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Preparation method of controlled-release drug-carried composite microsphere with small particle size and high mechanical strength

A technology of composite microspheres, mechanical strength

Inactive Publication Date: 2011-01-05
HUAIYIN INSTITUTE OF TECHNOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, this method must reduce the concentration of chitosan (generally about 1% to 2%) when preparing small particle size microspheres, especially when the particle size is less than 100 μm, which will not only lead to microsphere adhesion and uneven particle size distribution, but also due to shell With the decrease of polysaccharide content, the spheroidization and mechanical strength of the microspheres decreased, and the drug encapsulation efficiency and sustained release properties decreased.

Method used

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  • Preparation method of controlled-release drug-carried composite microsphere with small particle size and high mechanical strength
  • Preparation method of controlled-release drug-carried composite microsphere with small particle size and high mechanical strength
  • Preparation method of controlled-release drug-carried composite microsphere with small particle size and high mechanical strength

Examples

Experimental program
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Effect test

Embodiment 1

[0021] Example 1: Preparation of drug-loaded composite microspheres according to the following steps:

[0022] The attapulgite was added to a 37% hydrochloric acid solution with a mass concentration of 1:10 and soaked for 12 hours, filtered, washed with water to neutrality, and dried to obtain acidified attapulgite; 4g acidified attapulgite was dispersed in 100ml of deionized water, and 0.3g of ten was added. Hexaalkyltrimethylammonium bromide, ultrasonic for 15min, filtered and washed until no bromide ion is detected, dried and ground through a 200-mesh sieve to obtain organic attapulgite; weigh the chitosan with a molecular weight of 500,000 and a degree of deacetylation of 90% Sugar 7.5g, mixed with 1.5g organic attapulgite, grind for 30min, add 150ml of 1% acetic acid, slowly stir and swell for 10h at room temperature, then compound with 3000rpm stirring speed at 70℃ for 0.5h to obtain viscous chitosan / organic attapulgite Compound; Add 225ml liquid paraffin to the above compo...

Embodiment 2

[0023] Example 2: Preparation of drug-loaded composite microspheres according to the following steps:

[0024] The attapulgite was added to a 37% hydrochloric acid solution with a mass concentration of 1:10 and soaked for 12 hours, filtered, washed with water until neutral, and dried to obtain acidified attapulgite; 2g of acidified attapulgite was dispersed in 200ml of deionized water, and 0.04g was added. Octaalkyltrimethylammonium bromide, ultrasonic for 15min, filtered and washed until no bromide ion is detected, dried and ground through a 200-mesh sieve to obtain organic attapulgite; weigh the shell with a molecular weight of 400,000 and a degree of deacetylation of 80% 4g of polysaccharides, mixed with 2g of organic attapulgite, grind for 30min, add 100ml of 0.5% acetic acid and slowly stir and swell for 6h at room temperature, and then compound at 60℃ for 40min at a stirring speed of 2000rpm to obtain a viscous chitosan / organic attapulgite complex Add 200ml liquid paraffin ...

Embodiment 3

[0025] Example 3: Preparation of drug-loaded composite microspheres according to the following steps:

[0026] The attapulgite was added to a 37% hydrochloric acid solution with a mass concentration of 1:10 and soaked for 12h, filtered, washed with water until neutral, and dried to obtain acidified attapulgite; 3g purified attapulgite was dispersed in 100ml deionized water, and 0.45g ten Hexaalkyltrimethylammonium chloride, ultrasonic for 15min, filtered and washed until no chloride ion is detected, dried and ground through a 200-mesh sieve to obtain organic attapulgite; weigh the shell with a molecular weight of 600,000 and a degree of deacetylation of 85% 8g of polysaccharides, mixed with 3g of organic attapulgite, grind for 30min, add 133ml of 3% acetic acid, slowly stir and swell for 12h at room temperature, and then compound with 4000rpm stirring speed at 50℃ for 50min to obtain viscous chitosan / organic attapulgite complex Add 250ml liquid paraffin to the above compound, add...

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Abstract

The invention discloses a preparation method of a controlled-release drug-carried composite microsphere with small particle size and high mechanical strength, which comprises the following steps of: firstly, soaking attapulgite in hydrochloric acid to obtain acidified attapulgite, and organically modifying the acidified attapulgite by an ultrasonic method to obtain organic attapulgite; secondly, mixing the organic attapulgite with chitosan powder, grinding, adding a dilute acetum for swelling, and compounding in high-speed stirring to obtain a chitosan / organic attapulgite compound; thirdly, treating the chitosan / organic attapulgite compound by an emulsion-crosslinking method to obtain a controlled-release composite microsphere; and finally, adding the composite microsphere in a water solution or ethanol solution of a model drug, carrying the drug at room temperature, washing and drying to obtain the controlled-release drug-carried composite microsphere. The microsphere with great mechanical strength and small particle size between 30 and 100 mum is prepared by using the compatibility between the organic attapulgite and chitosan. Because of the dual embedding and controlled release actions of the attapulgite and the chitosan, the encapsulation rate, the drug carrying quantity and the controlled release property of the microsphere are effectively improved.

Description

Technical field [0001] The invention relates to a technology for preparing a sustained-release material, in particular to a method for preparing a small particle size, high mechanical strength sustained-release drug-loaded composite microsphere. Background technique [0002] In the traditional drug delivery system, the drug is released in the body once ingested by the human body, causing the concentration of the drug in the serum to fluctuate within a wide range, which not only brings unexpected side effects to the human body, but also leads to a decrease in the efficacy of the drug. In order to solve the above problems, drug sustained-release technology came into being. The key of this technology is to find a sustained and controlled release carrier that can be gradually degraded in the body without causing rejection in the human body. Among many sustained-release materials, chitosan As the only alkaline polysaccharide naturally occurring, sugar has become one of the most popula...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/46A61K47/36C09C1/42C09C3/06C09C3/08C08J3/24B01J13/14
Inventor 吴洁陈静喻春皓舒畅
Owner HUAIYIN INSTITUTE OF TECHNOLOGY
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