Preparation method for porous slow-release microsphere of chitosan graft copolymer

A technology of slow-release microspheres and porous microspheres, which is applied in the directions of non-active ingredients, such as medical preparations, glycopeptide components, and drug combinations, can solve the problem of slow drug mass transfer rate, gel de-swelling response rate, and unsuitable for practical applications. , difficult to shape and other problems, to achieve the effect of controllable particle size and porosity, beneficial to curative effect, and improved release performance

Inactive Publication Date: 2014-08-06
EAST CHINA UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the disadvantage of sustained-release microspheres synthesized based on NPIAPAm is that they are too soft in the swollen state and difficult to shape; at the same time, the drug mass transfer rate and the gel deswelling response rate are slow, which is not suitable for practical applications.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] Chitosan: N-isopropylacrylamide: acrylamide is implemented in a mass ratio of 100:10:2.

[0014] (1) Preparation of porous chitosan microspheres

[0015] 1.0g chitosan is dissolved in the acetic acid solution of 100mL mass fraction 1%, adds the blocked polyethylene glycol porogen (water phase) of certain proportioning; Cyclohexane and n-hexanol mix by volume 11:6, Add a small amount of emulsifier to make an oil phase; mix the oil / water phase at a volume ratio of 17:4 and stir vigorously to make a reverse-phase suspension dispersion system; dropwise add epichlorohydrin solution to cross-link and solidify for 24 hours, separate by microsphere filtration, The obtained microspheres are soaked in distillation to remove the porogen, and the porous chitosan microspheres are washed repeatedly with distilled water and then dried.

[0016] (2) Preparation of chitosan-grafted poly(N-isopropylacrylamide / acrylamide) porous sustained-release microspheres

[0017] Add 60 mL of cyclo...

Embodiment 2

[0023] Chitosan: N-isopropylacrylamide: acrylamide is implemented in a mass ratio of 100:20:4.

[0024] The same steps as in Example 1 were adopted. When preparing chitosan grafted poly(N-isopropylacrylamide / acrylamide) porous sustained-release microspheres, chitosan microspheres (1.0g) were first swollen with potassium persulfate (APS) initiator solution for 30min, Then add the reaction system, flow nitrogen into the liquid phase for 30 minutes, start stirring, and then rapidly heat up to a certain reaction temperature under the protection of nitrogen. After 5 minutes, 0.20 g of N-isopropylacrylamide and 0.04 g of acrylamide were added to the polymerization reaction system in a semi-continuous feeding manner. After 5 hours of reaction, hydroquinone was added to terminate the reaction, and the product was obtained by filtration. The steps of product post-processing and drug embedding are the same as in Example 1.

[0025] The particle diameter of the microsphere is 5-20 μm, ...

Embodiment 3

[0027] Chitosan: N-isopropylacrylamide: acrylamide is implemented in a mass ratio of 100:30:6.

[0028] The same steps as in Example 1 were adopted. When preparing chitosan grafted poly(N-isopropylacrylamide / acrylamide) porous sustained-release microspheres, chitosan microspheres (1.0g) were first swollen with potassium persulfate (APS) initiator solution for 30min, Then add the reaction system, flow nitrogen into the liquid phase for 30 minutes, start stirring, and then rapidly heat up to a certain reaction temperature under the protection of nitrogen. After 5 minutes, 0.30 g of N-isopropylacrylamide and 0.06 g of acrylamide were added to the polymerization reaction system in a semi-continuous feeding manner. After 5 hours of reaction, hydroquinone was added to terminate the reaction, and the product was obtained by filtration. The steps of product post-processing and drug embedding are the same as in Example 1.

[0029] The particle diameter of the microsphere is 5-20 μm, ...

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Abstract

Provided is a preparation method for porous slow-release microspheres of chitosan grafting poly(N-isopropyl acrylamide / acrylamide). The method includes: first taking chitosan as a base material, adding a terminated polyethylene glycol porogenic agent, forming chitosan porous microspheres by inverse suspension dispersion and chemical cross-linking solidification, and conducting further graft copolymerizing with N-isopropyl acrylamide / acrylamide by taking the porous microspheres as substrates to obtain chitosan grafting poly(N-isopropyl acrylamide / acrylamide) porous slow-release microspheres. The microspheres have temperature sensitivity and a porous characteristic, and are uniform in pore distribution, good in dispersibility, controllable in particle size, and mild in preparation process. The microspheres can be used for embedding drug pingyangmiein. Using a microsphere dosage form helps to improve drug curative effects and reduce toxic and side effects.

Description

technical field [0001] The invention belongs to a drug slow-release dosage form, in particular to a porous slow-release microsphere which uses chitosan grafted poly(N-isopropylacrylamide / acrylamide) as a base material to coat the drug. Background technique [0002] Pingyangmiein (PYM) is widely used in the treatment of head and neck malignant tumors, and has a unique effect on squamous cell carcinoma. Its mechanism of action is to break the single strand of DNA in cells, reduce the solubility of DNA, inhibit mitosis, and combine with DNA to destroy it. However, PYM has irreversible side effects such as pulmonary fibrosis and inflammatory cell infiltration, which limits the dosage in chemotherapy. In order to change the biological distribution of Pingyangmycin in the body, improve the curative effect of the drug, and reduce toxic and side effects, the present invention uses chitosan-grafted poly(N-isopropylacrylamide / acrylamide) porous slow-release microspheres to load Pingy...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K38/14A61K47/48A61K47/36A61P35/00A61K31/722
Inventor 周利民
Owner EAST CHINA UNIV OF TECH
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