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Cefepime hydrochloride medicinal preparation for treating new indications of tympanitis

A technology of cefepime hydrochloride and preparations, which is applied in the field of drug preparation, can solve problems such as allergic reactions, pharmacological hazards, and unfavorable human health, and achieve the effect of improving the safety of use and reducing impurities

Inactive Publication Date: 2020-08-21
广东赛法洛药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Anaphylaxis occurs rapidly and is difficult to treat. If it is not treated in time, it will have serious consequences
[0007] Although cefepime hydrochloride injection is a sterile preparation, which greatly reduces the occurrence of adverse reactions, because cefepime hydrochloride remains or introduces impurities in the synthesis, purification, and preparation of preparations, the stability of cefepime hydrochloride will deteriorate. Causes cefepime to form macromolecular polymers, eventually leading to allergic reactions
In addition, some impurities can also cause pharmacological hazards to the human body, which is not conducive to human health.

Method used

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  • Cefepime hydrochloride medicinal preparation for treating new indications of tympanitis
  • Cefepime hydrochloride medicinal preparation for treating new indications of tympanitis
  • Cefepime hydrochloride medicinal preparation for treating new indications of tympanitis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0096] Example 1 Synthesis of Cefepime Hydrochloride

[0097] Preparation of compound 1:

[0098] Add 160g of ACLE·HCl and 320mL of tetrahydrofuran into the reaction vessel in turn, add 55ml (0.39mol) of triethylamine dropwise under ice bath, after the drop is complete, remove the ice bath, and stir at room temperature for 1 h. Filter, wash with 150mL tetrahydrofuran for 3 times, and the filtrate is set aside

[0099] In another reaction vessel, add 44ml of formic acid and 110ml (1.17mol) of acetic anhydride, and stir at 40-50°C for 0.5h. Cool down, stir in an ice bath for 1 h, filter, and wash with ethanol to obtain 119 g of compound 1 with a yield of 86%.

[0100] Preparation of Compound 2:

[0101] Add 110g of compound 1, 330mL of dichloromethane-210ml of anisole (volume ratio 3:2) into the reaction vessel in turn, add 213ml of trifluoroacetic acid dropwise in ice bath, stir at room temperature for 1 hour, pour the reaction solution into the container In a reaction fla...

Embodiment 2

[0108] Example 2 Synthesis of Cefepime Hydrochloride

[0109] The synthesis process is the same as in Example 1, the only difference is that in the synthesis of compound 1, ethyl acetate is used as the reaction solvent I. Finally, 74.7 g of compound 1 was prepared, with a yield of 54%, indicating that tetrahydrofuran as the reaction solvent I is beneficial to the improvement of the conversion rate of raw materials compared with ethyl acetate.

Embodiment 3～4

[0110] Embodiment 3~4 Synthesis of Cefepime Hydrochloride

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PUM

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Abstract

The invention relates to the technical field of medicinal preparation, and discloses cefepime hydrochloride, a preparation, a preparation method and a new indication for treating tympanitis. The cefepime hydrochloride provided by the specific preparation method is low in impurity content, high in stability and remarkable in medicine effect, the quality of a preparation product is improved, the safety and effectiveness of the preparation product are guaranteed, and the cefepime hydrochloride has the application in the aspect of preparing a medicine for treating tympanitis.

Description

technical field [0001] The invention relates to medicine preparation technology, in particular to a cefepime hydrochloride composition, a preparation method and an application thereof. Background technique [0002] Cefepime hydrochloride, English name: CEFEPIME HYDROCHLORIDE, listed by Bristol-Myers Squibb (Bristol-Myers Squibb) in 1997, is a fourth-generation cephalosporin antibiotic, and its antibacterial mechanism is to affect the synthesis of bacterial cell walls. Similar to other cephalosporins, it can inhibit the transpeptidation of transpeptidase in the last step of cross-linking in cell wall synthesis, so that cross-linking cannot be formed, thereby affecting cell wall synthesis and leading to bacterial lysis and death. [0003] The chemical name of cefepime hydrochloride is 1-[[(6R,7R)-7-[(2Z)-(2-amino-4-thiazolyl)(methoxyimino)acetamido)]-2-carboxy -8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]-1-methylpyrrolidinium hydrochloride, its molecular formula is C 19 h...

Claims

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Application Information

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IPC IPC(8): C07D501/46C07D501/06C07D501/04A61K31/546A61P27/16
CPCA61K31/546A61P27/16C07D501/04C07D501/06C07D501/46
Inventor 傅苗青周白水郭丽娟吴丰喆马庆双俞玉萍李秋荣应鹏
Owner 广东赛法洛药业有限公司
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