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

Preparation method of sustained-release microparticles, prepared sustained-release microparticles and applications thereof

A technology for slow-release microparticles and microparticles, which can be applied to medical preparations without active ingredients, medical preparations containing active ingredients, pharmaceutical formulas, etc., and can solve problems such as denaturation, aggregation and precipitation of active substances, and unstable release.

Active Publication Date: 2021-01-22
AC PHARMA CO LTD
View PDF12 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the process of volatilizing organic solvents to prepare solids is not conducive to temperature-sensitive active substances, which can easily cause their denaturation; if organic solvents are volatilized at lower temperatures, the active substances will aggregate and precipitate during solidification due to the slow volatilization of the solvent. The active substance in the final solid dispersion will also exist in a larger volume, such as block, ribbon, and filament, which will cause difficulties or waste in the subsequent preparation of fine particles, and will also lead to unstable release.

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
  • Preparation method of sustained-release microparticles, prepared sustained-release microparticles and applications thereof
  • Preparation method of sustained-release microparticles, prepared sustained-release microparticles and applications thereof
  • Preparation method of sustained-release microparticles, prepared sustained-release microparticles and applications thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0104] Example 1 Preparation of albiglutide / PLGA microparticles

[0105] (1) Preparation of solid dispersion

[0106] Dissolve 0.90g PLGA (molecular weight 25kDa, monomer ratio 65 / 35, carboxyl-terminated) in about 6.00mL glacial acetic acid, then add 0.10g albiglutide acetate, dissolve under vortex, and then slowly pour into a stirring In water ether (6°C), a white precipitate was produced, collected the white precipitate and extracted about 5 times with anhydrous ether, dried in a vacuum oven for 24 hours (10°C) after collecting the precipitate, to obtain a solid dispersion.

[0107] (II) Preparation of microparticles

[0108] The solid dispersion obtained in step I was uniformly dispersed in about 6.00 g of dichloromethane to obtain an internal oil phase, and then the internal oil phase was injected into 230 mL of 0.05% (w / w) lecithin / peanut oil that had been pre-warmed to about 4°C solution, and use a high-speed homogenizer to prepare S / O / O emulsion (rotor speed about 3...

Embodiment 2

[0109] Example 2 Preparation of dulaglutide / PLGA microparticles

[0110](1) Preparation of solid dispersion

[0111] Dissolve 0.95g PLGA (molecular weight 30kDa, monomer ratio 50 / 50, carboxyl-terminated) in about 7.92mL acetonitrile, then add 0.05g dulaglutide acetate, dissolve under vortex, and then slowly pour into the cyclohexane under stirring In alkanes (6°C), a white precipitate was produced, which was collected and extracted about 5 times with cyclohexane. After the collected precipitate was dried in a vacuum oven for 24 hours (10°C), a solid dispersion was obtained.

[0112] (II) Preparation of microparticles

[0113] The solid dispersion obtained in step I was uniformly dispersed in about 7.92 g of chloroform to obtain an internal oil phase, and then the internal oil phase was injected into 420 mL of a 0.1% (w / w) lecithin / liquid paraffin solution that had been pre-warmed to about 5°C , and use a high-speed homogenizer to prepare S / O / O emulsion (rotor speed about 3...

Embodiment 3

[0114] Example 3 Preparation of follicle stimulating hormone / PLA microparticles

[0115] (1) Preparation of solid dispersion

[0116] Dissolve 0.97g PLA (molecular weight 20kDa, terminal ester group) in about 5.39mL dimethyl sulfoxide, then add 0.03g follicle-stimulating hormone acetate, 0.05g xylitol and 0.03g zinc chloride, dissolve under vortex, Then it is slowly injected into n-hexane (8°C) under stirring to produce a white precipitate, which is collected and extracted about 5 times with n-hexane, and dried in a vacuum oven for 24 hours (10°C) after the precipitate is collected to obtain Solid dispersion.

[0117] (II) Preparation of microparticles

[0118] The solid dispersion obtained in step I was uniformly dispersed in a mixed solution of about 5.39 g of dichloromethane and chloroform to obtain an internal oil phase, and then the internal oil phase was injected into 410 mL of 0.25% (w / w ) lecithin / soybean oil solution, and emulsified using a turbine homomixer to p...

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
molecular weightaaaaaaaaaa
molecular weightaaaaaaaaaa
particle diameteraaaaaaaaaa
Login to View More

Abstract

A preparation method of sustained release microparticulates, comprising the following steps: 1) preparing a solid dispersion of water-soluble drug and biodegradable and biocompatible water-insoluble polymer; 2) dissolving the prepared solid dispersion in an organic solvent to obtain a solid dispersing emulsion; 3) injecting the obtained solid dispersing emulsion into an oil solution which contains surfactant to form a uniform emulsion; and 4) solidifying microparticulates in the emulsion by means of solvent volatilization or solvent extraction, collecting and washing the solidified microparticulates, and drying the microparticulates to obtain the sustained release microparticulates. The sustained release microparticulates prepared by the preparation method and use thereof in an implanted sustained release pharmaceutical composition. The whole process of the preparation method of the sustained release microparticulates is carried out at normal temperature or low temperature; the prepared sustained release microparticulates have a sustained-released effect close to zero order; the drug concentration is stable in the sustained release period.

Description

technical field [0001] The invention belongs to the field of water-soluble drugs, and in particular relates to a preparation method of sustained-release microparticles, the prepared sustained-release microparticles and the application of the sustained-release microparticles in implantable sustained-release pharmaceutical compositions. Background technique [0002] In recent years, a large number of biologically active substances such as oligopeptides, polypeptides and proteins have received a lot of attention as drug candidates, which play an important role in the treatment of serious conditions (cancer, anemia, multiple sclerosis, hepatitis, etc.). However, these macromolecular active ingredients are fragile because of their poor stability in the gastrointestinal tract (easily degraded by low pH or proteolysis), short circulating half-lives, and their poor permeability across the intestinal wall, leading to biological The availability is very low, making it difficult to adm...

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 Patents(China)
IPC IPC(8): A61K9/16A61K47/34A61K47/36A61K47/42A61K31/7088A61K38/16A61K38/20A61K38/22A61K38/24A61K38/26A61K38/29A61K38/35
CPCA61K9/0002A61K9/0024A61K9/1647A61K31/7088A61K38/16A61K38/20A61K38/22A61K38/24A61K38/26A61K38/29A61K38/35A61K9/16A61K47/34
Inventor 刘锋赖树挺郑阳曹付春连远发
Owner AC 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