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Ion cross-linked chitosan microballoon, its preparing process and use

A technology of chitosan microspheres and cross-linked chitosan, applied in sulfuric acid cross-linked chitosan microspheres, chitosan microspheres are used as pharmaceutically acceptable carriers for therapeutic agents, and the field of preparation of microspheres, It can solve the problems of weak ionic cross-linking strength and achieve the effects of avoiding toxicity or other side effects, convenient and economical preparation process, and good dispersibility

Inactive Publication Date: 2004-03-31
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

Although the choice of ionic crosslinking can avoid the toxicity or other side effects that chemical crosslinking may cause, how to solve the problems of weak ionic crosslinking strength, morphology, particle size distribution and dispersibility will be the key to the successful application of this method to chitosan. Prerequisites for Sugar Microspheres as Drug Sustained and Controlled Release Carriers

Method used

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  • Ion cross-linked chitosan microballoon, its preparing process and use
  • Ion cross-linked chitosan microballoon, its preparing process and use
  • Ion cross-linked chitosan microballoon, its preparing process and use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Get 10ml of chitosan solution of 5% (w / v), join it in the there-necked flask that 80ml liquid paraffin, 2ml Span83 are housed, then add the calcium stearate that dissolves in ether as dispersant, calcium stearate The quality of the solution is 50mg, after stirring for 10 minutes at 20°C and 600 rpm, add 5ml of 50% (W / W) sulfuric acid solution, then add 5ml of sulfuric acid solution at this concentration in 35 minutes, stop stirring after 70 minutes, and turn to 2500 Centrifuge under the condition of 1 / min, wash the solid product alternately and fully with volatile organic solvent and deionized water, and finally dry it under vacuum at 30°C. The particle size of the microspheres is 400-450 μm (>60%).

Embodiment 2

[0046] Get 20ml of chitosan solution of 4% (w / v), join it in the there-necked flask that 100ml sunflower oil, 4ml Span80 are housed, add the sulfuric acid solution of 15% (W / W) after stirring for 10 minutes at 40 ℃ 5ml, add 5ml of sulfuric acid solution of this concentration after 35 minutes, stop stirring after 60 minutes, centrifuge at 3000 rpm, wash the solid product alternately with petroleum ether, acetone and deionized water, and finally dry it under vacuum at 70°C. Can. The particle size of the microspheres is 150-300 μm (>70%).

[0047] From image 3 and Figure 4 It can be seen that, compared with the comparative example—the microspheres prepared by using sodium sulfate as cross-linking agent figure 2 Compared (the preparation method is the same as Example 2, the difference is only that the cross-linking agent is different), although the surface of the microspheres prepared in this embodiment is rough, it is denser, and the appearance is also relatively regular. C...

Embodiment 3

[0050] Get 10ml of chitosan solution of 4.5% (w / v), join it in the there-necked flask that 150ml liquid paraffin, 2ml Span80 and 1ml Tween60 (dissolved in 20ml petroleum ether) are housed, then add the stearin soluble in ether Acid is used as a dispersant, and the quality of calcium stearate is 100 mg. After stirring for 10 minutes at 30° C., add 5 ml of sulfuric acid solution of 25% (W / W), add 5 ml of sulfuric acid solution of this concentration in 20 minutes, and stop stirring after 120 minutes. Centrifuge at 4000 rpm, wash the solid product alternately with volatile organic solvents and deionized water, and dry it in vacuum at 40°C. The particle size of the microspheres is 20-40 μm (>80%).

[0051] From Figure 5 and Figure 6 It can be seen that, compared with using sodium sulfate as cross-linking agent ( figure 2 ) and the case of using sulfuric acid as crosslinking agent but without dispersant ( image 3 and Figure 4 ), the surface of the microspheres prepared in t...

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Abstract

An ion-exchanging chitosan microsphere, especially a chitosan microsphere cross-linked with sulfuric acid, the preparation method and a medicinal carrier of the chitosan microsphere cross-linked withsulfuric acid. The method relates to preparing chitosan microspheres by phase separation, comprises: first adding the chitosan solution into a nontoxic oil phase, then adding an emulsifying agent anda dispersing agent, adding sulfuric acid solution for cross-linking, after reaction, washing the resultant product, drying by vacuum and getting chitosan microsphere cross-linked with sulfuric acid. The microspheres of the invention are smooth, have the sphere configuration, could be used for a medicinal controllable carrier.

Description

technical field [0001] The present invention relates to a kind of ion cross-linked chitosan microsphere, relate in particular to a kind of sulfuric acid cross-linked chitosan microsphere, the preparation method of this microsphere, and this sulfuric acid cross-linked chitosan microsphere is used for As a pharmaceutically acceptable carrier for a therapeutic agent. Background technique [0002] The rapid development of modern biotechnology, molecular biology, and recombinant DNA technology has led to the emergence of a large number of protein and peptide drugs, some of which have entered the market or are in the regulatory review stage of the US FDA. For example, the global sales of erythropoietin and interferon drugs, which treat anemia-related diseases, have increased by 20% in recent years. Protein and peptide drugs generally cannot be taken orally, and are easily degraded by proteolytic enzymes in the body and gastrointestinal tract. Most peptide drugs are not easy to pa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36C08B37/08C08J3/24C08L5/08
Inventor 仰振球宋宝珍
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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