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Ceftizoxime sodium crystalline hydrate and preparation method and application thereof

A technology of ceftizoxime sodium and crystalline hydrate, which is applied in the field of ceftizoxime sodium crystalline hydrate and its preparation, can solve the problems of reporting the preparation method and application of ceftizoxime sodium crystalline hydrate, achieve good dissolution performance, improve Effect of bioavailability, increased man-hour cost

Inactive Publication Date: 2010-07-21
刘力
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] At present, the published literature only reports Ceftizoxime sodium (Ceftizoxime sodium) (C 13 h 12 N 5 NaO 5 S 2 , Molecular Weight: 405.38, CAS No.: 68401-82-1), so far, there is no published literature at home and abroad to report ceftizoxime sodium crystalline hydrate of the present invention and its preparation method and use

Method used

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  • Ceftizoxime sodium crystalline hydrate and preparation method and application thereof
  • Ceftizoxime sodium crystalline hydrate and preparation method and application thereof

Examples

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Effect test

Embodiment 1

[0032] Example 1 Preparation of ceftizoxime sodium 1.75 hydrate Add 10 g of ceftizoxime acid and 20 ml of water into a 50 ml Erlenmeyer flask, stir to form a suspension, add 4 ml of triethylamine dropwise at 5°C, stir to dissolve, add activated carbon 0.1 g, stirred for 30 minutes, suction filtered, washed with water, suction filtered, 20ml of sodium isooctanoate and ethanol mixed solution (containing 6.5g of sodium isooctanoate) was added dropwise to the filtrate at 5°C, stirred, adjusted pH to about 7.0 with glacial acetic acid, slowly Add dropwise a mixed solution of 50ml of acetone and 150ml of ethanol, place it below 5°C, allow the solid to fully separate out, filter it with suction, wash it with a small amount of ethanol for 3 times, and filter it with suction, recrystallize the obtained solid with a mixed solvent of water-ethanol-acetone, place it below 5°C, and make it The crystals were fully separated, filtered with suction, and dried in vacuum at 40°C for about 4 hour...

Embodiment 2

[0033] Example 2 Preparation of Ceftizoxime Sodium 1.75 Hydrate Add 20 g of Ceftizoxime Acid and 50 ml of water into a 250 ml Erlenmeyer flask, stir to form a suspension, add dropwise 20 ml of an aqueous solution of 2.9 g of anhydrous sodium carbonate at 5°C, and stir To dissolve, add 0.2g of activated carbon, stir for 30 minutes, filter with suction, wash with water, filter with suction, adjust the pH to about 7.0 with glacial acetic acid, slowly add 100ml of acetone and 250ml of ethanol dropwise, place it below 5°C, let the solid fully separate out, and filter with suction , washed 3 times with a small amount of ethanol, and suction filtered. The obtained solid was recrystallized with water, ethanol, isopropanol, and isopropyl ether as the crystallization solvent, and placed below 5°C to allow the crystals to fully separate out, suction filtered, and vacuum-dried at 40°C for about 4 hours. Obtained 14.1 g of off-white crystals, melting point: decomposition at 204°C (ELECTROTH...

Embodiment 3

[0034] Example 3 Take 100g of ceftizoxime sodium hydrate, stir to dissolve, add 20g of mannitol, 0.05g of disodium EDTA, add about 400-500ml of water for injection, stir to dissolve, and use about 1-5M citric acid and hydrogen phosphate Adjust the pH of the disodium solution to 6.5-7.5, add activated carbon 0.01-0.5% (W / V), stir for 15-30min, filter, filter with a 0.22 micron microporous membrane, pack in 0.5g / bottle or 1g / bottle, Vacuum freeze-drying and corking to obtain the finished product.

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Abstract

The invention relates to a ceftizoxime sodium crystalline hydrate and a preparation method and application thereof. The ceftizoxime sodium crystalline hydrate has high storage stability, and is suitable for preparing medicaments for treating or preventing diseases such as infection of respiratory systems, liver and biliary systems, five sense organs and urinary tracts of human bodes or animals, infection of abdominal cavity, infection of pelvic cavity, ichorrhemia, infection of skin tissues, and infection of bones and joint caused by gram positive or negative bacteria, meningitis caused by streptococcus pneumonia or haemophilus influenza, and simple gonorrhea.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to provide an antibacterial drug-cefuzoxime sodium crystalline hydrate, a preparation method and application thereof. Background technique [0002] At present, the published literature only reports Ceftizoxime sodium (Ceftizoxime sodium) (C 13 h 12 N 5 NaO 5 S 2 , Molecular weight: 405.38, CAS No.: 68401-82-1), so far, there is no published literature at home and abroad to report the ceftizoxime sodium crystalline hydrate of the present invention and its preparation method and use. Contents of the invention [0003] The present invention relates to ceftizoxime sodium crystalline hydrate and its preparation method and application, furthermore, it relates to an antibacterial infection drug, that is, the pharmaceutically acceptable salt crystalline hydrate of alkyl acetaldehyde sulfite and its preparation method and purposes, its molecular formula is C 13 h 12 N 5 NaO 5 S ...

Claims

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Application Information

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IPC IPC(8): C07D501/20A61K31/546A61K9/19A61K9/14A61K9/20A61K9/48A61P31/04
CPCA61K31/546C07D263/58A61P1/00A61P11/00A61P13/02A61P15/00A61P15/02A61P17/00A61P19/02A61P19/08A61P25/00A61P31/04
Inventor 刘力
Owner 刘力
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