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Orally-taken tuckahoe polysaccharide sulfate-chitosan nanoparticle and preparation method thereof

A technology of chitosan nanoparticles and polysaccharides, applied in the field of medicine, can solve the problems of high quality specifications of film-forming materials, low encapsulation rate, and poor reproducibility, so as to reduce the risk of mucosal bleeding, prevent and treat vascular embolism, and process The effect of mild conditions

Inactive Publication Date: 2012-07-11
HEFEI CHENGEN BIOTECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

The preparation of liposomes has poor reproducibility, low encapsulation efficiency, instability, and high quality requirements for film-forming materials. At present, a small amount of liposomes is used in eye drops, aerosols, and external preparations in China

Method used

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  • Orally-taken tuckahoe polysaccharide sulfate-chitosan nanoparticle and preparation method thereof
  • Orally-taken tuckahoe polysaccharide sulfate-chitosan nanoparticle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0037] A kind of oral pachyrhin sulfate-chitosan nanoparticle, is characterized in that: when it is dissolved in the solution of 7zeta Potential<+40mV, dispersion coefficient<0.3;

[0038] It is made from the following raw materials: pachyan sulfate, chitosan and acetic acid; the weight ratio of chitosan and pachyan sulfate is 10:0.1-10, and the amount of said acetic acid needs to be able to completely dissolve chitosan sugar.

[0039] Described a kind of oral pachyan sulfate-chitosan nanoparticle, is characterized in that: described chitosan degree of deacetylation is greater than 60%, and its molecular weight is between 0.5-500,000 Da, and described acetic acid is The volume ratio is 0.1-1%.

[0040] Described a kind of oral pachysan sulfate-chitosan nanoparticle, is characterized in that: described chitosan deacetylation degree is greater than 90%.

[0041] Described a kind of oral pachysan sulfate-chitosan nanoparticle is characterized in that: described chitosan molecul...

Embodiment 2

[0049] 1, the preparation of pachyphyllan sulfate ester

[0050] (1) Poria cocos polysaccharide was extracted from traditional Chinese medicine Poria cocos by conventional alkali dissolution-acid precipitation method, and the content of polysaccharide detected by phenol-sulfuric acid method was 99.2%. The results of Soxhlet extraction and elemental analysis showed that no protein, nucleic acid and lipid substances could be detected in the obtained Poria cocos polysaccharide. The viscosity average molecular weight measured by viscosity method is 2.15×10 5 Da

[0051] (2) Add 240ml of pyridine to a 1000ml flat-bottomed flask, cool to 4°C and stir, slowly add 40ml of chlorosulfonic acid dropwise through a separatory funnel to prepare the sulfonation reagent;

[0052] (3) Add 12 g of pachyphyllan pre-swelled in dimethyl sulfoxide (100 ml) to the sulfonation reagent, and stir vigorously at 75-80 °C for 1 hour;

[0053] (4) Adjust the pH to 6 with 4N NaOH, distill off water and ...

Embodiment 3

[0063] 1, the preparation of pachyphyllan sulfate ester

[0064] (1) Poria cocos polysaccharide was extracted from the traditional Chinese medicine Poria cocos by conventional alkali dissolution-acid precipitation method, and the polysaccharide content was 98.8% detected by the phenol-sulfuric acid method. The results of Soxhlet extraction and elemental analysis showed that no protein, nucleic acid and lipid substances could be detected in the obtained Poria cocos polysaccharide. The viscosity average molecular weight measured by viscosity method is 1.98×10 5 Da

[0065] (2) Add 200ml of dimethylformamide (DMF) into a 1000ml pear-shaped bottle, heat it in a water bath to 80°C, add 90g of sulfamic acid and dissolve it completely;

[0066] (3) Add 30 g of polysaccharides, the molar ratio of sulfamic acid and monosaccharide residues of polysaccharides is 5:1, and the solid-liquid ratio (g:mL) of polysaccharides to DMF is 15:100; the pear-shaped bottle is connected to a rotary ...

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Abstract

The invention discloses an orally-taken tuckahoe polysaccharide sulfate-chitosan nanoparticle and a preparation method thereof. The preparation method comprises the following steps of: slowly adding a tuckahoe polysaccharide sulfate solution into a chitosan solution with stirring and continuously stirring, wherein at the same time, a mixed solution becomes turbid and a stable nano colloid solution is obtained; and spraying and drying the nano colloid solution by adopting a spraying and drying method at the high temperature of 70-120DEG C to obtain the orally-taken tuckahoe polysaccharide sulfate-chitosan nanoparticle. The nano-particle prepared by the preparation method is high in drug-loading rate, is small in particle size and is high in stability under the acidic environments of which the pH value is smaller than 7.5 and the temperature is about 37DEG C; and the nano-particle can be affined with small intestine and penetrates through the small intestine at the duodenum part in a form of complete nanoparticle and the medicament slowly releases in the blood.

Description

technical field [0001] The invention belongs to the field of medicine, and in particular relates to an oral pachyan sulfate-chitosan nanoparticle and a preparation method thereof. Background technique [0002] Polysaccharide sulfate is a polysaccharide derivative formed by substituting some hydroxyl groups on the monosaccharide molecules of the polysaccharide chain with sulfate groups. Polysaccharide sulfates can be roughly divided into two categories, one is natural sulfated polysaccharides, such as animal glycosaminoglycans, fucoidan sulfate, carrageenan, etc. Such drugs need to be obtained through separation and purification, the sources are limited, the purification process is complicated, the price is expensive, and the product quality is not easy to control. The other is artificial semi-synthetic products, which are rich in natural polysaccharides obtained through simple separation, and polysaccharide sulfate esters are obtained through sulfated structural modificatio...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/737A61K47/36A61P3/06A61P7/02A61P31/12A61P31/16A61P31/18A61P31/20A61P31/22A61P35/00
Inventor 陈群曹明成
Owner HEFEI CHENGEN BIOTECH
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