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Eye preparation containing lactose-azithromycin

A technology of azithromycin and lactobionic acid, which is applied in the field of pharmaceuticals, can solve the problems of loss of antibacterial activity, uneven drug dosage, eye irritation, etc., and achieve the effect of reducing re-pollution, no appearance and good stability

Inactive Publication Date: 2007-11-28
SHENYANG XINGQI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It shows that this patent fails to solve the stability problem of making a solution, and cannot make a kind of long-term stable eye drops
In addition, the preparation has obvious eye irritation, which is unbearable for most patients, which limits its application in ophthalmology
The combined preparation of "tablets + water" is more inconvenient to use: opening the bottle will cause re-contamination, differences in tablet weight and the size of the liquid medicine will cause uneven dosage, and foreign objects such as dust, Fine hair, etc. brought into eye drops, etc.
[0007] Studies have shown that both azithromycin and its acid salts have unstable factors, such as oxidation, hydrolysis, etc., which can lead to a decrease in their potency and loss of antibacterial activity, local toxicity such as increased toxicity to the liver, and increased toxicity to the vestibular system, resulting in tinnitus , hearing impairment, increased local irritation and allergic reactions, etc.
[0008] Limited to the instability of azithromycin and the irritation of ophthalmic preparations, there are no azithromycin eye drops, ophthalmic gels, etc. on the market at present in the domestic market. In terms of the stability of the ophthalmic preparations of azithromycin and its acid salts, it is technically impossible to guarantee the stability of azithromycin eye drops and ophthalmic gels within the validity period of 2 years, so there is only a 2-in-1 preparation of "tablet + water"

Method used

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  • Eye preparation containing lactose-azithromycin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1: Consists of the following components and mass percentages, which contain: azithromycin lactobionate 0.59% (as azithromycin 0.3%), sodium bisulfite 1.0%, povidone K 30 0.5%, hydrogenated castor oil 0.8%, medium chain glycerides 0.1%, Transcutol-p 0.4%, boric acid 1.0%, borax 0.2%, lactose 0.75%, ethyl paraben 0.03%, and the rest is water. The preparation process is the same as above.

Embodiment 2

[0041] Example 2: It is composed of the following components and mass percentages, which contains: 0.59% azithromycin lactobionate (0.3% as azithromycin), 0.6% vitamin C, and povidone K 30 0.5%, hydrogenated castor oil 0.8%, medium chain glycerides 0.1%, Transcutol-p 0.4%, boric acid 1.0%, borax 0.2%, lactose 0.75%, ethyl paraben 0.03%, and the rest is water. The preparation process is the same as above.

Embodiment 3

[0042] Example 3: Consists of the following components and mass percentages, which contain: azithromycin lactobionate 0.59% (0.3% as azithromycin), carbopol 0.5%, borax 1.4%, sodium bisulfite 1.0%, hydrogenated castor oil 1.5%, 0.3% medium chain glycerides, 0.6% Transcutol-p, 0.1% boric acid, 0.5% lactose, 0.03% ethyl paraben, and the rest is water. The preparation process is the same as above.

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PUM

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Abstract

The present invention is one kind of composition for eye medicine preparation. The composition contains antibiotic azithromycin lactobionate as active component; at least one kind of surfactant and / or co-surfactant, such as hydrogenated castor oil and Transcutol-p, in such amount as to form micro emulsion; and medicinal supplementary material, such as boric acid, borax and sodium bisulfite. The composition is prepared into eye drop or eye gel, and when it is prepared into gel, carbomer is used as the gel matrix. Compared with similar products, the composition of the present invention has high stability, less irritation to eye, capacity of be used to child and other advantages.

Description

Technical field [0001] The invention belongs to the field of medicine technology. [0002] The invention relates to an ophthalmic preparation composition prepared by an antibiotic drug-azithromycin lactobionate-plus medicinal auxiliary materials according to a conventional method, such as eye drops, ophthalmic gel and other dosage forms. The composition of the present invention relates to azithromycin lactobionate eye drops and azithromycin lactobionate eye gel. Background technique [0003] Azithromycin Lactobionate (Azithromycin Lactobionate) is a semi-synthetic aza-fifteen-membered macrolide antibiotic, its chemical name is (2R, 3S, 4R, 5R, 8R, 10R, 11R, 12S, 13S, 14R)-13-[(2,6-Dideoxy-3-C-methyl-3-O-methyl-(-L-nucleo-hexapyranosyl)oxy)-2-ethyl-3, 4,10-Trihydroxy-3,5,6,8,10,12,14-heptamethyl-11-[(3,4,6-tideoxy-3-(dimethylamino)-β-D- Wood-hexylpyranosyl)oxy]-1-oxa-6-azacyclopentadecan-15one 2 lactobionate, molecular formula C 38 H 72 N 2 O 12 ·2C 12 H 22 O 12 , Molecular weight...

Claims

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Application Information

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IPC IPC(8): A61K31/7052A61K47/44A61K9/00A61K9/08A61P27/02
Inventor 刘继东杨宇春宋长海
Owner SHENYANG XINGQI PHARM CO LTD
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