Infection contamination resistance pharmaceutical combination containing optimum proportioning cefoperazone natrium and sulbactam sodium and method of preparing the same

Abstract

The invention relates to an anti-infective pharmaceutical composition comprising cefoperazone sodium and sulbactam sodium in optimal proportion. In the pharmaceutical composition, the weight ratio of the cefoperazone sodium and the sulbactam sodium is (2-4):1, preferably 4:1. The pharmaceutical composition with the weight ratio is excellent in antibacterial activity to drugs containing equal amounts (1:1) of cefoperazone sodium and sulbactam sodium in clinic. The dosage of sulbactam sodium in the inventive pharmaceutical composition is reduced by more than two times than the existing similar drugs, which improves safety of kidney and reduces production cost. The raw materials used in the invention meet the standards of Chinese Pharmacopoeia. Therefore, the pharmaceutical composition has good quality, safety and stability.

Description

technical field [0001] The invention relates to an anti-infection pharmaceutical composition and a preparation method thereof, in particular to a pharmaceutical composition containing optimal ratio of cefoperazone sodium and sulbactam sodium and a preparation method thereof. Background technique [0002] About 25% to 75% of patients with Gram-negative bacterial infection who fail or relapse are caused by bacteria producing β-lactamases. Therefore, facing the increasingly serious problem of bacterial drug resistance caused by bacterial enzymes, It is necessary to develop new antibacterial drugs to deal with it. In addition to continuing to work on screening effective antibacterial drugs with new chemical structures, new mechanisms of action, or new targets for drug-resistant bacteria, the most economical and effective means is to choose a combination of appropriate antibiotics and β-lactamase inhibitors. Drugs are used to suppress drug-resistant bacteria and enable antibioti...

AI Technical Summary

Problems solved by technology

This temporary addition of cefoperazone sodium dose brings trouble to the timely preparation of the drug, the dose is not easy to control, and it also increases the chance of drug contamination, which is extremely unsafe

The pharmacokinetics of sulbactam sodium shows that sulbactam sodium is metabolized by the kidneys, and high content of sulbactam sodium not only aggravates the damage of the kidneys, but also the high price of sulbactam sodium makes anti-infection treatment less effective. Fee increases that make it unacceptable or unaffordable for economically disadvantaged areas or families in financial distress

[0005] Chinese patent application number: 200610034315.3 discloses a stable cefoperazone-sulbactam drug compound preparation, which is composed of cefoperazone acid as raw material, sulbactam and sodium bicarbonate. The invention has the following obvious shortcomings : 1. The raw materials do not meet the requirements of Pharmacopoeia and injection preparations

Cefoperazone acid contains a large amount of impurities harmful to the human body. It cannot meet the requirements of the Chinese Pharmacopoeia for content, clarity, and pH value without purification. the poison of

2. Lack of scientific theoretical basis for prescription design

Cefoperazone acid and cefoperazone sodium are two different substances, although the production of cefoperazone sodium is obtained by the neutralization reaction of cefoperazone acid and alkali, but because of the relatively large molecular weight of cefoperazone acid, the preparation of medicine from cefoperazone acid is a raw material. In the process of using cefoperazone sodium, the reaction rate of cefoperazone acid and basic compounds such as sodium bicarbonate solid is not as fast as the general acid-base neutralization reaction. It is a complex reaction process, which is very affected by temperature and pH value. Big

Moreover, the impurities brought by the raw material cefoperazone acid and the lactam ring of cefoperazone acid caused by the violent chemical reaction in the production were destroyed and the newly produced by-products also remained in the drug and were not removed. This will cause great harm to the human body

3. There is an obvious unstable state between the groups, and there will be reactions between the groups

[0007] The cefoperazone sodium / sulbactam sodium pharmaceutical composition provided by the present invention consists of chemically stable cefoperazone sodium and sulbactam sodium. The optimal ratio of cefoperazone sodium and sulbactam sodium described in the present invention has not been listed or reported.

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