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

A composition containing linezolid and its preparation method

A technology of linezolid and its composition, which is applied in the field of linezolid tablets and its preparation, can solve the problems of poor compressibility, easy change of linezolid crystal form, slow disintegration speed, etc., and achieves low cost and is suitable for industrial production , the effect of improving compliance

Active Publication Date: 2017-01-11
HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
View PDF6 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] The purpose of the present invention is to overcome the technical defects of linezolid in the existing process, such as easy crystal transformation, poor compressibility, and slow disintegration speed, and to provide a stable, good dissolution, simple operation, low cost, and high efficiency. The preparation process is suitable for industrialized large-scale production

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
  • A composition containing linezolid and its preparation method
  • A composition containing linezolid and its preparation method
  • A composition containing linezolid and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0030] Prescription (1000 tablets)

[0031]

[0032] Process:

[0033] The linezolid raw material is micronized together with mannitol, sodium bicarbonate and anhydrous citric acid to a suitable particle size (D90 is less than 30 μm).

[0034] First heat polyethylene glycol 4000 to melt (65°C±5°C), add Tween 80 and stir evenly, keep warm. Then put the above micronized mixture into a fluidized bed for fluidization, the air inlet temperature is 45-55°C, and at the same time spray the above molten liquid at a speed of 8-12g / min to prepare solvent-free spray particles. Then add crospovidone XL and silicon dioxide, mix evenly and press into tablets.

example 2

[0036] Prescription (1000 tablets)

[0037]

[0038] Process:

[0039] The linezolid raw material is micronized together with mannitol, sodium bicarbonate and anhydrous citric acid to a suitable particle size (D90 is less than 40 μm).

[0040] First heat polyethylene glycol 4000 to melt (65°C±5°C), add Tween 80 and stir evenly, keep warm. Then put the above micronized mixture into a fluidized bed for fluidization, the air inlet temperature is 50-60°C, and at the same time spray the above molten liquid at a speed of 5-8g / min to prepare solvent-free spray particles. Then add crospovidone XL and silicon dioxide, mix evenly and press into tablets.

example 3

[0042] Prescription (1000 tablets)

[0043]

[0044] Process:

[0045] The linezolid raw material is micronized together with mannitol, sodium bicarbonate and anhydrous citric acid to a suitable particle size (D90 is less than 30 μm).

[0046] First heat polyethylene glycol 4000 to melt (65°C±5°C), add Tween 80 and stir evenly, keep warm. Then put the above micronized mixture into a fluidized bed for fluidization, the air inlet temperature is 45-55°C, and at the same time spray the above molten liquid at a speed of 11-14g / min to prepare solvent-free spray particles. Then add crospovidone XL and silicon dioxide, mix evenly and press into tablets.

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
Login to View More

Abstract

The invention relates to a composition containing linezolid tablets, which is composed of mannitol, sodium bicarbonate, anhydrous citric acid, polyethylene glycol, Tween 80, crospovidone and silicon dioxide; the invention also discloses A method for preparing a linezolid composition was developed. After solvent-free spray granulation and ethylene glycol surface modification, the technical defects of linezolid crystal form IV easy to change crystal form and produce impurities were solved during the preparation process. . The linezolid composition disclosed by the invention, especially the linezolid tablet, has stable quality and good dissolution rate; the disclosed preparation method is simple in operation and low in cost, and is very suitable for industrial production.

Description

technical field [0001] The invention relates to the technical field of pharmaceutical preparations, in particular to a linezolid tablet and a preparation method thereof. Background technique [0002] Linezolid, a synthetic oxazolidinone antibiotic, was approved by the US FDA in 2000 for the treatment of infections caused by Gram-positive (G+) cocci, including suspected or confirmed hospital-acquired pneumonia (HAP) caused by MRSA, Community-acquired pneumonia (CAP), complicated skin or skin and soft tissue infection (SSTI), and vancomycin-resistant enterococci (VRE) infection. [0003] Linezolid is a bacterial protein synthesis inhibitor that acts on the bacterial 50S ribosomal subunit and is closest to the site of action. Unlike other drugs, linezolid does not affect the activity of peptidyl transferase, but only acts on the initial stage of the translation system, inhibits the connection between mRNA and ribosomes, prevents the formation of the 70S initiation complex, and...

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): A61K9/20A61K31/5377A61K47/26A61K47/02A61K47/12A61K47/34A61P31/04
Inventor 王琼吴红霞
Owner HANGZHOU HUADONG MEDICINE GRP PHARMA RES INST
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