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Cefodizime sodium hydrate, preparation method thereof and application thereof

A technology of cefodizime sodium and hydrate, which is applied in the field of medicine, can solve the problems such as the preparation method and application of cefodizime sodium crystalline hydrate that have not been reported in the literature, and achieve improved bioavailability, operability, and convenience The effect of storage and transportation

Inactive Publication Date: 2010-09-15
胡梨芳
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] At present, the published literature only reports cefodizime sodium (Cefodizime sodium) (C 20 h 18 N 6 Na 2 o 7 S 4 , Molecular Weight: 628.63, CAS No.: 86329-79-5), so far, there is no published literature at home and abroad to report the cefodizime sodium crystalline hydrate of the present invention and its preparation method and use

Method used

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  • Cefodizime sodium hydrate, preparation method thereof and application thereof
  • Cefodizime sodium hydrate, preparation method thereof and application thereof
  • Cefodizime sodium hydrate, preparation method thereof and application thereof

Examples

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Embodiment 1

[0038] Example 1 Preparation of cefodizime sodium monohydrate Add 10 g of cefodizime acid and 30 ml of water to a reaction flask, stir to form a suspension, add 5 ml of triethylamine dropwise at 5 °C, stir for 30 min, dropwise at 5 °C Add 28% ethanol solution of sodium isooctanoate to make the pH to 6.9 (after adding more, adjust the pH to about 6.9 with glacial acetic acid), stir, slowly add 50ml of acetone and 150ml of acetonitrile dropwise, place it below -5°C, and allow the solid to be fully separated out. Suction filtration, washed 3 times with a small amount of acetone, suction filtration, the obtained solid was just dissolved with a small amount of water, 0.15 g of activated carbon was added, stirred for 30 minutes, suction filtration, washed with water, suction filtration, and then recrystallized with 200 ml of acetonitrile and 200 ml of acetone, Place below 5°C to fully separate out the crystals, filter with suction, wash with 30ml of chloroform, filter with suction, a...

Embodiment 2

[0039] Example 2 Preparation of cefodizime sodium monohydrate Add 10 g of cefodizime acid and 30 ml of water to a reaction flask, stir to make a suspension, add 3.8 ml of diethylamine dropwise at 5°C, stir to dissolve, add activated carbon 0.2g, stirred for 30 minutes, suction filtered, washed with water, suction filtered, add 28% ethanol solution of sodium isooctanoate dropwise to the filtrate at 5°C to make the pH to 6.9, stir, slowly add it to 400ml of acetone, place below 0°C, The solid was fully separated out, filtered with suction, washed 3 times with a small amount of acetone, filtered with suction, the obtained solid was just dissolved with a small amount of water, then recrystallized with 500 ml of acetone, placed below -10°C to fully separate out the crystals, filtered with suction, 30 ml Washed with chloroform, suction filtered, and vacuum dried at 45°C for about 8 hours to obtain 5.6g of off-white crystals, melting point: 196°C discoloration (ELECTROTHERMAL MELTING ...

Embodiment 3

[0040] Example 3 Preparation of cefodizime sodium 1.5 hydrate Add 20 g of cefodizime acid and 50 ml of water to a reaction flask, stir to form a suspension, and dropwise add a saturated aqueous solution of 3.8 g of anhydrous sodium carbonate at 5°C to make the pH to 7.0 (after adding more, adjust the pH to about 7.0 with glacial acetic acid), stir, add activated carbon 0.3g, stir for 30 minutes, suction filter, wash with water, suction filter, slowly add acetone 50ml, isopropanol 250ml dropwise to the filtrate, -5 Place below ℃ to make the solid fully separate out, filter with suction, wash with acetone for 3 times, filter with suction, the obtained solid is just dissolved with a small amount of water, add 0.3 g of activated carbon, stir for 30 minutes, suction filtration, wash with water, suction filtration, use isopropyl Recrystallize it with 300ml of alcohol and 420ml of acetone, put it at below 5°C overnight to fully separate out the crystals, filter with suction, wash with...

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Abstract

The invention relates to a cefodizime sodium hydrate, a preparation method thereof and application thereof. The cefodizime sodium hydrate has high storage stability, and is suitable to be used in the preparation of medicaments for treating and preventing diseases, caused by Gram-positive or negative bacterial sensitive bacteria, such as diseases in respiratory systems, liver and gall systems and five sense organs of human beings and animals, urinary tract infection, enterocoelia infection, pelvic cavity infection, ichorrhemia, skin and soft tissue infection, bone and joint infection, annexitis, intrauterine infection, parametric connective tissue inflammation, cephalomeningitis, gonorrhoea and the like.

Description

technical field [0001] The invention relates to the technical field of medicine, and specifically provides an antibacterial drug-ceftizazim sodium hydrate and a preparation method and application thereof. Background technique [0002] Cefodizime sodium is a third-generation cephalosporin for intravenous or intramuscular injection. Cefidiazine sodium has a broad-spectrum antibacterial effect, and has strong antibacterial activity against gram-negative bacteria such as Lebsiella pneumoniae, Proteus, Shigella, Shigella, Salmonella, Typhoid Bacillus, Haemophilus influenzae It also has good antibacterial activity against Gram-positive bacteria such as Staphylococcus, Streptococcus pneumoniae, Streptococcus, Neisseria gonococcus (including penicillin-producing strains), and Neisseria meningitidis. It has a certain antibacterial effect on methicillin-sensitive Staphylococcus aureus (MSSA) and Staphylococcus epidermidis, and has a certain antibacterial effect on Pseudomonas aerugin...

Claims

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Application Information

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IPC IPC(8): C07D501/36C07D501/04A61K31/546A61K31/424A61K31/43A61K31/431A61P31/04
CPCA61K31/546A61K31/424C07D501/04A61K31/43A61K31/431C07D501/36A61P31/04
Inventor 刘力
Owner 胡梨芳
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