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A nanoparticle preparation for the treatment of brain diseases

A technology of nanoparticles and preparations, which can be used in blood diseases, antiviral agents, extracellular fluid diseases, etc., and can solve problems such as inability to generate surface charges

Active Publication Date: 2011-12-21
JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the shielding effect of the surface, after entering the endosome-lysosome, even in an acidic environment, the surface charge cannot be changed, so the endosome-lysosome escape into the cytoplasm cannot occur through charge attraction.

Method used

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  • A nanoparticle preparation for the treatment of brain diseases
  • A nanoparticle preparation for the treatment of brain diseases
  • A nanoparticle preparation for the treatment of brain diseases

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0240] Preparation of the geniposide nanoparticles modified by embodiment 1 chitosan

[0241] (1) Geniposide and hydrogenated castor oil are dissolved in water as the inner water phase, wherein the concentration of geniposide is 30g / L, and the concentration of hydrogenated castor oil is 10g / L;

[0242] (2) Polylactic acid-glycolic acid copolymer is dissolved in methylene chloride as an organic phase, and the concentration of polylactic acid-glycolic acid copolymer is 20g / L;

[0243] (3) polyvinyl alcohol and chitosan are dissolved in water as the external water phase, wherein the concentration of polyvinyl alcohol is 10g / L, and the concentration of chitosan is 4g / L;

[0244](4) Mix 0.5ml of the internal aqueous phase with 5ml of the organic phase, and make colostrum in an ice bath at 400W ultrasonic for 4 minutes;

[0245] (5) Immediately inject the colostrum into the 25ml external water phase, and make double milk in an ice bath at 200W ultrasonic for 2 minutes;

[0246] (6...

Embodiment 2

[0248] The preparation of embodiment 2 geniposide nanoparticles

[0249] (1) Geniposide and hydrogenated castor oil are dissolved in water as the inner water phase, wherein the concentration of geniposide is 30g / L, and the concentration of hydrogenated castor oil is 10g / L;

[0250] (2) Polylactic acid-glycolic acid copolymer is dissolved in methylene chloride as an organic phase, and the concentration of polylactic acid-glycolic acid copolymer is 20g / L;

[0251] (3) Polyvinyl alcohol is dissolved in water as the external water phase, wherein the concentration of polyvinyl alcohol is 10g / L;

[0252] (4) Mix 0.5ml of the internal aqueous phase with 5ml of the organic phase, and make colostrum in an ice bath at 200W ultrasonic for 4 minutes;

[0253] (5) Immediately inject the colostrum into the 25ml external water phase, and make double milk in an ice bath at 400W ultrasonic for 2 minutes;

[0254] (6) Inject the double emulsion into a large amount of 0.5% g / L polyvinyl alcoho...

Embodiment 3

[0256] Take 1 kg of gardenia coarse powder, add 6 times of water to decoct 3 times, each time for 30 minutes, filter, combine the decoction, concentrate to 1000 ml of thick paste (each 1 ml is equivalent to 1 g of medicinal materials), add 730 ml of 95% ethanol to contain Alcohol content 40%, stand for 24 hours, take the supernatant, recycle ethanol, concentrate to 500ml of thick cream with no alcohol smell (each 1ml is equivalent to 2g of medicinal materials), add 2700ml of 95% ethanol to alcohol content of 80%, stand for 24 hours, Filter, the filtrate is concentrated to a relative density of 1.05 to 1.10 (60° C.), and dried to obtain 130 g of dry cream. The content of total iridoid glycosides of geniposide is determined to be 55% by ultraviolet spectrophotometry, and the content of total iridoid glycosides of geniposide is determined by high-performance liquid phase. The glycoside content is 27.2%.

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Abstract

The invention discloses a nanoparticle preparation for treating brain diseases. The nanoparticle preparation comprises the following raw materials in part by weight: 10 to 250mg of geniposide or total iridoid glycoside of cape jasmine fruit serving as a medicament carried by the nanoparticle preparation; 50 to 300mg of polylactic acid-glycolic acid copolymer serving as a carrier of the nanoparticle preparation; and 200 to 500mg of polyvinyl alcohol and 1 to 30mg of tween-80 or hydrogenated castor oil serving as emulsifiers of the nanoparticle preparation. The invention also discloses the nanoparticle preparation, which is modified by chitosan, wherein the geniposide or total iridoid glycoside of cape jasmine fruit serves as a carried medicament of the nanoparticle preparation. The nanoparticle preparation is prepared by a multiple emulsion-solvent evaporation method. The preparation is administrated through nasal cavities, so the concentration of the geniposide or total iridoid glycoside of cape jasmine fruit in brain tissues is effectively increased. Compared with preparations prepared from the geniposide or total iridoid glycoside of cape jasmine fruit, which are administrated through gastrointestinal tracts, intramuscular injection and the like, the nanoparticle preparation has the advantages of small dosage and high patient compliance.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a nanoparticle preparation for treating brain diseases, which uses geniposide or total iridoid glycosides of gardenia as loaded drugs. Background technique [0002] Gardenia has the effects of clearing heat, purging fire, cooling blood, and detoxifying. It is often used in the treatment of heat syndrome in traditional Chinese medicine. Modern research has found that the total iridoid glycosides of Gardenia jasminoides represented by Geniposide is one of the main active ingredients of Gardenia jasminoides. Geniposide pure product is white powder, molecular formula: C 17 h 24 o 10 , Molecular weight: 388.366. Geniposide is easily soluble in water with a solubility of 0.18g·mL -1 , is a hydrophilic compound, easily soluble in polar organic solvents such as ethanol, acetone, n-butanol, and insoluble in lipophilic organic solvents such as chloroform, benzene...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/7048A61K36/744A61K47/34A61K47/44A61K47/36A61K9/12A61P25/00A61P9/10A61P7/04A61P7/02A61P9/00A61P31/22
Inventor 张海燕杨明汪建民万娜杨军宣芦乾
Owner JIANGXI UNIVERSITY OF TRADITIONAL CHINESE MEDICINE
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