Cefonicid sodium hydrate and preparation method and application thereof

A technology of cefnixime 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 reported in the literature, and achieve improved bioavailability, increased labor costs, and good dissolution performance 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

[0034] 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, added dropwise a solution of 20% sodium isooctanoate in isopropanol to the filtrate at 5°C under stirring to make the pH to 6.8 (after the alkali is excessive, adjust the pH to 6.8 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, filtered with suction, the obtained solid was just dissolved completely with a small amount of water, and 200ml of ethanol was added , Acetone 200ml mixed solvent for recrystallization, place below 5°C to fully separate the crystals, filt...

Embodiment 2

[0035] Example 2: Preparation of Cefnixin Sodium Monohydrate Add 20 g of cefonic acid and 50 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 6.9, add 0.1g of activated carbon, stir for 30 minutes, filter with suction, slowly add 400ml of acetonitrile and 250ml of ethanol dropwise to the filtrate, place it below 10°C, let the solid fully separate out, filter with suction, wash with ethanol for 3 times, and filter with suction. A small amount of water to make it completely dissolved, add 300ml of ethanol, 420ml of acetonitrile, and 80ml of isopropyl ether as the crystallization solvent to carry out recrystallization, place it under 5°C overnight to fully separate the crystals, filter it with suction, and dry it in vacuum at 40°C for about 4 hours to obtain off-white Crystal 10.6g, melting point: decomposed at 165°C (ELECTROTHERMAL MELTING POINT APPARATUS, unco...

Embodiment 3

[0036]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 7.0 (alkali After excess, use glacial acetic acid to adjust the pH to 7.0), 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. Make it completely dissolved in water, add 300ml of ethanol, 420ml of acetonitrile, and 80ml of isopropyl ether as the crystallization solvent to carry out recrystallization, place it under 5°C overnight to allow the crystals to fully separate out, filter with suction, wash with 10ml×3 chloroform for 3 times, and filter with suction. Vacuum-dried at 40°C for about 4 hours to obtain 12.1 g of off-white crystals, melting point: decomposed at 165°C (ELECTROTHERMAL MELTING POINT APPARAT...

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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): C07D501/36C07D501/02A61K31/546A61P31/04A61K9/19A61K9/16A61K9/20A61K9/08
Inventor 刘力胡梨芳
Owner 胡梨芳
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