Preparation technology of dexamethasone sodium phosphate injection

A technology of dexamethasone sodium phosphate and a preparation process, applied in the field of medicine, can solve the problems of low yield, fast reduction of efficacy of active ingredients, etc., and achieve the effects of easy availability of raw materials, avoiding reduction of efficacy and improving yield

Inactive Publication Date: 2016-02-24
CHINA CHENGDU ANIMAL HUSBANDRY IND BIOPHARM
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  • 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 a kind of preparation technology of dexamethasone sodium phosphate injection, to overcome the lo

Method used

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] A preparation process for dexamethasone sodium phosphate injection, comprising the following steps:

[0026] 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;

[0027] 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;

[0028] Recrystallization: add acetone or ether to the dexamethasone ac...

Embodiment 2

[0035] A preparation process for dexamethasone sodium phosphate injection, comprising the following steps:

[0036] 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;

[0037] 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;

[0038] The recrystallization: add aceto...

Embodiment 3

[0045] A preparation process for dexamethasone sodium phosphate injection, comprising the following steps:

[0046]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;

[0047] 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;

[0048] The recrystallization: add acetone...

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Abstract

The invention relates to a preparation technology of dexamethasone sodium phosphate injection. The preparation technology comprises the following steps: synthetizing dexamethasone sodium phosphate; sequentially carrying out ring-opening reaction, recrystallization, base-catalyzed hydrolysis, pyrophosphoryl chloride esterification and salt-formation from neutralization to obtain a dexamethasone sodium phosphate solution, and carrying out further recrystallization on the dexamethasone sodium phosphate solution to obtain a dexamethasone sodium phosphate crystal by taking dexamethasone acetate epoxide as a starting material; drying the dexamethasone sodium phosphate crystal, and ball-milling the dried crystal into powder; and dissolving the dexamethasone sodium phosphate powder by water for injection for dilution, adding medicinal propylene glycol, and phosphate buffered solution with the pH being 8.0 to prepare the dexamethasone sodium phosphate injection. With the adoption of the method, the problems that in the existing preparation methods, the yield is low, and the active ingredients of the prepared dexamethasone sodium phosphate injection are rapid in efficacy-decreasing speed 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

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Application Information

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