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A kind of chondroitin sulfate modified natamycin eye drops and preparation method thereof

A technology of chondroitin sulfate and natamycin, which is applied to medical preparations with no active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc., which can solve the problem of the large number of raw materials and the long-term efficacy of eye drops preparation technology Short, short ocular surface half-life and other issues, to achieve the effect of simple preparation process, enhanced compliance, and quick effect

Active Publication Date: 2022-08-05
SHENYANG XINGQI PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to overcome the shortcomings of the prior art, design and propose a kind of oxidized chondroitin sulfate modified natamycin eye drops and its preparation method, to solve the poor local corneal permeability of the existing antifungal eye drops , strong irritation, and high toxicity; overcome the shortcomings of the existing eye drops, such as short drug action time and frequent medication, prolong the short half-life of the ocular surface, enhance the compliance of patients with medication, and solve the problem of raw materials for the preparation of existing eye drops Numerous and complex issues

Method used

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  • A kind of chondroitin sulfate modified natamycin eye drops and preparation method thereof
  • A kind of chondroitin sulfate modified natamycin eye drops and preparation method thereof
  • A kind of chondroitin sulfate modified natamycin eye drops and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0039] The components and contents of the chondroitin oxysulfate-modified natamycin eye drops involved in this example are: in every 100 ml of phosphate buffer solution, the chondroitin oxysulfate-natamycin freeze-dried powder added The content is 10-80mg. The preparation method steps of the chondroitin oxysulfate-modified natamycin eye drops include three process steps: preparing chondroitin oxysulfate, preparing chondroitin oxysulfate-natamycin pharmaceutical granules, and preparing eye drops:

[0040] The first step is to prepare oxychondroitin sulfate:

[0041] (2) put 2~10g of chondroitin sulfate in every 100ml of deionized water, after dissolving, add 1~5g of sodium periodate, and continue stirring reaction at room temperature and dark condition for 12 hours to generate chondroitin sulfate oxide, The reaction formula is:

[0042]

[0043] (3) 0.5~2ml of ethylene glycol was added to the reaction solution obtained in step (1), and stirred for 5 minutes to quench the s...

Embodiment 2

[0053] The components and contents of the chondroitin oxysulfate-modified natamycin eye drops involved in this example are: in every 100 ml of phosphate buffer solution, the chondroitin oxysulfate-natamycin freeze-dried powder added The content is 40mg. The eye drops are prepared according to the process steps of Example 1:

[0054] The first step is to prepare oxychondroitin sulfate:

[0055] (1) 5g of chondroitin sulfate was dissolved in 100ml of deionized water, then 3.5g of sodium periodate was added, and the reaction was continuously stirred for 12 hours at room temperature and under the dark condition, and the reaction formula was:

[0056]

[0057] (2) 1ml of ethylene glycol was added to the reaction solution obtained in step (1), and stirred for 5 minutes to quench the sodium periodate in the reaction solution to terminate the oxidation reaction;

[0058] (3) 200ml of ethanol with a concentration of 75% was added to the reaction solution obtained in step (2), stir...

Embodiment 3

[0067] The present embodiment is prepared according to the process steps of Example 2, and the chondroitin oxysulfate and chondroitin oxysulfate-natamycin structures generated in the preparation process are detected, analyzed and identified:

[0068] The structure of chondroitin oxysulfate was detected by ultraviolet spectrum and X-ray photoelectron spectroscopy analysis: (1) For details of ultraviolet spectrum, please refer to the accompanying drawings in the description. image 3 : Chondroitin sulfate has obvious characteristic absorption peak, the maximum absorption wavelength is at 213nm, and the characteristic absorption peak of oxidative chondroitin sulfate has obvious chemical shift, and the maximum absorption wavelength is at 231nm. It shows that the oxidation reaction is successful and a new compound is formed. (2) For details of X-ray photoelectron spectroscopy, please refer to the accompanying drawings in the description. Figure 4 : The C1s spectrum of chondroitin...

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Abstract

The invention belongs to the technical field of medicine and material chemistry, and relates to a chondroitin sulfate-modified natamycin eye drop and a preparation method thereof. The components of the eye drop and its content are: , the content of the added chondroitin oxysulfate-natamycin freeze-dried powder is 10-80 mg, and the preparation method steps include: preparing chondroitin oxysulfate-natamycin granules, preparing chondroitin oxysulfate-natamycin drug granules, preparing eye drops Three process steps, the prepared chondroitin sulfate-natamycin is applied in ophthalmology to prepare eye drops for the treatment of fungal keratitis, the eye drops have strong water solubility, strong corneal penetration, and toxicity Small, anti-fungal, and anti-inflammatory, it directly acts on the ocular surface without releasing and degrading, and has quick effects, promotes the proliferation and migration of corneal epithelial cells, and promotes corneal epithelial repair. The preparation process is simple, easy to operate, and widely used.

Description

Technical field: [0001] The invention belongs to the field of medicine and material chemistry, and relates to a chondroitin sulfate-modified natamycin ophthalmic solution and a preparation method thereof, in particular to a natural biological polysaccharide chondroitin sulfate modified by chondroitin sulfate and natamycin. Chondroitin oxysulfate-natamycin eye drops, the prepared eye drops have strong water solubility, low toxicity, great antifungal and anti-inflammatory effects, and are used for the treatment of fungal keratitis. Background technique: [0002] Fungal keratitis is an inflammatory disease of the cornea caused by fungal infection, which can be caused by ocular trauma, chronic ocular inflammation and decreased body resistance. Eye disease, clinical treatment is more difficult. At present, most of the antifungal eye drops clinically used are lipid-soluble suspensions, which have problems such as poor local penetration of the cornea, strong irritation, high toxic...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/08A61K31/7048A61K31/737A61K47/55A61K47/02A61P27/02A61P29/00A61P31/10A61K47/61
CPCA61K9/0048A61K9/08A61K31/7048A61K47/02A61P27/02A61P31/10A61P29/00A61K31/737A61K47/55A61K47/61A61K9/19A61K2300/00
Inventor 赵桂秋彭旭东林静李翠田雪
Owner SHENYANG XINGQI PHARM CO LTD
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