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Regorafenib-coated nano-porous hydroxyapatite sustained-release microsphere as well as preparation method and application thereof

A technology of coating regorafenib and hydroxyapatite, which is applied in the field of nanoporous hydroxyapatite sustained-release microspheres and its preparation, can solve the problem of increased cumulative residues of drug molecules, side effects of patients, high drug concentration, etc. problem, to achieve the effect of increasing concentration, improving solubility and reducing damage

Active Publication Date: 2021-06-22
GUANGDONG MEDICAL UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the field of clinical medicine, although the traditional anti-cancer drug injection therapy is convenient and quick, and has a certain therapeutic effect, it will cause excessive local drug concentration in the body and cause damage. Because the human body metabolizes drug molecules quickly, the effective drug concentration in the body The retention time is short, which can only temporarily relieve the pain of the disease, and requires long-term repeated administration of drugs to the patient, which will lead to a continuous increase in the cumulative residue of drug molecules in the human body, thereby causing certain toxic and side effects to the patient

Method used

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  • Regorafenib-coated nano-porous hydroxyapatite sustained-release microsphere as well as preparation method and application thereof
  • Regorafenib-coated nano-porous hydroxyapatite sustained-release microsphere as well as preparation method and application thereof
  • Regorafenib-coated nano-porous hydroxyapatite sustained-release microsphere as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0024] A nanoporous hydroxyapatite slow-release microsphere coated with regorafenib, the preparation method of the slow-release microsphere comprises the following steps:

[0025] (1) Preparation of porous spherical calcium carbonate: Tween-80 is dissolved in the toluene of 0.5% in concentration, gets the mixed solution of 70ml toluene and Tween-80 in 30ml, in the sodium carbonate solution of 1mol / L, supersonic emulsification 11min; pour the emulsion into CaCl with a concentration of 0.2mol / L 2 solution, stirred for 2.5 hours, the obtained product was separated, filtered, rinsed repeatedly with distilled water, washed 3 times with absolute ethanol, and dried in an oven at 80°C for 10 hours to obtain porous spherical calcium carbonate powder;

[0026] (2) Preparation of porous hydroxyapatite: Weigh 1g of porous spherical calcium carbonate powder and add it into 200ml water to prepare a suspension, and mix 0.03mol / L Na 2 HPO 4 Add 200ml of the solution dropwise to the above su...

Embodiment 2

[0029] A nanoporous hydroxyapatite slow-release microsphere coated with regorafenib, the preparation method of the slow-release microsphere comprises the following steps:

[0030] (1) Preparation of porous spherical calcium carbonate: Tween-80 is dissolved in the toluene of 0.5% in concentration, gets the mixed solution of 70ml toluene and Tween-80 in 30ml, in the sodium carbonate solution of 1mol / L, supersonic emulsification 11min; pour the emulsion into CaCl with a concentration of 0.2mol / L 2 solution, stirred for 2.5 hours, the obtained product was separated, filtered, rinsed repeatedly with distilled water, washed 3 times with absolute ethanol, and dried in an oven at 80°C for 10 hours to obtain porous spherical calcium carbonate powder;

[0031] (2) Preparation of porous hydroxyapatite: Weigh 1g of porous spherical calcium carbonate powder and add it into 200ml water to prepare a suspension, and mix 0.03mol / L Na 2 HPO 4 Add 200ml of the solution dropwise to the above su...

Embodiment 3

[0034] A nanoporous hydroxyapatite slow-release microsphere coated with regorafenib, the preparation method of the slow-release microsphere comprises the following steps:

[0035] (1) Preparation of porous spherical calcium carbonate: Tween-80 is dissolved in the toluene of 0.5% in concentration, gets the mixed solution of 70ml toluene and Tween-80 in 30ml, in the sodium carbonate solution of 1mol / L, supersonic emulsification 11min; pour the emulsion into CaCl with a concentration of 0.2mol / L 2 solution, stirred for 2.5 hours, the obtained product was separated, filtered, rinsed repeatedly with distilled water, washed 3 times with absolute ethanol, and dried in an oven at 80°C for 10 hours to obtain porous spherical calcium carbonate powder;

[0036] (2) Preparation of porous hydroxyapatite: Weigh 1g of porous spherical calcium carbonate powder and add it into 200ml water to prepare a suspension, and mix 0.03mol / L Na 2 HPO 4 Add 200ml of the solution dropwise to the above su...

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Abstract

The invention relates to the field of drug sustained-release preparations, and in particular, relates to a regorafenib-coated nano-porous hydroxyapatite sustained-release microsphere as well as a preparation method and application thereof. The sustained-release microsphere disclosed by the invention contains 5 to 10 parts of regorafenib and 10 to 20 parts of nano-porous hydroxyapatite; the nano porous hydroxyapatite is modified by polyglutamic acid, polyaspartic acid or polylysine. The nano-porous hydroxyapatite is subjected to polyamino acid modification, so that the release rate of the active ingredient regorafenib can be effectively controlled, the drug release rate and the treatment effect are improved, the side effects of drugs on patients can be remarkably reduced, and the nano-porous hydroxyapatite has wide application prospects in the field of drug sustained-release carriers.

Description

technical field [0001] The invention relates to the field of drug sustained-release preparations, in particular to nanoporous hydroxyapatite sustained-release microspheres coated with regorafenib, a preparation method and application thereof. Background technique [0002] In modern society, cancer is one of the main factors threatening human life. The "World Cancer Report" released by the International Cancer Research Center (IARC) of the World Health Organization in 2014 predicts that global cancer cases will show a rapid growth trend, from 14 million in 2012 to 19 million in 2025 and 19 million in 2035. The annual population will reach 24 million. In such a severe situation, it is very important to find an effective treatment for cancer. In the field of clinical medicine, although the traditional anticancer drug injection therapy is convenient and quick, and has a certain therapeutic effect, it will cause excessive local drug concentration in the body and cause damage. B...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/34A61K47/04A61K47/59A61K47/52A61K31/44A61P35/00
CPCA61K9/1641A61K9/1611A61K31/44A61P35/00
Inventor 于凤波孟焕高俊霞王强崔燎黄春明张治平
Owner GUANGDONG MEDICAL UNIV
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