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Composite nanoparticles of polymer coated curcumin eutectic/synergistic components, and preparation and application thereof in pharmacy

A composite nanoparticle and curcumin-coated technology, which is applied to medical preparations with non-active ingredients, polymer compound non-effective ingredients, medical preparations containing active ingredients, etc., can solve the problem of difficult to obtain coated structure nanoparticles, solid Wide particle size distribution, organic solvent residue and other problems, to achieve good solubility, increase yield per unit time, improve dissolution rate and oral bioavailability

Active Publication Date: 2019-04-09
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, low encapsulation efficiency, and residual organic solvents in the preparation process, etc.

Method used

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  • Composite nanoparticles of polymer coated curcumin eutectic/synergistic components, and preparation and application thereof in pharmacy
  • Composite nanoparticles of polymer coated curcumin eutectic/synergistic components, and preparation and application thereof in pharmacy

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Disperse the curcumin-2,5-dihydroxybenzoic acid eutectic compound and piperine at a mass ratio of 40:1 in the liquefied CO 2 middle. will CO 2 (containing curcumin-2,5-dihydroxybenzoic acid eutectic compound and piperine) is pumped into the autoclave, and after the temperature of the autoclave reaches 35°C and the pressure is the preset value of 10MPa and stabilizes for 5min, add 0.5ml The flow rate of / min was pumped into an aqueous solution of polyvinylpyrrolidone with a concentration of 5 mg / ml, wherein the mass ratio of polyvinylpyrrolidone and curcumin-2,5-dihydroxybenzoic acid eutectic compound was 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 710nm, and the encapsulation efficiency is 74%.

[0060] Morphology analysis of polymer-coated curcumin co-crys...

Embodiment 2

[0063] Disperse the curcumin-2-aminopyridine co-crystal compound and acarbose in the liquefied CO at a mass ratio of 100:1 in the dark 2 middle. will CO 2 (containing curcumin-2-aminopyridine eutectic compound and acarbose) 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 The flow rate pumped into the poloxamer aqueous solution with a concentration of 20 mg / ml, wherein the mass ratio of poloxamer and curcumin-2-aminopyridine cocrystal compound was 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 690nm, and the encapsulation efficiency is 70%.

Embodiment 3

[0065] Disperse the curcumin-4-aminophenol eutectic compound and piperine in the liquefied CO at a mass ratio of 40:1 in the dark 2 middle. will CO 2 (containing curcumin-4-aminophenol eutectic compound and piperine) is pumped into the autoclave, and after the temperature of the autoclave reaches 50° C., the pressure is the preset value of 10 MPa and stabilizes for 5 minutes, the flow rate of 0.5ml / min Pump in an aqueous solution of hydroxypropyl cyclodextrin with a concentration of 5 mg / ml, wherein the mass ratio of hydroxypropyl cyclodextrin and curcumin-4-aminophenol eutectic compound is 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 530nm, and the encapsulation efficiency is 72%.

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Abstract

The invention belongs to the field of medicines, and particularly relates to composite nanoparticles of polymer coated curcumin eutectic / synergistic components. The composite nanoparticles comprise acore and a shell coating the surface of the core, the core is a mixture of curcumin eutectic and synergistic components, and the shell is a hydrophilic polymer. The invention also discloses a preparation method and application of the composite nanoparticles. In the preparation method, the curcumin eutectic is innovatively utilized, and the composite nanoparticles with in-situ coated structures aresuccessfully prepared by supercritical antisolvent crystallization (SAS). The composite nanoparticles have superior solubility, 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, curcumin is a fat-soluble compound, insoluble in water, easily oxidized in vitro, less absorbed in the body, and metabolized too fast (elimination half-life in plasma is only 7.4min), poor stability, which restricts the clinical application of curcumin. widely used. [0003] In recent years, the dosage forms of curcumin mainly include microemulsions, microspheres, solid dispersions, liposomes, phospholipid complexes, micelles, nanoparticles, a...

Claims

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Application Information

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IPC IPC(8): A61K31/12A61K31/352A61K31/7036A61K31/4525A61K9/52A61K47/32A61K47/10A61K47/40A61K47/22A61K47/12A61P29/00A61P35/00A61P39/06A61P31/10A61P31/04A61P31/12A61P37/02
CPCA61K9/5138A61K9/5146A61K9/5161A61K31/12A61K31/352A61K31/4525A61K31/7036A61K47/10A61K47/12A61K47/22A61P29/00A61P31/04A61P31/10A61P31/12A61P35/00A61P37/02A61P39/06A61K2300/00
Inventor 刘晓忠靳奇峰郑和校李郡李楚雄
Owner MEDONCARE PHARMA CO LTD
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