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Novel cefuroxime sodium compound
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A technology of cefuroxime sodium and its compound, which is applied in the field of medicine, and can solve problems such as poor solubility, slow dissolution rate of cefuroxime sodium, and incomplete dissolution
Inactive Publication Date: 2016-08-24
石药集团中诺药业(石家庄)有限公司
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However, its aqueous solution is very unstable. This product should be used as soon as possible after dissolving. It should not be stored for more than 24 hours at room temperature, and not more than 48 hours in a refrigerator at 5°C. This will bring a lot of inconvenience to clinical use.
[0007] Cefuroxime sodium generally has the following problems: 1. Poor stability, mainly reflected in the rapid color change, and the color is easily deepened during storage
It is mainly reflected in the fact that the dissolution rate of cefuroxime sodium in water is slow and the solubility is small, and even the large-scale injection of cefuroxime sodium cannot be completely dissolved in half an hour, which brings great problems to the dispensers in clinical use. inconvenient
3. Cefuroxime sodium products generally have small crystal size and serious agglomeration, which makes it difficult to filter and dry during the production process, and the labor intensity is high
[0008] The above problems can be solved by changing the crystal form. At present, there has been some research on the crystal form of cefuroxime sodium. Patent CN201410814452.3 discloses a new crystal form of cefuroxime sodium and its crystal preparation method. The stability of cefuroxime sodium crystals has been improved to some extent, but it is still not ideal, and it is easy to produce impurities, which will increase the occurrence of adverse drug reactions
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Embodiment 1
[0032] Embodiment 1 prepares new cefuroxime sodium compound of the present invention
[0033] Add 1000g of crude cefuroxime sodium into a 15L three-necked flask, add 7000mL of water and 1200mL of cycloethanol, stir and heat to reflux to dissolve, then add 600mL of ethyl acetate to the solution, then slowly cool down to 10°C, stir and crystallize, filter , washed with ethyl acetate, and vacuum-dried at 50° C. to obtain 956 g of dry cefuroxime sodium, with a yield of 95.6%.
[0034] The X-raypowder diffraction pattern of the new cefuroxime sodium compound at the reflection angle 2θ is (with an accuracy of ±0.1°): 11.78°, 14.86°, 16.12°, 17.24°, 19.74°, 21.11°, 23.07°, 23.72° , 24.08°, 24.33°, 24.82°, 25.96°, 26.26°, 27.16°, 28.77°, 29.82° have characteristic absorption peaks, such as figure 1 shown.
[0035] Its DSC spectrum has an endothermic peak near 207.34°C (with an accuracy of ±2°C), such as figure 2 shown.
Embodiment 2
[0036] Embodiment 2 prepares the new cefuroxime sodium compound of the present invention
[0037] Add 1,000 g of crude cefuroxime sodium into a 15 L three-necked flask, add 6,000 mL of water and 800 mL of cyclohexanol, stir and heat to reflux to dissolve, then add 400 mL of ethyl acetate to the solution, then slowly cool down to 15°C, stir and crystallize, Filter, wash with ethyl acetate, and dry under vacuum at 40°C to obtain 917 g of dry cefuroxime sodium, with a yield of 91.7%.
Embodiment 3
[0038] Embodiment 3 prepares new cefuroxime sodium compound of the present invention
[0039]Add 1,000 g of crude cefuroxime sodium into a 15 L three-necked flask, add 8,000 mL of water and 1,600 mL of cyclohexanol, stir and heat to reflux for dissolution, then add 800 mL of ethyl acetate to the solution, then slowly cool down to 0°C, stir and crystallize, Filter, wash with ethyl acetate, and dry under vacuum at 60°C to obtain 922 g of dry cefuroxime sodium, with a yield of 92.2%.
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Abstract
The invention relates to a novel cefuroximesodium compound and a preparation method thereof and belongs to the technical field of medicine. According to the novel cefuroximesodium compound, in an X-raypowderdiffraction spectrum of the novel cefuroximesodium compound, characteristic peaks are displayed at the positions where 2theta equals to 11.78 + / -0.1 degrees, 14.86 + / -0.1 degrees, 16.12 + / -0.1 degrees, 17.24 + / - 0.1 degrees, 19.74 + / -0.1 degrees, 23.07 + / -0.1 degrees, 25.96 + / -0.1 degrees and 27.16 + / - 0.1 degrees, and an endothermic peak exists at the position where the temperature is 200-210 DEG C in a differential scanning calorimetry spectrum. The novel cefuroxime sodium compound is good in mobility, more meets requirements of technology of pharmaceutics and is more suitable for preparing various pharmaceutic preparations. Due to the fact that powder-injection prepared from the novel cefuroxime sodium compound is good in stability, besides, stability can reach 72 hours or above after the powder-injection is prepared into an injection solution, storage time is greatly prolonged, therefore safety and efficiency of drug use are improved, and the occurrence rate of adverse reactions is reduced.
Description
technical field [0001] The invention relates to a new compound and a preparation method thereof, in particular to a new cefuroxime sodium compound and a preparation method thereof, belonging to the technical field of medicine. Background technique [0002] CefuroximeSodium, chemical name: (6R,7R)-7-[2-furyl(methoxyimino)acetamido]-3-carbamoyloxymethyl-8-oxo-5 - Sodium thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylate. Molecular formula is C 16 h 15 N 4 NaO 8 S, the molecular weight is 446.37. Chemical Structure: [0003] [0004] Cefuroxime sodium is a cephalosporin antibiotic developed by the British Glaxo Company and belongs to the second-generation cephalosporin. It inhibits cell division and growth by binding to penicillin-binding proteins (PBPs) on the bacterial cell membrane, and finally lyses and kills the bacteria. It has a broad-spectrum antibacterial effect and a wide range of applications. It has a high antibacterial effect on Staphylococcus aureus, Stre...
Claims
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