Composite nanometer particle obtained by coating curcumin eutectic crystal with polymers, preparation of composite nanometer particle and application thereof to pharmacy

A technology of composite nanoparticles and curcumin coating, applied in the field of medicine, can solve the problems of low encapsulation rate of coated structure nanoparticles, wide solid particle size distribution, residual organic solvent, etc., to achieve excellent dissolution rate and sustained release effect, The effect of improving the yield per unit time and improving the dissolution rate

Active Publication Date: 2019-03-08
MEDONCARE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] In order to solve the technical problems of high energy consumption in the prior art, wide distribution of solid particle size obtained, difficulty in obtaining coated structure nanoparticles or low encapsulation efficiency, and residual organic solvents in the preparation process, etc.

Method used

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  • Composite nanometer particle obtained by coating curcumin eutectic crystal with polymers, preparation of composite nanometer particle and application thereof to pharmacy
  • Composite nanometer particle obtained by coating curcumin eutectic crystal with polymers, preparation of composite nanometer particle and application thereof to pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] Dispersion of curcumin-2-aminopyridine co-crystal compound into liquefied CO in the dark 2 middle. will CO 2 (containing curcumin-2-aminopyridine eutectic compound) is pumped into the autoclave, and after the temperature of the autoclave reaches the preset value of 35°C and the pressure is 10MPa and stabilizes for 5min, the concentration is pumped in at a flow rate of 0.5ml / min It is 5mg / ml PVP-k30 aqueous solution, wherein the mass ratio of PVP-k30 and curcumin-2-aminopyridine cocrystal compound is 5:1. After the solution is pumped, continue to pass through the CO 2 After 0.5h, stop feeding CO 2 , release the pressure, and collect the particles in the reactor to obtain the curcumin eutectic composition nanoparticles. Its average particle diameter is 610nm, and the encapsulation efficiency is 75%.

[0052] Morphology Analysis of Curcumin Co-crystal Composition Nanoparticles

[0053] Take a small amount of composite nanoparticles prepared in this case, add an appro...

Embodiment 2

[0055] Dispersion of curcumin-4-aminophenol co-crystal compound into liquefied CO in the dark 2 middle. will CO 2 (containing curcumin-4-aminophenol eutectic compound) is pumped into the autoclave, and after the temperature of the autoclave reaches the preset value of 35°C and the pressure is 10MPa and stabilizes for 5min, the concentration is pumped in at a flow rate of 1.0ml / min It is 15mg / ml PVP-k30 aqueous solution, wherein the mass ratio of PVP-k30 and curcumin-4-aminophenol eutectic compound is 20:1. After the solution is pumped, continue to pass through the CO 2 After 0.5h, stop feeding CO 2 , release the pressure, and collect the particles in the reactor to obtain the curcumin eutectic composition nanoparticles. Its average particle diameter is 890nm, and the encapsulation efficiency is 73%.

Embodiment 3

[0057] Dispersion of curcumin-2,5-dihydroxybenzoic acid co-crystal compound into liquefied CO in the dark 2 middle. will CO 2 (containing curcumin-2,5-dihydroxybenzoic acid eutectic compound) is pumped into the autoclave, and after the temperature of the autoclave reaches 35°C and the pressure is the preset value of 20MPa and stabilizes for 5min, the A F68 aqueous solution with a concentration of 20 mg / ml was pumped in at a flow rate, wherein the mass ratio of F68 and curcumin-2,5-dihydroxybenzoic acid eutectic compound was 10:1. After the solution is pumped, continue to pass through the CO 2 After 0.5h, stop feeding CO 2 , release the pressure, and collect the particles in the reactor to obtain the curcumin eutectic composition nanoparticles. Its average particle diameter is 730nm, and the encapsulation efficiency is 69%.

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Abstract

The invention belongs to the field of medicines, and particularly relates to a composite nanometer particle obtained by coating curcumin eutectic crystal with polymers. The composite nanometer particle comprises a core and a shell coating the surface of the core, wherein the core is the curcumin eutectic crystal and the shell is a hydrophilic polymer. The invention also discloses a preparation method and application of the composite nanometer particle. According to the preparation method provided by the invention, the composite nanometer particle with an in-situ coating structure is successfully prepared by creatively utilizing the curcumin eutectic crystal through a supercritical fluid anti-solvent method (SAS). The invention provides the composite nanometer particle with the advantages of better dissolution performance, stability and bioavailability.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to a curcumin co-crystal medicine. Background technique [0002] Curcumin is a polyphenolic compound extracted from the rhizome of the perennial herb turmeric. Traditional curcumin is generally used as food dyes and additives. In recent years, a large number of studies have shown that curcumin has a wide range of physiological activities. , such as lowering blood fat, anti-tumor, anti-inflammatory, choleretic, anti-oxidation, etc. However, the solubility of curcumin in aqueous environment is extremely poor and unstable; in addition, curcumin is also sensitive to light and heat, these factors greatly restrict the application of curcumin in different fields. [0003] Current methods for preparing curcumin nano-preparations include liposomes, micelles, nanoparticles, and nanofibers. Chinese patent CN 103550776 B discloses a hydrophobic drug nanoparticle, its preparation method and ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/12A61K47/32A61K47/10A61K47/40A61K47/22A61K47/12A61P29/00A61P31/04A61P31/12A61P35/00A61P37/02A61P39/06B82Y5/00
CPCA61K9/5138A61K9/5146A61K9/5161A61K31/12A61K47/10A61K47/12A61K47/22A61P29/00A61P31/04A61P31/12A61P35/00A61P37/02A61P39/06B82Y5/00
Inventor 刘晓忠靳奇峰郑和校李郡李楚雄
Owner MEDONCARE PHARMA CO LTD
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