Water soluble Azithromycin salt and its eye drop

A technology of azithromycin and water-soluble salt, which is applied in the field of eye drops and achieves the effects of convenient preparation, stable properties and clear solution

Inactive Publication Date: 2002-04-17
安徽省新药研究院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, the water solubility and stability of azithromycin must be solved

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0011] Non-limiting examples are described as follows:

[0012] One, the preparation of azithromycin water-soluble salt

[0013] 1. Azithromycin Lactate

[0014] Add 7.5g of azithromycin into a beaker containing 50ml of ethyl acetate, stir until the azithromycin is completely dissolved, and filter; gradually add 2.1ml of lactic acid that has been filtered until it becomes clear, and continue stirring until the precipitation of azithromycin lactate is complete. After filtration, the azithromycin lactate precipitate was dried under reduced pressure at 55°C±2°C to obtain 8.5 g of azithromycin lactate as a white solid. Take 0.25g of azithromycin lactate and put it into 100ml of water to fully dissolve, measure the pH value, and its pH value is 5.54.

[0015] 2. Azithromycin sulfate

[0016] Add 7.5 g of azithromycin and 10 ml of dilute sulfuric acid into a beaker filled with 40 ml of absolute ethanol, stir until the azithromycin is completely dissolved, and filter to obtain a c...

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PUM

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Abstract

Azithromycin is first reacted with equivalent organic or inorganic salt to produce water soluble salt, with it then further produced into eye drop, including eye tablet comprising the water soluble salt of Azithromycin and some medical supplementary material as well as special liquid comprising water, medical supplementary material and bacteriostat. When used, the eye tablet is thrown into the special liquid and the mixture liquid is shacked to obtain clear and transparent eye drop for dropping eye. Compared with available oral preparation, the eye drop is well soluble, low in dosage, direct absorbed in eye to reach the effective bacteriostasis density fast and other advantages.

Description

Technical field: [0001] The present invention relates to a water-soluble salt of an antibiotic and an eye drop formulated with the salt. Background technique: [0002] Azithromycin (Azithromycin, C 38 h 72 N 2 o 12 , molecular weight 748.99) is a kind of semi-synthetic macrolide antibiotic of azaza fifteen-membered ring, and its structural formula is as follows: [0003] Compared with the parent raw material erythromycin, azithromycin has the advantages of relatively stable acid, high concentration in body tissues, long duration of action, broad antibacterial spectrum, and low side effects. However, like erythromycin, its solubility in water is very small, and it cannot be directly made into eye drops to treat eye infections. The azithromycin disclosed in CN1046945C forms a water-soluble double salt with sodium dihydrogen phosphate, which can be used to process syrup, solution, transfusion, powder injection, water injection and the like. [0004] According to literat...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61P27/02
Inventor 黄小枫张承锋陈旭胡世林
Owner 安徽省新药研究院
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