Cefonicid sodium hydrate and preparation method and application thereof

A technology of cefnixin sodium and hydrate, which is applied in the field of medicine, can solve the problems such as the preparation method and application of cefnixin sodium hydrate that have not been published in the literature, and achieve the goals of improving operability, preventing adhesion, and good sliding properties Effect

Inactive Publication Date: 2011-10-12
胡梨芳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the published literature has only reported that cefnixime sodium (C 18 h 16 N 6 Na 2 o 8 S 3 , Molecular Weight: 586.53, CAS No.: 61270-7

Method used

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  • Cefonicid sodium hydrate and preparation method and application thereof
  • Cefonicid sodium hydrate and preparation method and application thereof
  • Cefonicid sodium hydrate and preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0049] Example 1 Preparation of Cefnixin Sodium Monohydrate Add 10 g of cefonicus acid and 20 ml of water to the reaction flask, stir to form a suspension, add 4 ml of triethylamine dropwise at 5°C, stir to dissolve, add 0.1 g of activated carbon , stirred for 30 minutes, filtered with suction, washed with water, filtered with suction, and added dropwise 20% sodium isooctanoate in isopropanol solution to the filtrate at 5°C under stirring to make the pH to 6.5 (after the alkali is excessive, adjust the pH to 6.5 with glacial acetic acid) , stirred for 40 minutes, slowly added dropwise 50ml of acetone and 150ml of ethanol, placed below 5°C, the solid was fully separated out, filtered with suction, washed 3 times with a small amount of ethanol, and filtered with suction, the obtained solid was dissolved with a small amount of water, and then mixed with 200ml of ethanol, Recrystallize with 200ml of acetone and 5ml of chloroform, place it below -5°C, let the solid fully separate ou...

Embodiment 2

[0050] Example 2: Preparation of Cefnicillin Sodium Monohydrate Add 20 g of Cefnicillin and 40 ml of water in a reaction flask, stir to form a suspension, stir, and add dropwise a saturated aqueous solution of anhydrous sodium carbonate at 5° C. to bring the pH to 6.6, add 0.1g of activated carbon, stir for 30 minutes, and filter with suction, add 400ml of acetonitrile and 250ml of isopropanol to the filtrate, place it below -10°C to allow the solid to fully separate out, filter with suction, wash with ethanol for 3 times, and filter with suction, the obtained solid is used for A small amount of water to dissolve it completely, use 300ml of isopropanol, 420ml of acetonitrile, and 80ml of isopropyl ether as the crystallization solvent for recrystallization, place it overnight at -15°C to allow the solid to fully separate out, filter it with suction, and dry it under vacuum at 40°C and 20mmHg for about 4 hours , to obtain 10.6 g of off-white solid, melting point: 165 ° C decompos...

Embodiment 3

[0051] The preparation of embodiment 3 cefnisin sodium 1 hydrate is added in reaction flask 20g, water 5ml, methyl alcohol 200ml, stirs, drips the ethanolic solution of 28% sodium isooctanoate at 5 ℃ and makes pH to 6.6 (alkali After excess, use glacial acetic acid to adjust the pH to 6.6), stir for 30 minutes, slowly add 50ml of acetone and 150ml of ethanol dropwise, place below 5°C to allow the solid to fully separate out, filter with suction, wash with ethanol for 3 times, and filter with suction. Dissolve it in water, use 300ml of ethanol, 420ml of acetonitrile, and 80ml of isopropyl ether as the crystallization solvent to carry out recrystallization, place it overnight at -10°C to allow the crystals to fully separate out, filter with suction, wash 3 times with 10ml×3 chloroform, and filter with suction for 40 Vacuum drying below 20mmHg for about 4 hours to obtain 12.1g of off-white crystals, melting point: 166°C decomposition (ELECTROTHERMAL MELTING POINT APPARATUS, uncorr...

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Abstract

The invention relates to a cefonicid sodium hydrate and a preparation method and application thereof. The cefonicid sodium hydrate has better storage stability and is applicable to preparation of the medicaments for treating or preventing such diseases caused by gram positive or negative sensitive bacteria as respiratory system infection, hepatobiliary system infection, five sense infection, urinary tract infection, abdominal infection, pelvic infection, sepsis, skin soft tissue infection, bone and joint infections, annexitis, intrauterine infection, parametritis, meningitis, gonorrhea and the like of human or animals.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to provide an antibacterial drug-cefenicid sodium hydrate, a preparation method and application thereof. Background technique [0002] Cefonicid sodium is a second-generation cephalosporin for intravenous or intramuscular injection. Compared with the first-generation cephalosporins, the antibacterial effect of cefnicillin sodium has a broad-spectrum anti-gram-negative bacilli effect. Compared with cefamandole, it has anti-E. The effects of Citrobacter and Enterobacter are better, but they are less effective against indole-positive Proteus. Cefnixime sodium has a good effect on Haemophilus influenzae and Neisseria gonorrhoeae. However, cefnixime is resistant to Streptococcus faecalis, Penicillin-resistant Staphylococcus aureus and Staphylococcus epidermidis, Pseudomonas, Serratia and Acetobacter. [0003] At present, the published literature has only reported that cefnixime sodiu...

Claims

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Application Information

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IPC IPC(8): C07D501/36C07D501/02A61K31/546A61K9/14A61K9/19A61K9/08A61K9/20A61K9/48A61P31/04A61P1/16A61P7/00A61P17/00A61P19/02A61P19/08A61P15/00
Inventor 刘力胡梨芳
Owner 胡梨芳
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