Method for preparing biological degradable polymer drug-carried fine particle by supercritical anti-solvent process

A technology of biodegradable and drug-loaded particles, which is applied in the fields of chemical and biomedical engineering, can solve the problems of low melting point and high solubility, and achieve the effects of high yield, high biological activity and convenient operation

Inactive Publication Date: 2006-01-18
TONGJI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, RESS and PGSS have great limitations. The former is suitable for processing materials that are better soluble in supercritical fluids (such as fluorine-containing amorphous polymers and polyorganosiloxanes), and the latter is suitable for processing materials with low solubility in SCF. Large, low melting point and no thermally unstable substances

Method used

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  • Method for preparing biological degradable polymer drug-carried fine particle by supercritical anti-solvent process
  • Method for preparing biological degradable polymer drug-carried fine particle by supercritical anti-solvent process
  • Method for preparing biological degradable polymer drug-carried fine particle by supercritical anti-solvent process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Inject CO into the reactor 2 , adjust the pressure and temperature to a steady state (34°C, 14MPa). With 1g polylactic acid (L-PLA) and 0.1g norcantharidin (can be used for the treatment of primary liver cancer, the character is to be white crystalline powder; Aqueous solution shows acid reaction, easily soluble in acetone or hot water, in Slightly soluble in ethanol or cold water.) Dissolved in 50ml of dichloromethane to form a uniform and stable solution, wherein the concentration of polylactic acid is 20mg / ml, and the drug concentration of norcantharidin is 2mg / ml. Then the above solution was sprayed into the autoclave with a spray flow rate of 1ml / min. During the spraying process, the organic solvent swelled and the dissolving power was reduced, so that the original solute in the organic solvent was supersaturated to form a crystalline powder precipitate. After the solution was sprayed, CO was introduced into the reaction kettle. 2 , maintain the original pressure...

Embodiment 2

[0032] Inject CO into the reactor 2, adjust the pressure and temperature to a steady state (room temperature, 20MPa). 1g of polylactic acid (L-PLA) and 0.5g of norcantharidin were dissolved in 50ml of dichloromethane to form a uniform and stable solution, wherein the concentration of polylactic acid was 20mg / ml, and the concentration of norcantharidin was 10mg / ml. ml. Then the above solution was sprayed into the autoclave with a spray flow rate of 1ml / min. During the spraying process, the organic solvent swelled and the dissolving power was reduced, so that the original solute in the organic solvent was supersaturated to form a crystalline powder precipitate. After the solution was sprayed, CO was introduced into the reaction kettle. 2 , maintain the original pressure and temperature to wash the residual organic solvent, and the process lasts for 100 minutes. Finally, the pressure was slowly lowered for about 30 minutes, and the product was collected. The results of scannin...

Embodiment 3

[0034] The concentration of L-PLA was changed to 60 mg / ml, and other conditions were the same as in Example 1. The average particle size of the obtained microspheres was 3.562 μm, the standard deviation was 0.793 μm, and the drug encapsulation efficiency was 37.6%.

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Abstract

The invention relates to a process for preparing biodegradable polymeric medicine-carrying particles through supercritical fluid solvent-resisting procedure which mainly comprises the following steps, (1) letting CO2 into a crystallization reaction kettle and reaching a predetermined temperature and pressure, (2) spraying the polymer solution containing dissolved medicine into the reaction kettle through a purpose-made injector, depositing the particles, (3) collecting a certain amount of particles and stopping solution spraying, continuously letting in CO2 to purify the residual solvent, sustaining the procedure for 90-120 minutes, (4) finally evacuating under reduced pressure at operation temperature. The prepared submicron-sized particulate product has a grain size range of 0.5-5um.

Description

technical field [0001] The invention belongs to the field of chemistry and biomedical engineering, and specifically relates to a preparation method of polymer drug-loaded microparticles, in particular to a method for preparing biodegradable polymer drug-loaded microparticles through a supercritical antisolvent process. technical background [0002] In 1984, Krukonis first proposed supercritical fluid nucleation technology (Krukonis VJ. Supercritical Fluid Nucleation of Difficult to Comminute Solids [C]. Paper Presented at AIChE Meeting, San Francisco, CA, 1984, 11), the principle is to dissolve solid compounds in In supercritical fluid (SCF), when the system pressure is reduced, the compound is nucleated, crystallized and precipitated. Compared with traditional methods such as grinding, vapor deposition, liquid deposition, spray granulation, etc., the use of supercritical fluid deposition technology has high crystal purity, uniform particle size, good fluidity, and is suitab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K38/16A61J3/00C08J3/14
CPCY02P20/54
Inventor 任杰张鹏滕新荣
Owner TONGJI UNIV
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