Chitosan drug carrying microsphere with uniform size, high embedding rate and high drug activity maintaining rate and its preparation process

A technology of drug-loaded microspheres and drug activity, which can be used in pharmaceutical formulations, medical preparations of inactive ingredients, and bulk delivery, etc. Good reproducibility, uniform particle size, mild conditions

Inactive Publication Date: 2005-11-23
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] This technology solves the problems of non-uniform particle size, low embedding rate, easy inactivation of active drugs and difficulty in release of chitosan drug carriers prepared by traditional stirring emulsification method and cross-linking method.

Method used

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  • Chitosan drug carrying microsphere with uniform size, high embedding rate and high drug activity maintaining rate and its preparation process
  • Chitosan drug carrying microsphere with uniform size, high embedding rate and high drug activity maintaining rate and its preparation process
  • Chitosan drug carrying microsphere with uniform size, high embedding rate and high drug activity maintaining rate and its preparation process

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] The hydrophobic membrane with a pore size of 4.7 μm is immersed in a lipophilic substance to fully wet the porous membrane to ensure that the hydrophobic chains on the membrane are completely stretched. Prepare the acetic acid-sodium acetate buffer solution of pH3-5, add a certain amount of NaCl and make it dissolve under stirring, its concentration is 0.9wt%, then add a certain amount of chitosan and make its concentration be 1.5wt%, wait for it After complete dissolution, the solution was centrifuged to remove impurities for later use. Add the oil-soluble emulsifier to 60 ml of the mixed oil phase of liquid paraffin and petroleum ether, and stir until completely dissolved to form the oil phase. Put 6.0g of water phase at 0.134kgf / cm 2 Under a constant pressure, press it into the oil phase through a hydrophobic microporous membrane with a uniform pore size to obtain a W / O emulsion; slowly add a certain amount of TPP aqueous solution to the obtained emulsion for gelati...

Embodiment 2

[0035] The hydrophobic membrane with a pore size of 4.7 μm is immersed in a lipophilic substance to fully wet the porous membrane to ensure that the hydrophobic chains on the membrane are completely stretched. Prepare acetic acid-sodium acetate buffer solution with pH 3-5, add a certain amount of NaCl and dissolve it under stirring, the concentration is 0.9wt%, then add a certain amount of hydrophilic drug insulin, and add a certain amount after the drug is completely dissolved The concentration of chitosan is 1.5wt%. After it is completely dissolved, the solution is centrifuged to remove impurities for subsequent use. Add the oil-soluble emulsifier to 60 ml of the mixed oil phase of liquid paraffin and petroleum ether, and stir until completely dissolved to form the oil phase. Put 6.0g of water phase at 0.134kgf / cm 2 Under a constant pressure, press it into the oil phase through a hydrophobic microporous membrane with a uniform pore size to obtain a W / O emulsion; slowly add ...

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Abstract

The invention provides a chitosan drug carrying microsphere with uniform size, high embedding rate and high drug activity maintaining rate characterized in that the embedding ratio of the medicament can be as high as over 75%, the activity sustaining ratio of the active medicament can reach 95%, and it can be released stably externally. The invention is also characterized that hydrophilic medicament is dissolved into the acetate-sodium acetate buffer solution of chitosan, the aqueous phase is pressed into the oil phase with pressure through microporous membrane, the obtained milk-like droplet with uniform dimension is subject to cross bonding solidification through two-step hardening.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations of medical engineering Background technique [0002] With the development of biotechnology and genetic engineering, more and more biologically active proteins and polypeptides have become drugs for disease prevention and treatment, but these biologically active drugs have many defects when used alone, and they are easily absorbed by enzymes in the body. This will lead to a significant reduction in its bioavailability in the body, and at the same time, the circulation half-life of this type of drug is short, resulting in frequent medication, causing large fluctuations in blood drug concentration in the body, and serious side effects. Therefore, it is very necessary to make these biologically active drugs into sustained-release systems. Up to now, many sustained-release systems have been applied to the research of active substances such as proteins and polypeptides, including PEGylation, c...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36
Inventor 马光辉苏志国王连艳
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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