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

Technology for preparing dexamethasone sodium phosphate injection

A technology for preparing dexamethasone sodium phosphate and its preparation process, which is applied in the field of medicine and can solve the problems of unstable content of active ingredients and small recrystallized particle size of dexamethasone sodium phosphate injection, so as to avoid the reduction of drug efficacy and improve the degree of dispersion , the effect of increasing the yield

Inactive Publication Date: 2016-02-17
CHINA CHENGDU ANIMAL HUSBANDRY IND BIOPHARM
View PDF0 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by this invention is to provide the preparation technology of dexamethasone sodium phosphate injection, to overcome existing preparation method and cause the size of recrystallization particle in recrystallization process to be less, the dexamethasone sodium phosphate injection of making The problem of unstable content of active ingredients

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The preparation technology of dexamethasone sodium phosphate injection comprises the following steps:

[0029] 1) Synthesis of dexamethasone sodium phosphate: using dexamethasone acetate epoxy as the starting material, sequentially undergoing ring-opening reaction, recrystallization, alkali-catalyzed hydrolysis, pyrophosphoryl chloride esterification, neutralization and salt formation reaction to obtain dexamethasone sodium phosphate Dexamethasone sodium phosphate solution, the dexamethasone sodium phosphate solution is recrystallized again to obtain dexamethasone sodium phosphate crystals;

[0030] Ring-opening reaction: using dexamethasone acetate epoxy as the starting material, adding HF and DMF, the reaction temperature is -10°C, and the reaction time is 3 hours for ring-opening reaction to obtain dexamethasone acetate solution, dexamethasone acetate epoxy , HF, the mol ratio of DMF are 1:92:44;

[0031] The recrystallization: add acetone and Tween 80 to the dexame...

Embodiment 2

[0038] The preparation technology of dexamethasone sodium phosphate injection comprises the following steps:

[0039] 1) Synthesis of dexamethasone sodium phosphate: using dexamethasone acetate epoxy as the starting material, sequentially undergoing ring-opening reaction, recrystallization, alkali-catalyzed hydrolysis, pyrophosphoryl chloride esterification, neutralization and salt formation reaction to obtain dexamethasone sodium phosphate Dexamethasone sodium phosphate solution, the dexamethasone sodium phosphate solution is recrystallized again to obtain dexamethasone sodium phosphate crystals;

[0040] The ring-opening reaction: using dexamethasone acetate epoxy as the starting material, adding HF and DMF, the reaction temperature is -5°C, and the reaction time is 3h to carry out the ring-opening reaction to obtain the dexamethasone acetate solution, and the dexamethasone acetate ring The molar ratio of oxygen, HF, DMF is 1.5:94:48;

[0041] The recrystallization: add ace...

Embodiment 3

[0049] The preparation technology of dexamethasone sodium phosphate injection comprises the following steps:

[0050] 1) Synthesis of dexamethasone sodium phosphate: using dexamethasone acetate epoxy as the starting material, sequentially undergoing ring-opening reaction, recrystallization, alkali-catalyzed hydrolysis, pyrophosphoryl chloride esterification, neutralization and salt formation reaction to obtain dexamethasone sodium phosphate Dexamethasone sodium phosphate solution, the dexamethasone sodium phosphate solution is recrystallized again to obtain dexamethasone sodium phosphate crystals;

[0051] The ring-opening reaction: using dexamethasone acetate epoxy as the starting material, adding HF and DMF, the reaction temperature is 0°C, and the reaction time is 3h to carry out the ring-opening reaction to obtain the dexamethasone acetate solution, and the dexamethasone acetate epoxy The mol ratio of substance, HF, DMF is 2:95:50;

[0052] The recrystallization: add ethe...

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

No PUM Login to View More

Abstract

The invention relates to a technology for preparing a dexamethasone sodium phosphate injection. The technology includes the following steps that dexamethasone sodium phosphate is prepared, wherein dexamethasone acetate epoxide serves as a staring material, a dexamethasone sodium phosphate solution is obtained sequentially through a ring-opening reaction, recrystallization achieved through acetone or diethyl ether, base-catalyzed hydrolysis, pyrophosphoryl chloride esterification and a salt formation reaction achieved through neutralization, and the dexamethasone sodium phosphate solution is recrystallized to obtain a dexamethasone sodium phosphate crystal; the dexamethasone sodium phosphate crystal is subjected to ball milling to be powder after being dried; the dexamethasone sodium phosphate powder is dissolved with injection water to be diluted, and excipient and a disodium hydrogen phosphate solution are added to prepare the dexamethasone sodium phosphate injection. By means of the technology, the problems that according to an existing preparation method, recrystallized particles are small in the recrystallization process and the content of effective components of a prepared dexamethasone sodium phosphate injection is not stable are solved.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation process of dexamethasone sodium phosphate injection. Background technique [0002] Dexamethasone sodium phosphate, chemical name 16α-methyl-11β,17α,21 trihydroxy-9α-flupregna-1,4-diene-3,20-dione-21-phosphate disodium salt, It is an adrenocortical hormone drug with anti-inflammatory, anti-allergic, anti-rheumatic and immunosuppressive effects. The mechanism of action is: (1) Anti-inflammatory effect: it can reduce and prevent the response of tissues to inflammation, thereby reducing the manifestation of inflammation. It can inhibit the accumulation of inflammatory cells, including macrophages and leukocytes at the site of inflammation, and inhibit phagocytosis, the release of lysosomes, and the synthesis and release of inflammatory chemical mediators. (2) Immunosuppressive effect: including preventing or inhibiting cell-mediated immune response, delayed allergic ...

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
IPC IPC(8): A61K9/08A61K31/661A61K47/04A61K47/22A61K47/08A61P19/04A61P29/00A61P19/02A61P37/02A61P11/06A61P17/00A61P1/04A61P1/00A61P35/02A61P35/00C07J51/00
Inventor 廖成斌卢朝成
Owner CHINA CHENGDU ANIMAL HUSBANDRY IND BIOPHARM
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