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Lactobionic acid azithromycin for injections and preparation method thereof

A technology of azithromycin and lactobionic acid, applied in the field of azithromycin lactobionate freeze-dried powder injection and its preparation, can solve the problems of reduced potency, increased toxicity, loss of antibacterial activity, etc. Effect

Inactive Publication Date: 2008-12-24
HAINAN JINRUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Studies have shown that both azithromycin and its acid salts have unstable factors, such as oxidation and hydrolysis, which can lead to a decrease in their potency and loss of antibacterial activity, and local toxicity such as liver toxicity increases significantly

Method used

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  • Lactobionic acid azithromycin for injections and preparation method thereof
  • Lactobionic acid azithromycin for injections and preparation method thereof
  • Lactobionic acid azithromycin for injections and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Dissolve 250g of azithromycin lactobionate finished product in 1600mL of water for injection, stir to dissolve, add 4.0g of activated carbon, stir and decolorize at a temperature of 5°C for 30 minutes, then filter through a 0.45μm microporous membrane to remove carbon, and then add water for injection to 2000ml, fully stirred for 20 minutes to mix the solution evenly, and the prepared solution was filtered and sterilized through a 0.22 μm microporous membrane. Put the final filtrate into the tray of the lyophilizer, quickly cool down to -38°C to make it initially solidify, then continue to cool down to -55°C, keep it frozen at -55°C for 4 hours, make it completely frozen, vacuumize, and then Gradually raise the temperature to -2°C within 11 hours, maintain -2°C and vacuum dry for 8 hours, continue to raise the temperature, rise to 30°C within 3 hours, and maintain 30°C for 7 hours to obtain azithromycin lactobionate freeze-dried powder injection The moisture in it is 0....

Embodiment 2

[0037] Dissolve 250g of the finished product of azithromycin lactobionate in 1600mL of water for injection, stir to dissolve, add 3.2g of activated carbon, stir and decolorize at a temperature of 3°C for 30 minutes, then filter through a 0.45μm microporous membrane to remove carbon, and then add water for injection to 2000ml, fully stirred for 20 minutes to mix the solution evenly, and the prepared solution was filtered and sterilized through a 0.22 μm microporous membrane. Put the final filtrate into the tray of the lyophilizer, quickly cool down to -35°C to make it initially solidify, then continue to cool down to -60°C, keep it frozen at -60°C for 4.5 hours, make it completely frozen, vacuumize, and then Gradually raise the temperature to 0°C within 12 hours, maintain 0°C and vacuum-dry for 9 hours, continue to raise the temperature, rise to 35°C within 3.5 hours, and maintain 35°C for 6.5 hours, the obtained azithromycin lactobionate freeze-dried powder injection Moisture ...

Embodiment 3

[0039] Dissolve 250g of the finished product of azithromycin lactobionate in 1600mL of water for injection, stir to dissolve, add 3.68g of activated carbon, stir and decolorize at a temperature of 8°C for 30 minutes, then filter through a 0.45μm microporous membrane to remove carbon, and then add water for injection to 2000ml, fully stirred for 20 minutes to mix the solution evenly, and the prepared solution was filtered and sterilized through a 0.22 μm microporous membrane. Put the final filtrate into the feed tray of the freeze dryer, quickly cool down to -30°C to make it initially solidify, then continue to cool down to -50°C, keep it frozen at -50°C for 5 hours, make it completely frozen, vacuumize, and then Gradually raise the temperature to -5°C within 9 hours, maintain -5°C for 11 hours in vacuum drying, continue to raise the temperature, rise to 30°C within 2 hours, maintain 30°C for 6 hours in vacuum drying, and obtain azithromycin lactobionate freeze-dried powder inje...

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Abstract

The invention provides lactose-azithromycin freeze-dried powder and a preparation method thereof. The freeze-dried powder with simple components only contains main drug component. The preparation method of the lactose-azithromycin freeze-dried powder is that main drug is dissolved in injection water, and then is decolorized and filtered through activated carbon, the filtrate is cooled at 30DEG below zero to 60DEG below zero in a freeze drier to be solidified, and then is heated to 0 DEG to 40 DEG by stages in the condition of high vacuum, meanwhile, freeze-drying curve is controlled strictly, and finally, the lactose-azithromycin freeze-dried powder is obtained. The obtained lactose-azithromycin freeze-dried powder has the advantages of favorable stability and resolubity, etc.

Description

technical field [0001] The invention relates to azithromycin lactobionate for injection, in particular to azithromycin lactobionate freeze-dried powder injection and a preparation method thereof. Background technique [0002] Azithromycin Lactobionate (Azithromycin Lactobionate) is a semi-synthetic azaza fifteen-membered ring macrolide antibiotics, its chemical name is (2R, 3S, 4R, 8R, 10R, 11R, 12S, 13S, 14R) -13-[(2,6-Dideoxy-3-C-methyl-3-O-methyl-(L-nuclear-hexapyranosyl)oxy)-2-ethyl-3,4,10 -Trihydroxy-3,5,6,8,10,12,14-heptamethyl-11-[(3,4,6-trideoxy-3-(dimethylamino)-β-D-wood-hexyl 2 lactobionate salt of pyranosyl)oxy]-1-oxa-6-azacyclopentadecan-15one, the molecular structure is: [0003] [0004] Azithromycin is introduced into NCH on 9a of erythromycin lactone 3 , a 15-membered ring antibiotic prepared by substituting a methyl group. Due to the change of chemical structure, the drug has better antibacterial properties, pharmacokinetic properties and therapeutic e...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K31/7052A61P31/04
Inventor 王小树
Owner HAINAN JINRUI PHARMA
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