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Method for improving natamycin by using rhizoma bletillae polysaccharide and application

A technology of natamycin and polysaccharide, which is applied in the field of improving natamycin and its application by Baiji polysaccharide, can solve the problems of poor solubility of natamycin, short drug action time, and short half-life of ocular surface, etc. Simple and easy to use, promotes the repair of corneal epithelium, and has a quick effect

Active Publication Date: 2021-12-14
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 method and application of improving natamycin with polysaccharides, to solve the problem of natamycin The problems of poor solubility and low corneal penetration solve the problems of many raw materials and complicated processes in the preparation of existing eye drops, and solve the problems of poor local corneal permeability, strong irritation and high toxicity in existing antifungal eye drops ; To overcome the shortcomings of the existing eye drops, such as the short duration of drug action and the need for frequent medication, to prolong the short half-life of the ocular surface and enhance the compliance of patients with medication

Method used

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  • Method for improving natamycin by using rhizoma bletillae polysaccharide and application
  • Method for improving natamycin by using rhizoma bletillae polysaccharide and application
  • Method for improving natamycin by using rhizoma bletillae polysaccharide and application

Examples

Experimental program
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Effect test

Embodiment 1

[0026] The method for improving natamycin by the Baihe polysaccharide involved in the present embodiment includes 5 process steps:

[0027] (2) Put 2~10g of Bletilla striata polysaccharide into every 200ml of phosphate buffer solution to make Bletilla striata polysaccharide solution, then add 2~10g of sodium periodate, and continue to stir and react for 12 hours at room temperature and in the dark , to obtain oxidized white and polysaccharide solution;

[0028] (3) 2ml of ethylene glycol was added to the oxidized white and polysaccharide solution obtained in step (1), and stirred for 5 minutes to quench the sodium periodate in the reaction solution to terminate the oxidation reaction;

[0029] (3) Dissolve 200-800 mg of natamycin in 40 ml of methanol, then drop it into the reaction solution prepared in step (2), and keep stirring for 12 hours at room temperature under the condition of avoiding light. Steps (2) and steps The reaction formula of (3) is:

[0030]

[0031] (4) ...

Embodiment 2

[0035] The method for improving natamycin by the Baihe polysaccharide involved in the present embodiment is implemented according to the process steps of Example 1:

[0036] (1) put 4g of Bletilla striata polysaccharide into every 200ml of phosphate buffer solution to make B. serrata polysaccharide solution, then add 4g of sodium periodate, and continue to stir and react for 12 hours at room temperature and dark conditions to obtain oxidized white glutinous rice. and polysaccharide solution;

[0037] (2) 2ml of ethylene glycol was added to the oxidized white and polysaccharide solution obtained in step (1), and stirred for 5 minutes to quench the sodium periodate in the reaction solution to terminate the oxidation reaction;

[0038] (3) 400mg of natamycin was dissolved in 40ml of methanol, and then dropped into the reaction solution prepared in step (2), under the condition of room temperature and dark, continuous stirring for 12 hours, step (2) and step (3) ), the reaction f...

Embodiment 3

[0044] This example is prepared according to the process steps of Example 2, and the obtained oxidized white and polysaccharide-natamycin (OBSP-NAT) is detected, analyzed and identified by infrared spectroscopy. Compare with polysaccharide (BSP), oxidized white and polysaccharide (OBSP): see the infrared spectrum in the accompanying drawings figure 2 : indicates that the oxidation reaction is successful and a new compound is formed.

[0045] The minimum inhibitory and bactericidal concentrations of the prepared OBSP-NAT and NAT were compared for the inhibition of Aspergillus fumigatus. For details, see image 3 : NAT can inhibit the growth of Aspergillus fumigatus by more than 90% at 8ug / ml; OBSP-NAT can inhibit the growth of Aspergillus fumigatus by more than 90% at 160ug / ml.

[0046] The cytotoxicity of corneal epithelial cells and mouse macrophages was compared between the prepared OBSP-NAT and NAT, see details Figure 4 : NAT began to appear epithelial cell toxicity at ...

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Abstract

The invention belongs to the technical field of medicine and material chemistry, and relates to a method for improving natamycin by using rhizoma bletillae polysaccharide and application. The preparation method of polyquercetin comprises the following five process steps: firstly, preparing an oxidized rhizoma bletillae polysaccharide solution, then adding ethylene glycol to terminate an oxidation reaction, adding a natamycin methanol solution to react to form an oxidized rhizoma bletillae polysaccharide-natamycin mixture, and preparing the oxidized rhizoma bletillae polysaccharide-natamycin freeze-dried powder through dialyzing and freeze-drying. The prepared oxidized rhizoma bletillae polysaccharide-natamycin freeze-dried powder is applied to the ophthalmology department for treating fungal keratitis and has the effects of high water solubility, high corneal penetrating power, low toxicity, great antifungal and anti-inflammatory effects and quick effect. The eye surface half-life period is prolonged, the administration frequency is reduced, the medication compliance of a patient is enhanced, the preparation process is simple, the raw material cost is low, and the preparation method is suitable for industrial production.

Description

Technical field: [0001] The invention belongs to the field of medicine and material chemistry, and relates to a method and application of improving natamycin by natural white and polysaccharide, especially using natural white and polysaccharide to improve natamycin to make oxidized white and polysaccharide-natamycin, which enhances The water solubility and antifungal effect of natamycin, oxidized white and polysaccharide-natamycin are used to treat fungal keratitis, and the prepared eye drops have strong water solubility, low toxicity, great antifungal and anti-inflammatory effects . Background technique: [0002] Fungal keratitis is a kind of corneal inflammatory disease caused by fungal infection. It can be caused by ocular trauma, chronic inflammation of the eye and decreased body resistance. It is a type of blinding disease caused by blinding fungal infection. Eye diseases are difficult to treat clinically. At present, most of the antifungal eye drops used clinically a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/08A61K31/7048A61K31/715A61K47/55A61K47/61A61P31/10A61P27/02A61P29/00
CPCA61K9/19A61K9/08A61K9/0048A61K31/7048A61K31/715A61K47/55A61K47/61A61P31/10A61P27/02A61P29/00A61K2300/00
Inventor 赵桂秋彭旭东王谦李翠张冉冉
Owner SHENYANG XINGQI PHARM CO LTD
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