A kind of ceftezole sodium compound and the pharmaceutical preparation containing the compound

Abstract

The invention belongs to the technical field of medicine, and particularly relates to a ceftezole sodium compound and a medicinal preparation including the same. The ceftezole sodium compound is ceftezole sodium trihydrate, and the structural formula is shown in the specification. An X-ray powder diffraction pattern, obtained through Cu-K alpha ray measurement, of the ceftezole sodium compound is shown as picture 1. A sterile powder-injection is adopted as the preparation including the ceftezole sodium compound. The content of polymer in the ceftezole sodium compound is low, and is almost not changed during an acceleration test and a long-term test. After a ceftezole sodium sterile power needle manufactured through the ceftezole sodium compound is combined with the five-percent glucose injection, the relative content of ceftezole sodium is hardly changed, and compatible stability is good.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a ceftezole sodium compound and a pharmaceutical preparation containing the ceftezole sodium compound. Background technique [0002] Ceftezole sodium is the first generation of cephalosporins for injection, developed by Fujisawa Company in Japan, and first listed in Japan, South Korea, Italy and other countries. Its English name is Ceftezole Sodium; its chemical name is: (6R,7R)-3-[(1,3,4-thiadiazol-2-yl)thiomethyl]-8-oxo-7-[2 -Sodium (1H-tetrazol-1-yl)acetamido]-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate. Its structural formula is: [0003] [0004] The chemical structure suggests that in the synthetic steps of conversion from ceftezole acid to ceftezole sodium, special attention should be paid to the conditions of salt formation. If the conditions are not well controlled, it is very likely to cause ring opening or other degradation of the β-lactam ring,...

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Problems solved by technology

[0008] In CN102286001A, step ceftezole acid crude product is added in the aqueous solution containing the sodium bicarbonate of equimolar amount and isopropanol, stir, evaporate part of solvent, stir and crystallize, filter and obtain ceftezole sodium, this method and It is not clear whether the crystals obtained are type I, type II or mixed type crystals, and their quality stability is in doubt

[0011] CN101229129A, on the basis of Mr. Hu Changqin's research, uses a designated solvent, gradient cooling crystallization, and clearly researches and controls the crystal form, but does not involve the removal of ceftezole sodium polymer, and the invention still uses the traditional solvent analysis. Crystallization method is used for production, crystals are prone to coalesce in the production process, resulting in the final product particle size is very small, difficult to filter, the product is mixed with a large amount of crystallization mother liquor, which affects the quality of the finished product, and the traditional method often adopts the addition of crystallization Seed method, but the particle size and adding time of the seed crystal have a certain influence on the final particle size distribution of the finished crystal, resulting in fluctuations in the quality of the finished product

[0015] The inventor finds after having carried out a large amount of researches to the ceftezole sodium of the prior art, the ceftezole sodium of the prior art has polymer content higher, and in accelerated test and long-term test, the content change of polymer is relatively small. big flaw

[0016] Moreover, because ceftezole sodium contains a β-lactam ring in its structure, after it is compatible with other drugs in the infusion solution, the curative effect may be degraded due to hydrolysis.

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