethylene glycol and 150 milliliters of isobutanol, and stir to dissolve. Add about 8% (W / W) sodium bicarbonate aqueous solution dropwise under stirring to adjust the pH to 4.5-6.0. Then cool down to -15°C under stirring, continue to stir and crystallize for 5 hours, filter the suspension, wash the obtained crystals with isobutanol, and vacuum-dry at 25°C to constant weight to obtain 15.8 grams of white granular crystals of fluoxetal sodium , the purity of the crystalline form obtained in this example was measured by high performance liquid chromatography (HPLC) to be 99.1%.

Embodiment 3

[0055] Add 50 grams of fluoxetal acid to a mixed solvent formed by 375 milliliters of ethylene glycol and 375 milliliters of isobutanol, and stir to dissolve. About 10% (W / W) sodium bicarbonate aqueous solution (saturated solution stirred for 1 hour at 25° C.) was added dropwise with stirring to adjust the pH to 4.5-6.0. Then cool down to -20°C under stirring, continue to stir and crystallize for 5 hours, filter the suspension, wash the obtained crystals with isobutanol, and vacuum-dry at 25°C to constant weight to obtain 40.1 g of white granular crystals of fluoxetal sodium , the purity of the crystalline form obtained in this example was measured by high performance liquid chromatography (HPLC) to be 99.6%.

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Abstract

The invention provides a crystal form of flomoxef sodium. An X-ray diffraction pattern of the crystal form comprises X-ray diffraction peaks as shown in the following 2[theta] angles: 5.2 + / -0.2 degrees and 16.2 + / -0.2 degrees. In addition, the invention also discloses a preparation method of the crystal form compound, a pharmaceutical composition and application of the crystal form compound and the pharmaceutical composition in preparation of anti-bacterial infection drugs. Compared with an amorphous product prepared by a freeze-drying process, the novel crystal form obtained by the preparation method disclosed by the invention has the advantages that the stability of the novel crystal form is obviously superior to that of the amorphous form, which means that the crystal form disclosed bythe invention has less degradation impurity generation and lower drug storage condition requirements within the validity period, and has a good medicinal use prospect.

Description

technical field [0001] The present invention relates to the technical field of pharmaceutical crystals, in particular to a new crystal form of fluoxetal sodium, a preparation method, a pharmaceutical composition and an application. Background technique [0002] Fluoxefem sodium is a broad-spectrum oxycephem antibiotic developed and prepared by Yoshishi Shiono in Japan in 1982. The structure of the 7- and 3-position side chains of the mother ring of oxacephem has been modified to make it possess Activity against Gram-negative bacteria, and further enhanced activity against Gram-positive bacteria. Due to the disulfide structure, fluoxefor sodium exhibits lower nephrotoxicity. The drug was first launched in Japan in 1988. Fluoxefor sodium is a broad-spectrum oxacephalosporin antibacterial drug, very stable to β-lactamase, and its antibacterial spectrum is similar to other third-generation cephalosporins. Fluoxef has a strong antibacterial effect on Staphylococcus aureus, esp...

Claims

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Application Information

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IPC IPC(8): C07D505/20C07D505/02A61P31/04A61K31/5365
CPCC07D505/20C07D505/02A61P31/04C07B2200/13
Inventor 沈载宽韩学文
Owner 泊诺(天津)创新医药研究有限公司
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