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Water-soluble medicine degradable polymer microcapsule injecta and preparing method

A technology for water-soluble drugs and degradable polymers, applied in microcapsules, capsule delivery, pharmaceutical formulations, etc., can solve the problems of difficult microcapsules, difficult to obtain long-acting sustained release, and few research reports and applications of drug release carriers. Achieve the effects of controllable performance, good biocompatibility and degradability, and excellent stability

Inactive Publication Date: 2006-03-08
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

For polyester synthetic polymers, the main chain of the molecule is composed of hydrophobic C-C bonds and ester bonds, and its relative chemical inertness makes it difficult to directly obtain microcapsules through chemical reactions. Therefore, the hollow microcapsule drug release carrier There are few research reports and applications
However, due to the good water solubility and permeability of the capsule material, the microencapsulated drug carrier of natural polymer is difficult to obtain long-term sustained release performance.

Method used

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  • Water-soluble medicine degradable polymer microcapsule injecta and preparing method
  • Water-soluble medicine degradable polymer microcapsule injecta and preparing method
  • Water-soluble medicine degradable polymer microcapsule injecta and preparing method

Examples

Experimental program
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example 1

[0031] (1) Grind lactide and stannous chloride crystals into powder, add a certain amount of allyloxyglycol, place in a reaction vessel, deoxidize and charge nitrogen, close the vessel, where the amount of stannous chloride It is 0.8‰ of the weight of lactide, and the molar ratio of lactide / allyloxyethylene glycol is 55;

[0032] (2) The above reaction device is placed in an oil bath at 140°C, kept at a constant temperature for 8 hours, and then cooled down. Using acetone as a solvent and deionized water as a precipitant, the impurity is removed by dissolving-precipitation purification, and vacuum drying at 40°C to constant weight. Get polylactic acid with double bond, its H 1 NMR see figure 1 ;

[0033](3) Dissolve methacrylic acid with a concentration of 1g / ml in an aqueous solution containing water-soluble carbodiimide at 25°C and pH 7.0. The weight ratio of methacrylic acid to carbodiimide is 1:2, After stirring for 2 hours, the diethylaminoethyl dextran (DEAE dextran) aqueou...

example 2

[0039] (1) Grind lactide and stannous chloride crystals into powder, add a certain amount of allyloxyglycol, place in a reaction vessel, deoxidize and charge nitrogen, close the vessel, where the amount of stannous chloride It is 2‰ of the weight of lactide, and the molar ratio of lactide / allyloxyethylene glycol is 200;

[0040] (2) The above reaction device was placed in an oil bath at 200°C, kept at a constant temperature for 24 hours, and then cooled down. Using acetone as a solvent and deionized water as a precipitant, the impurity was removed through dissolution-precipitation purification, and vacuum dried at 40°C to constant weight. To obtain polylactic acid containing double bonds;

[0041] (3) Dissolve double bond-containing polylactic acid and divinylbenzene (DVB) in dichloromethane at room temperature. The concentration of polylactic acid in dichloromethane is 17mg / ml, and the weight of DVB accounts for 5 percent of the weight of polylactic acid containing double bonds. ...

example 3

[0045] (1) Synthesis of double bond-containing polylactic acid. Repeat steps (1) and (2) in Example 1, except that the amount of stannous chloride is 10‰ of the weight of lactide;

[0046] (2) Dissolve acrylic acid with a concentration of 1g / ml in an aqueous solution containing water-soluble carbodiimide at 25°C and pH 7.0. The weight ratio of acrylic acid to carbodiimide is 1:2. After stirring for 2 hours , Add chitosan HCl aqueous solution (pH 3.0) dropwise to the above solution. The weight ratio of chitosan to methacrylic acid is 1:10. After the addition, the solution is kept at constant temperature for 1 day and night. The resulting solution is centrifuged and filtered and placed After dialysis in three-distilled water for 7 days, it was freeze-dried to obtain chitosan containing double bonds;

[0047] (3) At room temperature, dissolve medical grade polylactic acid (molecular weight 50,000), double bond-containing polylactic acid and polyethylene glycol diacrylate in chlorofor...

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Abstract

The present invention discloses a degradable polymer microcapsule injection preparation of water soluble medicine and its preparation method. It uses polysaccharide containing double-bond and polylactic acid which have good biological compatibility and biological degradability as capsule shell material, utilizes the control of ratio of mixing polysaccharide and polylactic acid and adopts W10 / w emulsion polymerization technique to obtain the medicine microcapsule injection preparation whose grain size is 100-2000nm.

Description

Technical field [0001] The invention relates to a degradable polymer microcapsule injection reagent for water-soluble drugs and a preparation method thereof, in particular to one and multiple degradable polymers of medical grade polylactic acid, polysaccharides containing double bonds, and polylactic acid It is a nano-microcapsule injection preparation with a water-soluble drug as the core material and its preparation technology. Background technique [0002] The biodegradable polymer carrier occupies an extremely important position in the field of drug controlled release systems due to its unique and excellent properties (good degradation characteristics and low biological toxicity). Compared with common biodegradable polymer microsphere carriers, microcapsules have the following advantages: lower density and material consumption can reduce physiological toxicity to a certain extent; relatively larger drug loading space; at the same time, through Changes to the properties of the...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K31/496A61K38/18A61K38/38A61K47/36
Inventor 高长有江兵兵沈家骢
Owner ZHEJIANG UNIV
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