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Cefuroxime sodium compound entity and application thereof

A technology of cefuroxime sodium and compound, which is applied in the field of medicine and achieves the effects of good stable storage, good sliding property, and convenient storage and transportation

Inactive Publication Date: 2014-10-01
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the published literature only reports the cephalosporin——Cefuroxime sodium (Cefuroxime sodium) (C 16 h 15 N 4 NaO 8 S, molecular weight: 446.37, CAS No.: 56238-63-2), so far, there is no published literature at home and abroad to report the novel cefuroxime sodium compound entity of the present invention, i.e. cefuroxime sodium crystalline hydrate and its preparation method and use

Method used

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  • Cefuroxime sodium compound entity and application thereof
  • Cefuroxime sodium compound entity and application thereof
  • Cefuroxime sodium compound entity and application thereof

Examples

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Embodiment 1

[0063] The preparation of embodiment 1 cefuroxime sodium 0.25 hydrate

[0064] At room temperature, add 10.6g of high-purity cefuroxime acid, 180ml of acetone, 10ml of ethanol, and 5ml of water into a 500ml flask, stir to dissolve, add 0.06g of activated carbon, stir for 30 minutes, filter with suction, and dissolve in the filtrate at 4°C Add 60ml of a mixed solution of sodium isooctanoate and ethanol (containing 4.72g of sodium isooctanoate) dropwise, stir, and place below 4°C to allow the solid to fully separate out, filter with suction, wash twice with a small amount of chloroform and twice with a small amount of ethanol, and filter with suction to obtain Dissolve the solid with a small amount of water, then use 260ml of ethanol, 20ml of isopropanol, and 20ml of acetone as solvents for recrystallization, place it below 4°C to allow the crystals to fully separate out, filter with suction, rinse with a small amount of ethanol and chloroform alternately, and filter with suction...

Embodiment 2

[0065] The preparation of embodiment 2 cefuroxime sodium 0.25 hydrate

[0066]At room temperature, add 20g of cefuroxime acid, 180ml of acetone, 10ml of methanol, and 5ml of water into a 1000ml flask, stir to dissolve, add 0.2g of activated carbon, stir for 30 minutes, filter with suction, add dropwise a mixed solution of sodium isooctanoate and ethanol to the filtrate (Containing 9.42g of sodium isooctanoate) 150ml, place it below 4°C, let the solid fully separate out, filter with suction, wash with a small amount of ethanol for 3 times, filter with suction, dissolve the obtained solid with a small amount of water, add 300ml of ethanol, 20ml of isopropanol, 20ml of isopropanol Recrystallize 5ml of ether, place it below 5°C to allow the crystals to fully separate out, filter with suction, wash twice with a small amount of dichloromethane, wash twice with a small amount of ethanol, filter with suction, dilute the obtained solid at about 20°C and blow dry for 1 day, then Vacuum ...

Embodiment 3

[0067] The preparation of embodiment 3 cefuroxime sodium 0.25 hydrate

[0068] Add 10g of cefuroxime acid and 20ml of water to a 500ml flask, add an appropriate amount of 95% ethanol and stir until dissolved, add a saturated aqueous solution of sodium bicarbonate dropwise at 10°C until the pH is about 8.9, stir to dissolve, add 0.1g of activated carbon, Stir for 30 minutes, filter with suction, slowly add 10ml of chloroform and 300ml of ethanol dropwise to the filtrate, place it below 10°C, let the solid fully separate out, filter with suction, wash with a small amount of chloroform and ethanol twice, filter with suction, dissolve the obtained solid with a small amount of water, Then use 220ml of ethanol, 10ml of isopropanol, 2ml of chloroform, and 2ml of ethyl acetate as crystallization solvents for recrystallization, place below 8°C to allow the crystals to fully separate out, filter with suction, and wash with a small amount of dichloromethane, ethyl acetate, and ethanol in ...

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Abstract

The invention discloses a cefuroxime sodium compound entity which is relatively poor in hygroscopicity, relatively good in storage stability and applicable to preparation of drugs for treating or preventing respiratory system infection, five-organ infection, urinary system infection, pelvic cavity infection, septicemia, skin soft-tissue infection, bone and joint infection, gonorrhea and meningitis of human or animals, caused by sensitive gram positive or negative bacteria.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular, it provides a new compound entity of the antibacterial drug cefuroxime sodium, a pharmaceutical composition thereof, a preparation method and application thereof. Background technique [0002] Cefuroxime sodium is a second-generation cephalosporin antibiotic. The antibacterial activity against Gram-positive cocci is similar to or slightly worse than that of the first-generation cephalosporins, but it is quite stable against β-lactamases produced by Staphylococci and Gram-negative bacilli. Methicillin-resistant Staphylococcus, Enterococcus and Listeria are drug-resistant, and other positive cocci (including anaerobic cocci) are sensitive to this product. The antibacterial activity against Staphylococcus aureus is worse than that of cefazolin, and 1-2 mg / L can inhibit all Staphylococcus aureus sensitive and resistant to penicillin, respectively. It has strong antibacterial activit...

Claims

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Application Information

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IPC IPC(8): C07D501/34C07D501/04A61K31/546A61P31/04A61K31/424A61K31/43A61K31/431
CPCC07D501/34C07D501/04
Inventor 刘力
Owner 刘力
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