Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Itraconazole enteric solid dispersion and preparation method and application thereof

A technology of solid dispersion and itraconazole intestine, applied in the field of medicine, can solve problems such as insignificant crystallization effect, and achieve the effects of no solvent residue, simple preparation method and excellent effect

Active Publication Date: 2017-05-10
GUANGZHOU NEWORLD PHARMA CO LTD
View PDF5 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Aiming at the bottleneck of crystallization in the gastrointestinal tract of amorphous solid dispersions, researchers have solved this problem by screening different carrier materials, but it is not obvious to inhibit the crystallization of drugs in the gastrointestinal tract simply by polymer carrier materials

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Itraconazole enteric solid dispersion and preparation method and application thereof
  • Itraconazole enteric solid dispersion and preparation method and application thereof
  • Itraconazole enteric solid dispersion and preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Example 1 Itraconazole enteric solid dispersion

[0044] An itraconazole enteric solid dispersion of this embodiment is prepared from the following components in weight percentage: 10% itraconazole, 80% enteric polymer carrier material, and 10% surfactant, wherein The enteric polymer carrier material is hypromellose phthalate, and the surfactant is poloxamer F188.

[0045] The preparation method of this itraconazole enteric-coated solid dispersion is as follows:

[0046] 1) Weigh 1.2g of itraconazole, 9.6g of hypromellose phthalate, and 1.2g of poloxamer F188, grind and mix them uniformly to make a physical mixture;

[0047] 2) Set the extrusion temperature of the twin-screw hot-melt extruder to 160°C, start the screw after reaching the preset temperature, and the screw speed is 150 rpm, and add the prepared physical mixture to the twin-screw hot-melt extruder In the process, the mixture is extruded in strips through the screw;

[0048] 3) The hot-melt extruded strip...

Embodiment 2

[0050] Example 2 Itraconazole enteric solid dispersion

[0051] A kind of itraconazole enteric solid dispersion of this embodiment is prepared from the following components by weight percentage: itraconazole 20%, enteric polymer carrier material 60%, surfactant 20%, wherein The enteric polymer carrier material is hypromellose acetate succinate (LF type), and the surfactant is sodium cholate.

[0052] The preparation method of the solid dispersion of this itraconazole is as follows:

[0053] 1) Weigh 2.4g of itraconazole, 7.2g of hypromellose acetate succinate (LF type), 2.4g of sodium cholate, grind and mix uniformly to make a physical mixture;

[0054] 2) Set the extrusion temperature of the twin-screw hot-melt extruder to 170°C, start the screw after reaching the preset temperature, and the screw speed is 100 rpm, and add the prepared physical mixture to the twin-screw hot-melt extruder In the process, the mixture is extruded in strips through the screw;

[0055] 3) The h...

Embodiment 3

[0056] Example 3 Itraconazole enteric solid dispersion

[0057] A kind of itraconazole enteric solid dispersion of this embodiment is prepared from the following components by weight percentage: itraconazole 36.4%, enteric polymer carrier material 50%, surfactant 13.6%, wherein The enteric polymer carrier material is acrylic resin (Eudragit L100-55), and the surfactant is Tween 80.

[0058] The preparation method of this itraconazole enteric-coated solid dispersion is as follows:

[0059] 1) Weigh 4.8g of itraconazole, 6.6g of acrylic resin (Eudragit L100-55), 1.8g of Tween 80, grind and mix evenly to make a physical mixture;

[0060] 2) Set the extrusion temperature of the twin-screw hot-melt extruder to 175°C, start the screw after reaching the preset temperature, and the screw speed is 120 rpm, and add the prepared physical mixture to the twin-screw hot-melt extruder In the process, the mixture is extruded in strips through the screw;

[0061] 3) The hot-melt extruded st...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

PUM

PropertyMeasurementUnit
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

The invention discloses itraconazole enteric solid dispersion and a preparation method and application thereof; the solid dispersion is prepared from itraconazole acting as an active ingredient, an enteric macromolecular carrier and a surfactant; the solid dispersion is prepared by means of hot-melt extrusion technology, and itraconazole is present in the solid dispersion in an amorphous form; experiments on in-vivo bioavailability for Beagle dogs indicate that the itraconazole enteric solid dispersion has relative bioavailability of 180% relative to a reference preparation (commercially available capsules); the enteric macromolecular carrier and the surfactant in the solid dispersion can improve dissolution degree of itraconazole, and can also inhibit the recrystallization of itraconazole in stomach and intestines, thereby improving bioavailability and reducing adverse effects.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an itraconazole enteric solid dispersion and a preparation method and application thereof. Background technique [0002] Itraconazole (English name: Itraconazole) has a chemical name of 4-[4-[4-[4-[[cis-2-(2,4-dichlorophenyl)-2-(1H-1,2 ,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(1RS) -1-methylpropyl]-1,2,4-triazol-3-one. Molecular formula: C 35 h 38 Cl 2 N 8 o 4 , molecular weight: 705.63, have following chemical structure: [0003] [0004] Itraconazole is a synthetic triazole derivative and a synthetic broad-spectrum antifungal drug. Its antibacterial spectrum is similar to ketoconazole. It exerts antibacterial activity by changing the permeability of fungal cell membranes. The pathogenic bacteria infected by fungi have antibacterial activity, which can inhibit the synthesis of ergosterol in fungal cell membranes, t...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to View More

Application Information

Patent Timeline
no application Login to View More
Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/496A61K47/38A61K47/10A61K47/28A61K47/32A61K47/26A61K47/20A61K47/22A61K47/34A61P31/10
CPCA61K9/145A61K9/146A61K31/496
Inventor 李革冯地桑陈航平王心怡周焕彬
Owner GUANGZHOU NEWORLD PHARMA CO LTD
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic, Popular Technical Reports.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com