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Preparation method of pH sensitiveness raphanin chitosan microsphere

A technology of chitosan microspheres and sulforaphane, which is applied in the direction of medical preparations, pharmaceutical formulas, anti-tumor drugs, etc. of non-active ingredients, to achieve the effects of simple and gentle experiments, improved bioavailability, and easy release

Inactive Publication Date: 2013-04-03
ZHEJIANG KUIRUI AGRI DEV CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] In the prior art, there is no report of using chitosan as a carrier and sodium tripolyphosphate as a cross-linking agent to prepare pH-sensitive sulforaphane-chitosan microspheres

Method used

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  • Preparation method of pH sensitiveness raphanin chitosan microsphere

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] 1) Dissolve chitosan powder with a degree of deacetylation of 91.2% in a 3% acetic acid solution to make the final concentration of chitosan in the solution reach 3mg / ml, adjust the pH value of the above solution to 5.0, and then in turn Filter through 85μm filter paper and 0.45μm filter membrane;

[0026] 2) Take an aqueous solution of sulforaphane at a concentration of 25mg / ml and add it to the chitosan acetic acid solution prepared in step 1) so that the final mass ratio of sulforaphane to chitosan in the solution is 1:2;

[0027] 3) Use a 7 gauge needle to drop 0.6 mg / ml of sodium tripolyphosphate solution into the mixed solution obtained in step 2) at 25°C and 300 rpm at a speed of 3 drops / sec to make the tripolyphosphate in the solution The final mass ratio of sodium to chitosan is 1:5, and stirring is continued for 1.2 hours to obtain sulforaphane-chitosan microspheres.

[0028] The sulforaphane chitosan microspheres have a particle size of 498.2nm, a Poly.Index of 0....

Embodiment 2

[0031] 1) Dissolve chitosan powder with a degree of deacetylation of 92% in a 1% acetic acid solution to make the final concentration of chitosan in the solution reach 0.5 mg / ml, adjust the pH of the above solution to 4.8, and then Filter by 80μm filter paper and 0.15μm filter membrane in turn;

[0032] 2) Take the 10mg / ml sulforaphane aqueous solution and add it to the chitosan acetic acid solution prepared in step 1), so that the final mass ratio of sulforaphane to chitosan in the solution is 1:1;

[0033] 3) At 10℃, 400rpm speed, use a 7 gauge needle to drop 0.4mg / ml sodium tripolyphosphate solution into the mixed solution obtained in step 2), the dropping rate is 5 drops / sec, so that the tripolyphosphate in the solution The final mass ratio of sodium to chitosan is 1:4, and stirring is continued for 1.5 hours to obtain sulforaphane-chitosan microspheres.

[0034] The sulforaphane chitosan microspheres have a particle size of 474.1nm, a Poly.Index of 0.613, a Zeta potential of 29...

Embodiment 3

[0037] 1) Dissolve chitosan powder with a degree of deacetylation of 95% in an acetic acid solution with a concentration of 5% to make the final concentration of chitosan in the solution reach 5.5 mg / ml, adjust the pH of the above solution to 4.8, and then Filter through 100μm filter paper and 0.55μm filter membrane in turn;

[0038] 2) Take an aqueous solution of sulforaphane with a concentration of 40mg / ml and add it to the chitosan acetic acid solution prepared in step 1) so that the final mass ratio of sulforaphane to chitosan in the solution is 1:4;

[0039] 3) Use a 7 gauge needle to drop 0.8 mg / ml sodium tripolyphosphate solution into the mixed solution obtained in step 2) at 30°C and 100 rpm rotation speed. The dropping rate is 1 drop / sec to make the tripolyphosphate in the solution The final mass ratio of sodium to chitosan is 1:6, and stirring is continued for 1 hour to obtain sulforaphane-chitosan microspheres.

[0040] The sulforaphane chitosan microspheres have a parti...

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Abstract

The invention discloses a preparation method of a pH sensitiveness raphanin chitosan microsphere. The preparation method comprises the following steps: 1) dissolving chitosan powder into an acetic acid solution; 2) taking a raphanin water solution and adding into the acetic acid solution; and 3) dropping a sodium tripolyphosphate solution into the mixture liquid obtained in the step 2) so as to obtain the raphanin-chitosan microsphere. The preparation method of the pH sensitiveness raphanin chitosan microsphere is reasonable in design, and the microsphere is prepared by using an ionic cross-linking method in a mode that the chitosan is taken as a carrier and the sodium tripolyphosphate is taken as a cross-linking agent, the experiment is simple and mild, and no organic solvents are used, so that the method is safe and environmental-friendly, a drug carrying microsphere solution of which the average particle size is 500 nm is successfully prepared, and moreover the prepared microsphere solution is good in stability and has no great change in particle size after being placed for a long time; under the acidic condition, the raphanin can be released more easily, and the higher the pH value is, the longer the releasing time is, and therefore the microsphere is an ideal slow release formulation of the raphanin.

Description

Technical field [0001] The invention belongs to a preparation method of a drug carrier, and specifically relates to a preparation method of pH-sensitive sulforaphane chitosan microspheres. Background technique [0002] Sulforaphane, also known as "sulforaphane", is produced by enzymatic or acid hydrolysis of glucoraphanin by myrosinase (EC 3.2.3.1). It is the strongest anti-cancer activity found in vegetables so far. Sulforaphane is an isothiocyanate compound in terms of its chemical composition, easily soluble in water, with a relative molecular mass of 177.3, and molecular formula C 6 H 11 S 2 NO, the structural formula is as follows: [0003] [0004] It is a multifunctional inducer that can induce the body to produce type II detoxification enzymes-glutathione transferase and quinone reductase. This enzyme can produce resistance to many carcinogens, thereby playing an anti-cancer effect. In addition, sulforaphane also has the ability to inhibit DNA deacetylase. In recent year...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K47/36A61K31/26A61P35/00
Inventor 吴元锋毛建卫黄俊
Owner ZHEJIANG KUIRUI AGRI DEV CO LTD
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