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Intelligent multifunctional hollow microsphere capable of quickly releasing medicine in acid environment and preparation method for intelligent multifunctional hollow microsphere

A hollow microsphere, intelligent technology, applied in the direction of microsphere preparation, drug combination, pharmaceutical formulation, etc., can solve the problem of destroying drug activity, etc., and achieve the effect of wide application prospect, dense and smooth surface, and simple method

Active Publication Date: 2012-02-22
WUXI ZHONGKE GUANGYUAN BIOMATERIALS
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

By modifying the carboxyl group (forming an ester bond, an amide bond, etc.), the drug is covalently bonded to the carrier to form a prodrug, and after entering the body, the introduced water-soluble covalent group is hydrolyzed to generate the original drug and play a role, but this Methods that may destroy drug activity

Method used

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  • Intelligent multifunctional hollow microsphere capable of quickly releasing medicine in acid environment and preparation method for intelligent multifunctional hollow microsphere

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043](1) Preparation solution: prepare chloroform solution of PLGA (5mg / mL), PVA (5.0mg / mL) aqueous solution containing sodium bicarbonate (2.5mg / mL), and PVA (5.0mg / mL) without sodium bicarbonate ) aqueous solution. Among them, the weight-average molecular weight of PLGA is 50,000, the molar ratio of chain segments is 40:60, and the weight-average molecular weight of PVA is 20,000.

[0044] (2) Preparation of water-in-oil emulsion: Mix 1mL of PVA aqueous solution containing sodium bicarbonate with 2mL of PLGA in chloroform, and use an ultrasonic instrument to complete emulsification in an ice-water bath at a power of 35W for 2 minutes to form water-in-oil lotion.

[0045] (3) Preparation of water-in-oil-in-water double emulsion: the emulsion obtained in (2) is transferred to 6 mL of PVA aqueous solution without sodium bicarbonate, and homogenized at a rate of 5000 rpm with a PT-1200 homogenizer in an ice-water bath A W / O / W double emulsion was obtained in 30 minutes.

[00...

Embodiment 2

[0050] (1) Preparation solution: prepare PLGA (1.0mg / mL) acetone solution, PVA (1.0mg / mL) aqueous solution containing sodium bicarbonate (8.0mg / mL), and PVA (20mg / mL) without sodium bicarbonate ) aqueous solution. Among them, the weight-average molecular weight of PLGA is 1 million, the molar ratio of chain segments is 80:30, and the weight-average molecular weight of PVA is 250,000.

[0051] (2) Preparation of water-in-oil emulsion: Mix 15mL of PVA aqueous solution containing sodium bicarbonate with 60mL of PLGA in acetone, and use an ultrasonic instrument to complete emulsification in an ice-water bath at a power of 10W for 0.5min to form water-in-oil lotion.

[0052] (3) Preparation of water-in-oil-in-water double emulsion: transfer the emulsion obtained in (2) to 2 mL of PVA (20 mg / mL) aqueous solution without sodium bicarbonate, and use a PT-1200 homogenizer in an ice-water bath Homogenize at 12000 rpm for 80 minutes to obtain a W / O / W double emulsion.

[0053] (4) Soli...

Embodiment 3

[0057] (1) Preparation solution: prepare a dichloromethane solution of PLGA (20mg / mL), an aqueous solution of polyoxyethylene amine (15mg / mL) containing sodium bicarbonate (1.0mg / mL), and a polyoxyethylene solution without sodium bicarbonate Vinylamine (1.0 mg / mL) in water. Among them, the weight-average molecular weight of PLGA is 2 million, the molar ratio of chain segments is 90:10, and the weight-average molecular weight of polyoxyethylene amine is 200,000.

[0058] (2) Preparation of water-in-oil emulsion: Mix 10 mL of polyoxyethylene amine aqueous solution containing sodium bicarbonate with 30 mL of PLGA in dichloromethane, and use an ultrasonic instrument to complete emulsification in an ice-water bath at a power of 150 W for 12 minutes. A water-in-oil emulsion is formed.

[0059] (3) Preparation of water-in-oil-in-water double emulsion: transfer the emulsion obtained in (2) to 70 mL of polyoxyethylene amine (1.0 mg / mL) aqueous solution without sodium bicarbonate, and ...

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Abstract

The invention belongs to the field of medicinal preparations, and relates to the fields of biodegradable high polymer materials and medicine control release, in particular to an acid sensitive and biocompatible intelligent hollow microsphere and a preparation method thereof. Weak alkaline salt is coated in a polylactic acid-glycollic acid copolymer microsphere by an emulsification method, a defect that the activity of a medicine is possibly damaged due to covalent connection of the medicine and the microsphere is overcome, the weak alkaline salt is reacted with hydrogen ions in cells to form carbon dioxide, the pressure in the microsphere is increased through the continuously generated carbon dioxide, the shell of the microsphere is cracked, and the medicine is quickly released. The hollow microsphere prepared by the method has a wide application prospect in the field of medicine release.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, relates to the field of biodegradable polymer materials and the field of drug controlled release, in particular to an acid-sensitive and biocompatible intelligent hollow microsphere and a preparation method thereof. Background technique [0002] Poly(lactic-co-glycolic acid), also known as poly(lactic-co-glycolic acid), PLGA, has excellent biocompatibility and biodegradability, and contains hydrophilic groups , which can be biodegraded into carbon dioxide and water in the body without obvious disintegration phenomenon, so it is widely used as a drug carrier in a drug controlled release system. The typical drug release mode of the carrier is diffusion release and degradation release. However, the degradation time of the polymer is long, which may be as long as several days or even several months, so the drug release process of PLGA carriers is generally relatively slow. Therefore, the ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K47/34B01J13/02A61P35/00
Inventor 韩志超许杉杉
Owner WUXI ZHONGKE GUANGYUAN BIOMATERIALS