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Composite nanometer particle obtained by coating curcumin eutectic crystal/piperine with polymers, and preparation of composite nanometer particle and application thereof to slow release pharmaceutical preparation

A technology of composite nanoparticles and curcumin coating, which is applied in the field of medicine, can solve problems such as the encapsulation rate of nanoparticles with difficult-to-coat structures, wide solid particle size distribution, and organic solvent residues, and achieve excellent dissolution rate and sustained release effect. Effect of improving productivity per unit time and good solubility

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

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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 nanoparticles or low encapsulation efficiency, and residual organic solvents in the preparation process, the present invention The second purpose is to provide a method for preparing the composite nanoparticles of the polymer-coated curcumin cocrystal / piperine, aiming to innovatively prepare the nanocomposite particles of the in-situ coating morphology

Method used

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  • Composite nanometer particle obtained by coating curcumin eutectic crystal/piperine with polymers, and preparation of composite nanometer particle and application thereof to slow release pharmaceutical preparation
  • Composite nanometer particle obtained by coating curcumin eutectic crystal/piperine with polymers, and preparation of composite nanometer particle and application thereof to slow release pharmaceutical preparation

Examples

Experimental program
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Effect test

Embodiment 1

[0054] Dispersion of curcumin-2-aminopyridine co-crystal compound and piperine into liquefied CO in the dark 2 Among them, the mass ratio of curcumin-2-aminopyridine cocrystal compound and piperine is 40:1. will CO 2 (containing curcumin-2-aminopyridine eutectic compound and piperine) is pumped into the autoclave, and after the temperature of the autoclave reaches 35° 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 polyvinylpyrrolidone with a concentration of 5 mg / ml, wherein the mass ratio of polyvinylpyrrolidone and curcumin-2-aminopyridine eutectic 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 size is 750nm, and the encapsulation efficiency is 72%.

[0055] Morphology analysis ...

Embodiment 2

[0058] Dispersion of curcumin-2-aminopyridine co-crystal compound and piperine into liquefied CO in the dark 2 Among them, the mass ratio of curcumin-2-aminopyridine cocrystal compound and piperine is 100:1. will CO 2 (containing curcumin-2-aminopyridine eutectic compound and piperine) is pumped into the autoclave, and after the temperature of the autoclave reaches 35° C., the pressure is the preset value of 20 MPa and stabilizes for 5 minutes, the flow rate of 0.5ml / min Pump in the poloxamer and hydroxypropyl cyclodextrin (poloxamer and hydroxypropyl cyclodextrin mass ratio is 1:1) polymer aqueous solution with a concentration of 20mg / ml, wherein the polymer aqueous solution and curcumin- The mass ratio of 2-aminopyridine co-crystal 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 ave...

Embodiment 3

[0060] Dispersion of curcumin-2-aminopyridine co-crystal compound and piperine into liquefied CO in the dark 2 Among them, the mass ratio of curcumin-2-aminopyridine cocrystal compound and piperine is 50:1. will CO 2 (containing curcumin-2-aminopyridine 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 15 MPa and stabilizes for 5 minutes, the flow rate of 1.5ml / min Pump in an aqueous solution of poloxamer with a concentration of 10 mg / ml, wherein the mass ratio of poloxamer to curcumin-2-aminopyridine cocrystal 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 710nm, and the encapsulation efficiency is 73%.

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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 / piperine with polymers. The composite nanometer particle comprises a core and a shell coating the core, wherein the core is a mixture of the curcumin eutectic crystal and the piperine; the shell is a hydrophilic polymer. The invention further 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 coatingstructure is successfully prepared by creatively utilizing a curcumin eutectic crystal compound through a supercritical fluid anti-solvent technology (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 phenolic pigment extracted from the rhizome of turmeric, a plant of the genus Curcuma longa in the family Zingiberaceae. It is widely used as a pigment and food additive, and curcumin plays an anti-inflammatory role based on protecting normal cells from various adverse factors. , anti-tumor, anti-oxidation, anti-bacterial, anti-viral and other biological activities and pharmacological effects, has broad prospects for drug application. However, curcumin has shortcomings such as strong hydrophobicity, low oral absorption, poor stability, and low bioavailability in vivo, which seriously affect its clinical use. [0003] At present, solving the insoluble problem of curcumin is a difficult problem of curcumin medicine. The method of improving the solubility and bioavailability of curcumin is mainly by prep...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/52A61K31/12A61K31/4525A61K47/10A61K47/32A61K47/40A61K47/22A61K47/12A61P29/00A61P31/04A61P31/12A61P35/00A61P37/02A61P39/06B82Y5/00
CPCA61K9/5138A61K9/5146A61K9/5161A61K31/12A61K31/4525A61K47/10A61K47/12A61K47/22A61P29/00A61P31/04A61P31/12A61P35/00A61P37/02A61P39/06B82Y5/00A61K2300/00
Inventor 刘晓忠靳奇峰郑和校李郡李楚雄
Owner MEDONCARE PHARMA CO LTD
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