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Lactobionic azithromycin aqua compound, production and use of the same

A technology of azithromycin and lactobionic acid, applied in the field of medicine, to achieve the effect of good water solubility

Inactive Publication Date: 2008-04-02
刘力
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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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  • Lactobionic azithromycin aqua compound, production and use of the same
  • Lactobionic azithromycin aqua compound, production and use of the same
  • Lactobionic azithromycin aqua compound, production and use of the same

Examples

Experimental program
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Effect test

Embodiment 1

[0050] Example 1 In a three-necked flask, add ethanol acetone and azithromycin dihydrate, stir to dissolve, add lactobionic acid or its aqueous solution, stir continuously at 1-40°C to complete the reaction, slowly add ethyl formate, cool to 0-10 At about ℃, wait for the solid to precipitate, filter, rinse the solid with acetone, drain, and dry 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 reference substance of azithromycin, melting point: 157 -160°C, decomposed (uncorrected), Karl Fischer's method to determine the moisture is 3.03%, which is within the error range with the result that the sample contains 2.5 crystal waters (theoretical value 2.98%). TG-DTA: The weight loss at 60-130°C is about 3.108%, which is within the error range with the result that the sample contains 2.5 crystal waters. TG-DTA shows that there is an obvious endothermic peak before 130°C, indicati...

Embodiment 2

[0053] Example 2 In a three-necked flask, add ethanol to dissolve azithromycin, stir the lactobionic acid at 15-55°C to dissolve, and continue the reaction for 2 hours. After the reaction is completed, slowly add 2-15 times of ethyl formate and isopropanol (1:1), cooling, until the solid precipitates, filter, the solid is rinsed with methanol, drained, and dried at about 50°C to obtain off-white powder, easily soluble in water, HPLC: the retention of the main peak of the sample and the main peak of the azithromycin reference substance The time is consistent. Melting point: 151.5-156°C, decomposed, uncorrected; Moisture (Karl Fischer method): 5.25%, TG-DTA: 60-130°C weight loss of about 5.197%, which is the same as the result of the sample containing 4.5 crystal water (theoretical value %) within the margin of error. TG-DTA shows that there is an obvious endothermic peak before 130 ° C, indicating that the sample contains crystal water (see Figure 2). The obtained sample was ...

Embodiment 3

[0057] Example 3 Put lactobionic acid and azithromycin in a molar ratio (2:1) into a reaction flask, add water, heat, stir, control the temperature between 2-40°C, and react for 10-90min. After the reaction is completed, freeze it to - 50°C, keep it for 0.5-6 hours, lower the temperature of the condenser to -55°C, vacuumize, and gradually raise the temperature to about -20°C through the shelf, then keep it at about -20°C for about 24 hours, continue heating to heat up the medicine Keep at about 28°C for 6 hours to obtain a self-colored crystalline 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 azithromycin reference substance. Melting point: 153-157° C. (uncorrected), decomposed; Karl Fischer’s method determined moisture to be 6.05%, which was within the error range with the result that the sample contained 5 crystal waters (theoretical value 5.79%). TG-DTA: The weight lo...

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Abstract

The invention provides an azithromycinl actobioate hydrate and the purpose. The formula of the azithromycinl actobioate hydrate of the invention is C38H72N2O12question mark 2C12H22O12question mark nH2O, in which n is between 2.0 to 5.5.the hydrate has good water solubility, high storage stability, and is applicable to treat and prevent human or animal infectious diseases caused by Gram positive or negative bacteria.

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 use. 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. [0004] Surprisingly, we found through research that the lactobionate a...

Claims

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Application Information

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IPC IPC(8): A61K31/7052A61K9/00A61K9/02A61K9/16A61K9/19A61K9/20A61K9/46A61K9/48A61P31/04
CPCY02A50/30
Inventor 刘力
Owner 刘力
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