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Lactose-azithromycin hydrate, preparation and use thereof

A technology of azithromycin and lactobionic acid, applied in the field of medicine, achieves the effects of easier cleaning, good dissolution performance, and less contamination

Active Publication Date: 2009-03-11
深圳朗欧医药集团有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] The literature only reports azithromycin lactobionate [C 38 h 72 N 2 o 12 2C 12 h 22 o 12 Molecular weight: 1465.58] (azithromycin lactobionate) and its application, so far, there is no open literature report lactobionate azithromycin hydrate [C 38 h 72 N 2 o 12 2C 12 h 22 o 12 ·nH 2 O, n=2.0~5.5] and its preparation method and use

Method used

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  • Lactose-azithromycin hydrate, preparation and use thereof
  • Lactose-azithromycin hydrate, preparation and use thereof
  • Lactose-azithromycin hydrate, preparation and use thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0055] Example 1 In a three-necked flask, add 100 g of azithromycin dihydrate, add a 7:3 mixed solvent of isopropanol and acetone, stir to dissolve, add 91.2 g of lactobionic acid or its aqueous solution, and keep stirring at about 5 to 10 ° C to make After the reaction is completed, slowly add 1000ml of isopropanol, cool to -20~5°C, wait for the solid to precipitate out, filter, rinse the solid with anhydrous acetone, drain it, and dry it in vacuum at 80°C to obtain an off-white crystalline powder, easily soluble In water, HPLC: the retention time of the main peak of the sample is consistent with that of the main peak of the azithromycin reference substance, melting point: 157-160° C., decomposed (uncorrected), and the moisture measured by the Karl Fischer method is 3.03%, which is consistent with the result that the sample contains 2.5 crystal waters ( Theoretical value 2.98%) is within the error range. TG-DTA: The weight loss of the platform before 130°C is about 3.11%, whi...

Embodiment 2

[0056]Example 2 In a three-necked flask, add 95% isopropanol to dissolve 100 g of azithromycin, stir the lactobionic acid at 15-55°C to dissolve, and continue to react for 2 hours. After the reaction is completed, slowly add 2-15 times of formic acid Ethyl ester and isopropanol mixed solvent, cooling, until the solid precipitated, filtered, the solid was rinsed with ethyl formate, drained, and dried at about 50°C to obtain a off-white powder, easily soluble in water, HPLC: the main peak of the sample and azithromycin The retention time of the main peak of the reference substance was the same. Melting point: 151.5-156°C, decomposed, uncorrected; Moisture (Karls method): 5.25%, TG-DTA: The weight loss of the platform before 130°C is about 5.20%, which is consistent with the result that the sample contains 4.5 crystal waters (theoretical value 5.27 %) is within the margin of error. TG-DTA shows that there is an obvious endothermic peak before 130°C (see Figure 2); MS (ESI) m / z: ...

Embodiment 3

[0057] Example 3 Put lactobionic acid and azithromycin in a molar ratio (2:1) into a reaction flask, add water, stir, control the temperature between 2-20°C, and react for 10-90min. After the reaction is complete, add 0.5% activated carbon and stir For about 30 minutes, filter and decarburize, then use a 0.22 micron microporous membrane to filter aseptically, freeze it to about -50°C, keep it for 6 hours, reduce the temperature of the condenser to -55°C, vacuumize, and let the temperature drop through the shelf. After gradually rising to about -20°C, keep it at about -20°C for about 24 hours, continue heating to raise the temperature of the drug to about 28°C, and keep it for about 6 hours to obtain a off-white powder with a yield of 99%. The sample is easily soluble in water. HPLC: The retention time of the main peak of the sample is consistent with that of the main peak of the azithromycin reference substance, melting point: 153-157°C (uncorrected), decomposed; pH=6.42, the w...

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Abstract

The invention provides an azithromycin lactobionate hydrate and the preparation and application thereof. The molecular formula of the azithromycin lactobionate hydrate is C38H72N2O12.2C12H22O12.nH2O, wherein n is equal to between 2.0 and 5.5, the hydrate has good water solubility and storage stability and is applicable to the treatment and prevention of human or animal infectious diseases caused by sensitive bacterium of gram-positive or-negative bacterium.

Description

technical field [0001] The invention relates to the technical field of medicine, and specifically provides azithromycin lactobionate hydrate and its preparation and application. Background technique [0002] The literature only reports azithromycin lactobionate [C 38 h 72 N 2 o 12 2C 12 h 22 o 12 Molecular weight: 1465.58] (azithromycin lactobionate) and its application, so far, there is no open literature report lactobionate azithromycin hydrate [C 38 h 72 N 2 o 12 2C 12 h 22 o 12 ·nH 2 O, n=2.0~5.5] and its preparation method and application. Contents of the invention [0003] The present invention relates to azithromycin lactobionate hydrate and its preparation and application. Azithromycin lactobionic acid hydrate of the present invention, its molecular formula is C 38 h 72 N 2 o 12 2C 12 h 22 o 12 ·nH 2 O, n=2.0~5.5, n can be 2, 2.3, 2.5, 4.5, 5.0, 5.2, 5.5 and the number between. The hydrates of azithromycin lactobionate of the present inventi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/08A61K31/7052A61P31/04
CPCY02A50/30
Inventor 刘力
Owner 深圳朗欧医药集团有限公司
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