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Preparation method of dexamethasone sodium phosphate for injection

A technology of dexamethasone sodium phosphate and dexamethasone sodium phosphate, which is applied in the field of medicine, can solve the problems of high cost and unstable content of active ingredients in injections, and achieve the effects of low cost, avoiding the reduction of drug efficacy, and simple steps

Inactive Publication Date: 2016-02-17
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 the present invention is to provide a preparation method of dexamethasone sodium phosphate for injection, to overcome the problems of high cost caused by the existing preparation method and unstable active ingredient content of the prepared dexamethasone sodium phosphate injection

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The preparation method of dexamethasone sodium phosphate for injection comprises the following steps:

[0028] 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;

[0029] 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;

[0030] The recrystallization: adding methanol to the dexamethasone a...

Embodiment 2

[0037] The preparation method of dexamethasone sodium phosphate for injection comprises the following steps:

[0038] 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;

[0039] 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;

[0040] The recrystallization: adding ...

Embodiment 3

[0048] The preparation method of dexamethasone sodium phosphate for injection comprises the following steps:

[0049] 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;

[0050] 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;

[0051] The recrystallization: adding met...

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Abstract

The invention relates to a preparation method of dexamethasone sodium phosphate for injection. The preparation method comprises the following steps that the dexamethasone sodium phosphate is synthesized, namely dexamethasone acetate epoxide is used as a starting raw material, and a dexamethasone sodium phosphate solution is obtained through ring-opening reaction, recrystallization, base-catalyzed hydrolysis, pyrophosphoryl chloride esterification and neutralization and salification reaction sequentially, and the dexamethasone sodium phosphate solution undergoes recrystallization again to obtain dexamethasone sodium phosphate crystals; the dexamethasone sodium phosphate crystals are dried and then are ball-milled into powder; the dexamethasone sodium phosphate powder is dissolved and diluted with water for injection, and an excipient and a disodium hydrogen phosphate solution are added into the solution to obtain dexamethasone sodium phosphate injection. The preparation method overcomes the problem that the dexamethasone sodium phosphate injection prepared by adopting an existing preparation method is higher in cost and unstable in active ingredient content.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a preparation method of dexamethasone sodium phosphate for 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 allerg...

Claims

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Application Information

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