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Cefoxitin sodium compound entity and composition and uses thereof

A technology of cefoxitin sodium and compound, which is applied in the field of cefoxitin sodium compound entity and its composition and preparation to achieve the effects of improving bioavailability, increasing labor cost and good dissolution performance

Inactive Publication Date: 2015-03-11
胡梨芳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, many published documents have reported that cefoxitin sodium (Cefoxitin sodium) (C 16 h 16 N 3 NaO 7 S 2 , Molecular weight: 449.44, CAS No.: 33564-30-6) synthesis, pharmacology and clinical etc., also disclosed cefoxitin sodium and other β-lactamase inhibitors sulbactam sodium or tazobactam sodium or carat Potassium tretinoin combined with synergistic antibacterial etc. [Reference 1, Wei Qingjie, Li Huifen, Cefoxitin sodium crystallization process improvement, Guangzhou Chemical Industry, 2011,39(21):102-103; Reference 2, Cefoxitin sodium Preparation method, CN201310369951.1; reference 3, an antibiotic composition, its preparation method and use, CN201010531963.6; reference 4, antibacterial drug composition, CN200410046224.2]; so far, there is no publication at home and abroad The bibliographical report of cefoxitin sodium crystalline hydrate of the present invention and its preparation method and application

Method used

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  • Cefoxitin sodium compound entity and composition and uses thereof
  • Cefoxitin sodium compound entity and composition and uses thereof
  • Cefoxitin sodium compound entity and composition and uses thereof

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Embodiment 1

[0057] The preparation of embodiment 1 cefoxitin sodium 0.5 hydrate

[0058] At room temperature, add 10g of cefoxitin acid, 90ml of methanol, and 5ml of water into a 500ml flask, stir to dissolve, add 0.1g of activated carbon, stir for 30 minutes, filter with suction, add sodium isooctanoate dropwise in the filtrate at about 8°C while stirring 4.12g of ethyl acetate 10ml and acetone 35ml solution, continue to stir for 1h after adding, then slowly add about 200ml of acetone, 30ml of ethanol, 2ml of ethyl acetate dropwise, and then place it at 6~-5℃ for 16-24 hours, Let the solid be fully separated, filter with suction, rinse the solid with a small amount of chloroform and ethanol for 3 times, filter with suction, dissolve the obtained solid with an appropriate amount of water, use 20ml of isopropanol, 30ml of ethanol, and about 200ml of acetone as solvents for recrystallization, and place it at about 4°C For about 2 hours, then put it at about 0°C for about 2 hours, then put i...

Embodiment 2

[0059] The preparation of embodiment 2 cefoxitin sodium 0.5 hydrate

[0060] At room temperature, add 20g of cefoxitin acid, 90ml of methanol, 10ml of ethanol, and 5ml of water into a 500ml flask, stir to dissolve, add 0.2g of activated carbon, stir for 30 minutes, filter with suction, add sodium isooctanoate dropwise to the filtrate at 5°C 8.2 g of 80ml of methanol and 10ml of acetone, stirred for 1 hour, then slowly added dropwise about 380ml of acetone and about 80ml of ethanol, then placed at 10-5°C for about 2 hours, and then placed at 0-8°C overnight to make the solid fully Precipitate, filter with suction, rinse the solid with a small amount of chloroform and ethanol for 3 times, filter with suction, dissolve the obtained solid with an appropriate amount of water, use about 350ml of acetone, about 80ml of ethanol, and 3ml of isopropyl ether as the crystallization solvent for recrystallization, and place at 4°C for 2 hours Then place it at about -6°C for about 2 hours, t...

Embodiment 3

[0061] The preparation of embodiment 3 cefoxitin sodium 0.5 hydrate

[0062]At room temperature, add 10g of cefoxitin acid and 80m of ethanol to a 500ml flask, stir to dissolve, add 0.1g of activated carbon, stir for 30 minutes, filter with suction, add sodium bicarbonate solution dropwise to the filtrate at about 4°C, stir, and make When its pH is about 7.0, slowly add it into a flask containing about 50ml of acetone and about 250ml of ethanol, and place it overnight below 0°C to allow the solid to fully separate out, filter it with suction, rinse the solid with a small amount of chloroform and ethanol for 3 times, and pump it out. Filter, and dissolve the obtained solid with an appropriate amount of water, about 220ml of ethanol, about 50ml of acetone, 2ml of chloroform, and 2ml of acetonitrile for recrystallization, and place it at 4°C for about 2 hours, then place it at 0°C for about 2 hours, and then place it at about -4°C Place it for 18-24 hours to allow the crystals to...

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Abstract

The invention discloses a cefoxitin sodium new chemical compound entity and a composition thereof, the cefoxitin sodium new chemical compound storage has better stability less hygroscopicity, and is suitable for preparation of drugs for the treatment or prevention of human or animal respiratory tract infection, endocarditis, peritonitis, pyelonephritis, urinary tract infection, blood poisoning and bone, joint, skin and soft tissue infection and the like caused by gram positive or negative bacteria sensitive bacteria.

Description

technical field [0001] The invention relates to the technical field of medicine, and specifically provides an antibacterial drug cefoxitin sodium compound entity and its composition, preparation method and application. Background technique [0002] Polymorphic forms of chemical drugs play an important role in drug research. In the field of pharmacology, the research work on drug crystal forms and drug hydrates or drug solvates has been listed in the research scope of the National Twelfth Five-Year Major New Drug Innovation Science and Technology Major Project. Solvents of compounds, including hydrates, have been prepared and used in medicines for a long time. For example, the antineoplastic drug cyclophosphamide recorded in the 36th edition of the US Pharmacopoeia, the 6.1th edition of the European Pharmacopoeia, and the 2010 edition of the Chinese Pharmacopoeia was prepared in a solid form at room temperature. It exists in the form of hydrate, and the compound entity begin...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D501/57C07D501/12A61K31/546A61P31/04A61K31/424A61K31/43A61K31/431
CPCC07D501/04C07D501/12C07D501/57
Inventor 刘力
Owner 胡梨芳
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