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Preparation method of cellulose-based insoluble or slightly soluble drug sustained-release microspheres

A technology of slow-release microspheres and cellulose, which is applied in drug delivery, pharmaceutical formulations, and medical preparations of non-active ingredients. It can solve problems such as limiting the development and application of functional materials, achieve high potential value, and solve slow-release problems. , good degradability effect

Active Publication Date: 2020-08-11
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the special structural properties of cellulose, it is insoluble in water and common organic solvents, which greatly limits its development and application as a functional material.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] A method for preparing cellulose-based water-insoluble or slightly soluble drug sustained-release microspheres of this embodiment comprises the following steps:

[0029] 1) 0.5g microcrystalline cellulose, 1.6g NaIO 4 Fully mix in the water system, avoid light and stir, the reaction temperature is 25-75°C, and the reaction time is 24h, then wash with deionized water and dialyze to obtain dialdehyde cellulose; disperse the dialdehyde cellulose in deionized water , heated at 100° C. for 1 h, centrifuged and concentrated to obtain a dialdehyde cellulose aqueous solution with a solid content of 107 mg / g; the dialdehyde cellulose aqueous solution was left to stand and sealed at 50-80° C. for 5 days to obtain nanoparticles.

[0030] 2) Take 50 mL of the nanocellulose solution obtained in step 1) (1% solid content) and 0.2 g of L-arginine, mix well, add 0.1 g of sodium borohydride and stir at room temperature for 2 h. Dialyze for 24 hours, centrifuge, and the supernatant is s...

Embodiment 2

[0034] The difference between Example 2 and Example 1 is: 2) Add 0.1 g of reducing agent sodium borohydride and stir at room temperature for 5 hours, then dialyze for 24 hours; 4) Transfer to a vacuum oven at 60°C for 24 hours to dry.

Embodiment 3

[0036] 1) Get 0.5g microcrystalline cellulose, 1.6g NaIO 4 Mix well in the water system, stir at room temperature for 24 hours in the dark, then wash with deionized water and dialyze to obtain dialdehyde cellulose;

[0037] 2) Take 50 mL of nanocellulose solution obtained in step 1) (solid content 1%) and 0.2 g of L-arginine, mix well, add 0.1 g of sodium borohydride and stir at room temperature for 6 h. Dialyze for 24 hours, centrifuge, and the supernatant is soluble oxidized cellulose.

[0038] 3) 5mL (0.5mol / L) of CaCl 2 Add to the positively charged cellulose-based hollow nanosphere solution obtained in step 2), let stand for 30min, then add 15mL (0.5mol / L) NaHCO under vigorous stirring 3 , stirred for 2h. After repeated centrifugation and ethanol washing, the cellulose-based mineralized microspheres are obtained.

[0039] 4) Add the poorly / slightly water-soluble drug soluble in ethanol to the mineralized microspheres obtained in step 3), shake for 12 hours, then trans...

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Abstract

The invention discloses a preparation method of cellulose base water-insoluble or slightly-soluble drug slow release microspheres. The preparation method comprises steps of performing oxidization withsodium periodates to obtain dialdehyde cellulose, and performing ageing on the dialdehyde cellulose at a certain temperature so as to obtain a nanocellulose solution; and performing reductamination with arginine or arginine salt so that dialdehyde cellulose DAC becomes cellulose base hollow nanometer microspheres with positive charges on the surface, then using the cellulose base hollow nanometermicrospheres as a nucleator, forming cellulose base mineralized microspheres, and finally, by a solvent evaporation method, enabling medicines which are soluble in ethanol but insoluble or slightly soluble in water to be packed in the microspheres, so as to prepare the drug slow release microspheres.

Description

technical field [0001] The invention belongs to the field of natural polymer materials, and in particular relates to a preparation method of cellulose-based insoluble or slightly soluble drug slow-release microspheres. Background technique [0002] Cellulose-based materials are a new type of renewable materials with high aspect ratio and specific surface area, high strength, high Young's modulus, good biocompatibility and ultra-fine structure, etc., with a diameter of 2-50nm Between them, the length can reach several microns, and the surface is rich in hydroxyl groups, which can be widely used in food, biology, enhancer, industrial purification, etc. However, due to the special structural properties of cellulose, it is insoluble in water and common organic solvents, which greatly limits its development and application as a functional material. Grafting modification on the surface of cellulose can improve and enhance its compatibility and dispersion in the substrate, and red...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/62A61K47/38A61K47/18
CPCA61K9/5015A61K9/5042
Inventor 曾宪海闫贵花孙勇唐兴雷廷宙林鹿
Owner XIAMEN UNIV
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