Cefoperazone sodium and sulbactam sodium composition

A technology of cefoperazone sodium sulbactam sodium and cefoperazone sodium, which is applied in the field of medicine, can solve the problems of poor uniformity, fluidity and stability of raw materials, large dosage, and reduced content of active ingredients of medicines, and reduce the types, contents, and types of impurities And the effect of less dosage and reducing the accumulation in the body

Active Publication Date: 2016-08-17
HAINAN HERUI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Because both cefoperazone sodium and sulbactam sodium contain a lactam ring, and cefoperazone sodium is a weak acid strong base salt, the mother nucleus in the chemical structure contains an unstable β-lactam ring, which is easily hydrolyzed and degraded, and its stability is poor, and degradation and degradation often occur. Polymerization reaction, which leads to the decrease of the content of the active ingredients of the drug, the increase of impurities, and is extremely sensitive to acid and alkali. Therefore, it is necessary to strictly control the production conditions, especially after the development of a compound formula, the requirements for the production process are also stricter, otherwise it will be very difficult. It is easy to cause the content of impurities to exceed the standard, leading to the occurrence of side effects
And the storage stability of sulbactam sodium in the prior art is relatively poor, its related substances will increase significantly in the light and humid environment, the long-term storage impurity content is higher, and the use safety is poor, when it is compounded with cefoperazone sodium, it is easy to Affect the stability of the compound
The current commercially available compound preparations of cefoperazone sodium and sulbactam sodium have poor stability and need to be stored in a dry and cold place with strict storage conditions, and the validity period can only reach 24 months
[0006] Publication No. CN104844624A provides a co-crystal of cefoperazone sodium and sulbactam sodium and its preparation method. The co-crystal of cefoperazone sodium and sulbactam sodium in the present invention has a concentrated particle size distribution, and the product has good fluidity, surface gloss and high crystallinity. , good stability, the preparation method of its crystal form has simple process, easy operation, and is suitable for wide-scale popularization and application. The buffer can adjust the pH value, which not only solves the problems of poor uniformity, fluidity and raw material stability of the mixed powder in the preparation, but also avoids the generation of carbonate carbon dioxide gas when the stabilizer is added, and the obtained powder injection dissolves quickly after being diluted by conventional infusion. , no crystallization and degradation products are produced, the clarity of the solution meets the requirements, the pH value of the solution has no obvious change, the content of cefoperazone sodium and sulbactam sodium is stable, although the cefoperazone sodium sulbactam sodium cocrystal prepared by the present invention has

Method used

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  • Cefoperazone sodium and sulbactam sodium composition
  • Cefoperazone sodium and sulbactam sodium composition
  • Cefoperazone sodium and sulbactam sodium composition

Examples

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Embodiment 1

[0036] The preparation of embodiment 1 sulbactam sodium crystal

[0037] (1) Grind the crude product of sulbactam sodium, cross a 100 mesh sieve, then add a mixed solution of deionized water and methanol whose volumetric amount is 18 times the weight of sulbactam sodium, and the volume ratio of deionized water and methanol is 8.5:1 , stirred evenly to dissolve, and adjusted the pH to 8;

[0038] (2) adding activated carbon for decolorization, filtering to obtain a clear solution;

[0039] (3) Add dropwise the mixed solution of acetone and ethyl acetate with a volume ratio of 1:3.5 to the above clear solution under the condition of stirring rate of 30rmp, then put it into a sound field with a frequency of 36KHz and an output power of 38W at a speed of 32rmp Stir under low temperature for 16 minutes to cool down to 5°C, let stand for 25min, then stir at 25rmp for 40min and cool to -18°C, stand for crystallization for 26h, wash, and vacuum dry to obtain the aztreonam crystal.

...

Embodiment 2

[0041] The preparation of embodiment 2 sulbactam sodium crystals

[0042] (1) Grind the crude product of sulbactam sodium, cross a 100-mesh sieve, then add a mixed solution of deionized water and methanol whose volumetric amount is 19 times the weight of sulbactam sodium, and the volume ratio of deionized water and methanol is 9:1 , stirred evenly to dissolve, and adjusted the pH to 8.5;

[0043] (2) adding activated carbon for decolorization, filtering to obtain a clear solution;

[0044] (3) Add dropwise the mixed solution of acetone and ethyl acetate with a volume ratio of 1:3.7 to the above clear solution at a stirring rate of 35rmp, then put it into a sound field with a frequency of 36KHz and an output power of 38W at a speed of 34rmp Stir under low temperature for 18 minutes and cool down to 7°C, stand still for 28 minutes, then stir at 27rmp for 44min and cool down to -16°C, stand for crystallization for 24h, wash, and dry in vacuum to obtain the aztreonam crystals.

...

Embodiment 3

[0046] The preparation of embodiment 3 sulbactam sodium crystals

[0047] (1) Grind the crude product of sulbactam sodium, cross a 100-mesh sieve, then add a mixed solution of deionized water and methanol whose volumetric amount is 20 times the weight of sulbactam sodium, and the volume ratio of deionized water and methanol is 9.5:1 , stirred evenly to dissolve, and adjusted the pH to 9;

[0048] (2) adding activated carbon for decolorization, filtering to obtain a clear solution;

[0049] (3) Add dropwise a mixed solution of acetone and ethyl acetate with a volume ratio of 1:4 to the above clear solution under the condition of a stirring rate of 36rmp, and then put it into a sound field with a frequency of 36KHz and an output power of 38W at a speed of 36rmp Stir under low temperature for 19 minutes and cool down to 8° C., stand still for 30 minutes, then stir at 28 rpm for 46 minutes and cool down to -15° C., stand for crystallization for 28 hours, wash, and dry in vacuum t...

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Abstract

The invention provides a cefoperazone sodium and sulbactam sodium composition, which comprises the following raw materials in parts by weight: 9-10 parts of cefoperazone sodium, 1 part of sulbactam sodium and 0.05-0.07 part of glutathione. The glutathione is added to the composition, so that the composition has relatively good antibacterial effect. Furthermore, a little of sulbactam sodium is utilized, so that accumulation of the sulbactam sodium in a body is reduced; and the production cost is reduced. In addition, by a novel sulbactam sodium crystal, the composition provided by the invention has relatively good stability.

Description

technical field [0001] The invention belongs to the technical field of medicine and specifically designs a cefoperazone sodium sulbactam sodium composition. Background technique [0002] Cefoperazone sodium (Cefoperazone sodium), its chemical name is: (6R, 7R)-3-[[(1-methyl-1H-tetrazol-5yl)sulfur]methyl]-7-[(R)-2- (4-Ethyl-2,3-dioxo-1-piperazinecarbonamido)-2-p-hydroxyphenyl-acetylamino]-8-oxo-5-thia-1-azabicyclo[ 4.2.0] Oct-2-ene-2-carboxylic acid sodium salt. [0003] Cefoperazone sodium is a representative of the third-generation cephalosporins. It exerts antibacterial effects by inhibiting the synthesis of bacterial cell walls. It belongs to lactam antibiotics and can resist the degradation of various β-lactamases. It has a wide antibacterial spectrum and is effective against Gram-positive All bacteria have effects, such as Staphylococcus aureus (including strains that produce or do not produce penicillin), Streptococcus pneumoniae, most strains of beta-hemolytic strep...

Claims

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Application Information

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IPC IPC(8): A61K31/546A61K47/18A61P31/04A61K31/43
CPCA61K31/43A61K31/546A61K47/183A61K2300/00
Inventor 钟正明
Owner HAINAN HERUI PHARMA
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