Cefoperazone sodium and tazobactam sodium pharmaceutical composition for injection

A technology of tazobactam sodium and cefoperazone sodium, which is applied in the field of medicine, can solve the problems of restricting large-scale production of preparations, poor long-term storage stability, and potential safety hazards in clinical treatment, and achieves good effectiveness and safety, low related substances, and low degradation little effect

Active Publication Date: 2016-07-13
CHINA MEHECO SANYANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

As we all know, it takes a lot of time to crush and sieve materials, and the mixing is uneven, the relative humidity is controlled in a low range, and the requirements for the production workshop environment are higher, thereby increasing production costs.
[0005] Chinese patent CN101348493A discloses a method for preparing high-purity cefoperazone sodium and high-purity tazobactam sodium compound powder injection. The production of the freeze-dried powder injection requires cefoperazone sodium and tazobactam sodium prepared according to a specific synthesis and refining process as raw materials , which limits the large-scale production of the preparation. At the same time, organic solvents such as N,N dimethylformamide and acetone are used in the crystal transformation process, which is easy to introduce impurities and bring safety hazards to clinical treatment.
[0009] At present, the conventional method is to directly mix tazobactam sodium and cefoperazone sodium. However, after the production process of the prior art is scaled up, the solution after reconstitution of the freeze-dried powder is still turbid, and foreign matter is unqualified. Poor solubility, darker color, poor long-term storage stability, high levels of related substances, high polymer content and high incidence of adverse reactions

Method used

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  • Cefoperazone sodium and tazobactam sodium pharmaceutical composition for injection
  • Cefoperazone sodium and tazobactam sodium pharmaceutical composition for injection
  • Cefoperazone sodium and tazobactam sodium pharmaceutical composition for injection

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] prescription:

[0039] Cefoperazone sodium 120kg (calculated as free cefoperazone)

[0040] Tazobactam sodium 30kg (calculated as free tazobactam)

[0041] Preparation:

[0042] (1) Refining of Tazobactam

[0043] Add the prescribed amount of tazobactam into the reaction kettle, add water, turn on the stirring and cooling device, and when the temperature reaches 0-5°C, add 8kg of sodium bicarbonate to adjust the pH to 6.2, and add 2Kg of neutral alumina to the reaction solution , stirred for 30 minutes, filtered, and the filtrate was neutralized with concentrated hydrochloric acid at 0-5°C until the pH was 1.5, a large amount of white crystals were precipitated, continued to stir for 2 hours, filtered, washed the filter cake with 0-5°C water for injection, and the filter cake was placed in Vacuum drying at around 45°C yields refined tazobactam.

[0044] (2) Preparation of Tazobactam Sodium

[0045] Add 64Kg of water for injection at 7-10°C to the reaction kettle, f...

Embodiment 2

[0050] prescription:

[0051] Cefoperazone sodium 120kg (calculated as free cefoperazone)

[0052] Tazobactam sodium 30kg (calculated as free tazobactam)

[0053] Preparation:

[0054] (1) Refining of Tazobactam

[0055] Add the prescribed amount of tazobactam into the reaction kettle, add water, turn on the stirring and cooling device, and when the temperature reaches 0-5°C, add 8kg of sodium bicarbonate to adjust the pH to 5.7, and add 2Kg of neutral alumina to the reaction solution , stirred for 30 minutes, filtered, and the filtrate was neutralized with concentrated hydrochloric acid at 0-5°C until the pH was 1.0, a large amount of white crystals were precipitated, continued to stir for 2 hours, filtered, washed the filter cake with 0-5°C water for injection, and the filter cake was placed in Vacuum drying at around 45°C yields refined tazobactam.

[0056] (2) Preparation of Tazobactam Sodium

[0057] Add 64Kg of water for injection at 7-10°C to the reaction kettle, f...

Embodiment 3

[0062] prescription:

[0063] Cefoperazone sodium 120kg (calculated as free cefoperazone)

[0064] Tazobactam sodium 30kg (calculated as free tazobactam)

[0065] Preparation:

[0066] (1) Refining of Tazobactam

[0067] Add the prescribed amount of tazobactam into the reaction kettle, add water, turn on the stirring and cooling device, and when the temperature reaches 0-5°C, add 8kg of sodium bicarbonate to adjust the pH to 6.4, and add 2Kg of neutral alumina to the reaction solution , stirred for 30 minutes, filtered, and the filtrate was neutralized with concentrated hydrochloric acid at 0-5°C until the pH was 2.0, a large amount of white crystals were precipitated, continued to stir for 2 hours, filtered, washed the filter cake with 0-5°C water for injection, and the filter cake was placed in Vacuum drying at around 45°C yields refined tazobactam.

[0068] (2) Preparation of Tazobactam Sodium

[0069] Add 64Kg of water for injection at 7-10°C to the reaction kettle, f...

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PUM

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Abstract

The invention belongs to the technical field of medicines, and particularly relates to cefoperazone sodium and tazobactam sodium pharmaceutical composition for injection and a preparation method of the cefoperazone sodium and tazobactam sodium pharmaceutical composition. The pharmaceutical composition is a freeze-dried powder preparation. The mass ratio of cefoperazone sodium to tazobactam sodium in the pharmaceutical composition is 4:1. The preparation method comprises the steps as follows: firstly, tazobactam is refined; then, tazobactam sodium is prepared from refined tazobactam and sodium bicarbonate; finally, cefoperazone sodium and prepared tazobactam sodium are uniformly mixed for preparation of freeze-dried powder. Compared with like products sold in the market, the pharmaceutical composition has the advantages of good solubility, light color, few related substances, small polymer content and low adverse reaction rate; besides, effective constituents in the pharmaceutical composition are stable, and when the pharmaceutical composition is preserved for a long term, few effective constituents are degraded, the content of impurities is low, the quality performance of products is relatively good, and the medication safety of patients is guaranteed accordingly.

Description

technical field [0001] The invention belongs to the technical field of medicines, in particular to a pharmaceutical composition of cefoperazone sodium and tazobactam sodium for injection. Background technique [0002] With the widespread use of antibiotics, the emergence of bacterial resistance has become an important factor that seriously affects the clinical efficacy. There are many mechanisms for bacterial resistance to antibacterial drugs, among which the production of β-lactamases by bacteria is the key factor for the development of β-lactamase. As an important mechanism of resistance to amide antibiotics, the increase of extended-spectrum β-lactamase (ESBLs)-producing strains has attracted more and more attention in recent years. In order to make clinically effective antibiotics continue to play a role, it is an effective method to add β-lactamase inhibitors to β-lactamase antibiotics. The currently clinically used β-lactamase inhibitors mainly include clavulanic acid...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/546A61K31/431C07D499/87C07D499/18A61K9/19A61K47/02A61P31/04
CPCA61K9/0019A61K9/19A61K31/431A61K31/546A61K47/02C07D499/18C07D499/87A61K2300/00
Inventor 朱峰王玉娟李锦云
Owner CHINA MEHECO SANYANG PHARMA CO LTD
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