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Bismuth alginate and preparation method and application thereof

A technology of bismuth alginate and alginic acid is applied in the field of preparation of bismuth-containing compounds, which can solve the problems of inattention, non-negligible toxic and side effects, memory loss, etc., so as to reduce the activity of pepsin, improve the development value of new drugs, and promote the wound surface. healing effect

Active Publication Date: 2014-07-23
INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Long-term application of bismuth can cause dizziness, headache, numb hands, fatigue, irritability, inattention, memory loss, constipation, etc. Its toxic and side effects cannot be ignored, and it is potentially toxic and unsafe

Method used

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  • Bismuth alginate and preparation method and application thereof
  • Bismuth alginate and preparation method and application thereof
  • Bismuth alginate and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Preparation of bismuth alginate: first weigh 11 g of food-grade sodium alginate, add it to a container, and stir with 1500 ml of distilled water with a mixer until the sodium alginate is completely dissolved. Then adjust the pH to 8-12 with NaOH aqueous solution, continue to stir, and slowly add Bi(OH) 3 Aqueous solution (containing Bi 0.8g), continue to stir for 0.5-1 hour, and place the stirred solution at room temperature. Then add 95% ethanol that is 2-4 times (V / V) of the uniformly stirred solution, stir, colloid precipitates, press filter the precipitate, then wash the precipitate with ethanol for 2-3 times, vacuum freeze-dry, pulverize, and pass through 100 mesh Sieve to obtain bismuth alginate white powder (see figure 1 and figure 2 ), n=200-250 as shown in formula one. The obtained bismuth alginate contains 4-6% bismuth (by weight).

Embodiment 2

[0024] Weigh 10.5 g of sodium alginate, pour it into a container, add 1500 ml of water, and stir mechanically until it is completely dissolved to obtain a sodium alginate solution. Weigh bismuth nitrate (Bi(NO 3 ) 3 ·5H 2 O, containing Bi 2.0g), add water and stir until the bismuth nitrate is completely dissolved, then adjust the pH to 8-12 with NaOH solution; slowly add the bismuth nitrate alkaline solution into the sodium alginate solution while stirring, and continue stirring for 30-60min , and then add 1-3 times (V / V) ethanol to precipitate the bismuth alginate colloid, and centrifuge to separate the solid from the liquid. Add 95% ethanol to the precipitate to dehydrate and desalt the precipitate, then dry the precipitate, pulverize it, and pass through a 100-mesh sieve to obtain white powder bismuth alginate. The bismuth content in the bismuth alginate is 15-17%.

Embodiment 3

[0026] Weigh 10 g of sodium alginate, add it to a container, add 1500 ml of water, and stir mechanically until the sodium alginate is completely dissolved to obtain a sodium alginate solution. Weigh bismuth nitrate (Bi(NO 3 ) 3 ·5H 2 O, containing Bi 3.0g), add distilled water to dissolve, then add NaOH solution to get Bi(OH) 3 Precipitate, filter. Transfer the filter cake to a container, add 1-3 times (W / W) polyol, add water and stir until completely dissolved to obtain a basic bismuth solution; slowly add the bismuth alkali solution into the sodium alginate solution while stirring, and then continue Stir for 0.5-1 hour to form a colloidal salt. Then add 1-3 times (V / V) 95% ethanol, stir to precipitate bismuth alginate, and centrifuge. The precipitate was washed with 80% ethanol, dehydrated and desalted, and then the obtained precipitate was dried, pulverized, and passed through a 100-mesh sieve to obtain a white bismuth alginate powder. The powder contains 24-26% bismu...

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Abstract

The invention relates to preparation of a bismuth-containing compound, in particular to bismuth alginate and a preparation method and application thereof. The structure of the bismuth alginate is shown as Formula 1, wherein n is equal to 200-250. The bismuth alginate is prepared via reaction of algin and bismuth salt or bismuth alkali in alkaline aqueous solution, and the alginic acid is prepared via ethanol precipitation and separation, dehydration, drying and grinding. The bismuth alginate is synthesized with alginic acid as a bismuth carrier, the bismuth content of the bismuth-containing compound is lower than the bismuth content of bismuth preparations universally applied in clinics at present, and the potential toxicity of long-term administration of the bismuth can be reduced. Moreover, the bismuth-containing compound has the biological activity of both bismuth preparations and alginic acid and has multi-functions of protecting the gastric mucosa, neutralizing the gastric acid, reducing the activity of pepsin, killing Hp, and promoting healing of peptic ulcer wounds. Therefore, the bismuth-containing compound has good values in new drug development. Formula I is shown in the description.

Description

technical field [0001] The invention relates to the preparation of bismuth-containing compounds, in particular to a bismuth alginate and its preparation method and application. Background technique [0002] Chronic gastritis and gastric ulcer are common diseases, frequently-occurring diseases, and the recurrence rate is high, seriously endanger people's health. A large number of studies have fully proved that Helicobacter pylori (Hp) infection is the main cause of peptic ulcer. [0003] Bismuth preparations have astringent, antidiarrheal, and antiseptic effects, and can inhibit and kill bacteria, viruses, and spirochetes. Bismuth preparation is the only non-antibiotic drug that can directly kill Helicobacter pylori, which can overcome the primary drug resistance of Helicobacter pylori to antibiotics and avoid secondary drug resistance. Therefore, bismuth preparations are widely used in the treatment of gastric ulcer and eradication of Hp infection worldwide. [0004] Oral...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/734C08B37/04A61P1/04A61P31/04
Inventor 李宪璀朱校斌王新亭袁毅郭书举
Owner INST OF OCEANOLOGY - CHINESE ACAD OF SCI
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