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Ceftizoxime sodium for injection and preparation method thereof as well as synthetic method for ceftizoxime sodium serving as crude drug

A technology of ceftizoxime and ceftizoxime sodium, which is applied in the field of medicine, can solve problems such as accelerated dissolution rate, reduced packaging efficiency, and slowed dissolution rate, so as to overcome poor clarity, improve stability, and improve solubility Effect

Inactive Publication Date: 2012-10-10
SINOPHARM ZHIJUN (SHENZHEN) PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The particle size of ceftizoxime sodium for injection affects the fluidity of drug packaging and the dissolution rate of the drug. Generally speaking, the larger the particle size, the better the fluidity. On the contrary, the smaller the particle size, the worse the fluidity, that is, the lower the efficiency of drug dispensing and the large difference in loading, but the higher the solubility, the faster the dissolution rate.

Method used

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  • Ceftizoxime sodium for injection and preparation method thereof as well as synthetic method for ceftizoxime sodium serving as crude drug
  • Ceftizoxime sodium for injection and preparation method thereof as well as synthetic method for ceftizoxime sodium serving as crude drug
  • Ceftizoxime sodium for injection and preparation method thereof as well as synthetic method for ceftizoxime sodium serving as crude drug

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] The synthetic method of crude drug ceftizoxime sodium is characterized in that the method comprises the following steps:

[0061] 1) Preparation of compound tert-butoxycarbonylaminothioxime acetic acid as shown in formula B

[0062] Add 100g of the compound 2-(2-amino-4-thioxime)-2-methoxyiminoacetic acid (aminothioxime acetic acid) shown in formula A into the dioxane-water mixed solution (dioxane : Dissolve in 500ml of water (2:1), adjust the pH to 9 with triethylamine, add 108g of di-tert-butyl dicarbonate to the ice-water bath, react for 6h, adjust the pH to 4.5 with hydrochloric acid, and precipitate a white solid, filter with suction, 50ml of chloroform Rinse the filter cake 2 times, and dry under reduced pressure to obtain 138 g of compound tert-butoxycarbonylaminothioxime acetic acid shown in formula B, yield 92.2%;

[0063] Formula A:

[0064] Formula B:

[0065] 2) Preparation of compound tert-butoxycarbonylaminothioxime acetic anhydride as shown in form...

Embodiment 2

[0088] The synthetic method of crude drug ceftizoxime sodium is characterized in that the method comprises the following steps:

[0089] 1) Preparation of compound tert-butoxycarbonylaminothioxime acetic acid as shown in formula B

[0090] Add 100g of the compound 2-(2-amino-4-thioxime)-2-methoxyiminoacetic acid (aminothioxime acetic acid) shown in formula A into the dioxane-water mixed solution (dioxane : Dissolve in 500ml of water (2:1), adjust the pH to 10 with triethylamine, add 108g of di-tert-butyl dicarbonate to the ice-water bath, react for 8h, adjust the pH to 5.5 with hydrochloric acid, and precipitate a white solid, filter with suction, 50ml of chloroform Rinse the filter cake 2 times, and dry under reduced pressure to obtain 148 g of compound tert-butoxycarbonylaminothioxime acetic acid as shown in formula B, with a yield of 98.9%;

[0091] Formula A:

[0092] Formula B:

[0093] 2) Preparation of compound tert-butoxycarbonylaminothioxime acetic anhydride as...

Embodiment 3

[0116] The synthetic method of crude drug ceftizoxime sodium is characterized in that the method comprises the following steps:

[0117] 1) Preparation of compound tert-butoxycarbonylaminothioxime acetic acid as shown in formula B

[0118] Add 100g of the compound 2-(2-amino-4-thioxime)-2-methoxyiminoacetic acid (aminothioxime acetic acid) shown in formula A into the dioxane-water mixed solution (dioxane : Dissolve in 500ml of water (2:1), adjust the pH to 10 with triethylamine, add 108g of di-tert-butyl dicarbonate to the ice-water bath, react for 8h, adjust the pH to 5.5 with hydrochloric acid, precipitate a white solid, filter it with suction, and add 50ml of chloroform Rinse the filter cake 2 times, and dry under reduced pressure to obtain 148 g of compound tert-butoxycarbonylaminothioxime acetic acid as shown in formula B, with a yield of 98.9%;

[0119] Formula A:

[0120] Formula B:

[0121] 2) Preparation of compound tert-butoxycarbonylaminothioxime acetic anhyd...

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Abstract

The invention provides ceftizoxime sodium for injection and a preparation method thereof as well as a synthetic method for ceftizoxime sodium serving as a crude drug. The ceftizoxime sodium for injection has the advantages of moderate grain size range, high purity, low impurity content, high and stable quality, good clarity and the like, so that the sub-packaging efficiency during production is high, the difference of the packaging amount is small, the dissolution speed of drugs in the clinical application is high and the dissolubility is good. The preparation method of the ceftizoxime sodium for injection is simple in process, low in energy consumption, low requirement on equipment and low in cost, is suitable for large-scale industrial production and application and has wide application prospect. The synthetic method for ceftizoxime sodium serving as crude drug is simple in process, low in energy consumption, low requirement on the equipment and low in cost, and is suitable for large-scale industrial production and application.

Description

technical field [0001] The invention relates to the technical field of medicines, in particular to ceftizoxime sodium for injection, a preparation method thereof, and a synthesis method of raw drug ceftizoxime sodium. Background technique [0002] Ceftizoxime sodium, English name: Ceftizoxime Sodium, chemical name: (6R,7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-2-methoxyiminoacetamide Base]-8-oxo-5-thia-1-aminobicyclo[4.2.0]oct-2-ene-2-carboxylic acid sodium salt. [0003] Molecular formula: C 13 h 12 N 5 NaO 5 S 2 [0004] Molecular weight: 405.38 [0005] The structural formula is formula G: [0006] [0007] Ceftizoxime sodium is a third-generation cephalosporin antibiotic developed by Fujisawa Pharmaceutical Co., Ltd. of Japan. It was first listed in Japan in 1982 under the trade name Ceftizox. This product is a third-generation cephalosporin antibiotic. Its mechanism of action is to achieve bactericidal effect by inhibiting the biosynthesis of bacterial cell wall mu...

Claims

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Application Information

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IPC IPC(8): C07D501/20C07D501/06C07D501/12
Inventor 闫志刚邓宝军王磊曾环想王泳程莹莹李娟权超
Owner SINOPHARM ZHIJUN (SHENZHEN) PHARMA CO LTD
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