Novel amoxicillin clavulanic acid composition

Abstract

The invention discloses a novel amoxicillin clavulanic acid composition. When pegylation is conducted on the amoxicillin, the medicine water-solubility is improved and at the same time good stability of the medicine is ensured; by modifying the clavulanic acid by using glucuronic acid, the original characteristic of strong hygroscopicity is changed, and problems that the clavulanic acid is poor in mobility, non-uniform when being mixed with the amoxicillin, easy to discolor, deteriorate and degrade and the like caused by the strong hygroscopicity are avoided, so that by carrying out molecular modification on the two active ingredients respectively, not only is the physiochemical property of the medicine changed, but also the stability is greatly improved, the effective content after entering human bodies is ensured, problems that the content is greatly reduced and related substances are increased after an ordinary preparation product in market is prepared into injection are solved, the problem of mass stability of the composition in the production, storage, preparation and injection process is substantially solved, and the use amount of the clavulanic acid is greatly reduced.

Description

technical field [0001] The invention relates to an antibiotic drug, in particular to a novel amoxicillin-clavulanic acid composition. Background technique [0002] Amoxicillin and clavulanic acid formed by the combination of clavulanic acid and amoxicillin belong to the β-lactam compound antibiotics. It was originally researched and developed by GlaxoSmithKline Pharmaceutical Company. It was approved by the FDA on August 6, 1984 and has been on the market for many years It ranks among the world's best-selling drugs, ranks first in the world's anti-infective drugs, and has been included in the Chinese Pharmacopoeia. It can inhibit the β-lactamase produced by Staphylococcus, Haemophilus influenzae, catarrhalis, Escherichia coli, Klebsiella, Proteus mirabilis, Proteus vulgaris, Neisseria gonorrhoeae, Legionella, Bacteroides fragilis and other microorganisms. The destruction of amoxicillin is therefore effective against enzyme-producing or non-enzyme-producing strains of the af...

AI Technical Summary

Problems solved by technology

Chinese patent CN1850074 discloses a method for preparing amoxicillin sodium and clavulanate potassium drug mixture by using carbon dioxide supercritical technology. This scheme improves the uniformity and fluidity of the drug mixture to a certain extent, but does not fundamentally improve The instability of amoxicillin sodium, in the later storage and transportation process, the drug is still easy to deteriorate

[0008] Chinese patents CN101804051 and CN101890007 respectively disclose a liposome injection and a microsphere injection of amoxicillin sodium clavulanate potassium pharmaceutical composition, which can improve the problem of poor stability of ordinary injections to a certain extent

These new injection preparations (liposome injections, microsphere injections) have certain advantages over traditional injections, but they also have low encapsulation efficiency, easy adhesion and aggregation, easy rupture, burst release effect, and possible cause immune response

In addition, the scale-up production of these new dosage forms in China is not mature enough, and the preparation process conditions are very strict, the production is difficult, the process reproducibility is poor, and the production cost is high, which virtually increases the financial burden of patients, so it does not not ideal

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