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A technology of cefathiamidine and single crystal, which is applied in the direction of single crystal growth, single crystal growth, crystal growth, etc., and achieves the effects of good stability, simple equipment, and easy preparation and operation
Active Publication Date: 2014-02-05
GUANGZHOU BAIYUNSHAN PHARM CO LTD
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[0007] But up to now, there is no report about cefathiamidine single crystal
Method used
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Embodiment 1
[0039] Add 12 g of cefathiamidine into a clean Erlenmeyer flask, then add 9.4 ml of water and 47.6 ml of ethanol in order, and dissolve at room temperature. Then, 37.3 ml of ethanol and 5.7 ml of acetone were added. Finally, a 0.12 g / ml cefathiamidine solution [equivalent to 100 ml of a mixed solvent of ethanol / water / acetone (volume ratio 9:1:0.6)] was prepared. Seal it with plastic film, and punch some small holes in the plastic film. Store at a certain temperature of 2-6°C. Stand still for 96 hours, that is.
[0040] Adopt R-AXIS-RAPID X-ray single crystal diffractometer of Japan Rigaku Company to analyze the obtained crystal sample, the results are shown in Tables 1-5 and attached Figure 1~2 ,in:
[0041] Table 1 is crystal data and structure optimization results;
[0042] Table 2 is the coordinates of non-hydrogen atoms
[0043] Table 3 key length
[0044] Table 4 bond angle (°);
[0045] Table 5 hydrogen atom coordinates
[0046] figure 1 is the molecular...
Embodiment 2
[0050] Add 100ml of a mixed solvent of ethanol / water / acetone (4:1:0.05 by volume) into a clean Erlenmeyer flask, then add 5g of cefathiamidine to prepare a 0.15g / ml cefathiamidine solution. Seal it with plastic film, and punch some small holes in the plastic film. Store at a certain temperature of 0-8°C. Stand still for 96 hours, that is.
[0051] The obtained cefathiamidine crystal diffraction experiment is shown in attached table 1~5 and attached table Figure 1~2 .
Embodiment 3
[0053] Add 75ml of ethanol / water mixed solvent with a volume ratio of 10:1 in a clean Erlenmeyer flask, then add 50g of cefathiamidine, dissolve at room temperature, then add dropwise 25ml of acetone to prepare a 0.5g / ml cefathiamidine solution【 Equivalent to 100ml of a mixed solvent with a volume ratio of ethanol / water / acetone of 10:1:3.67]. Seal it with plastic film, and punch some small holes in the plastic film. Store at a certain temperature of 7-15°C. Stand still for 96 hours, that is.
[0054] The obtained cefathiamidine crystal diffraction experiment is shown in attached table 1~5 and attached table Figure 1~2 .
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Abstract
The invention relates to cefathiamidine monocrystal, a preparation method, use and a composition thereof. The cefathiamidine monocrystal disclosed by the invention is prepared by comprising the following steps of: adding three solvents, namely ethanol, water and acetone, into a clean conical flask in any sequence according to any proportion, wherein the volume ratio of ethanol, water to acetone is (4-10):1:(0.05-3.67), during, before or after adding various solvents, adding cefathiamidine, dissolving at room temperature, and preparing cefathiamidine solution with the concentration of 0.05-0.5 g / ml; sealing by using a plastic film, and pricking a plurality of small holes on the plastic film; storing at 0-15 DEG C; and beginning to generate tiny crystals after about 48 h, and then obtaining cefathiamidine monocrystal after above 96 h. The preparation method disclosed by the invention is simple and convenient for operation and simple in equipment; the prepared monocrystal is good in stability; the cefathiamidine monocrystal composition disclosed by the invention is a composition composed of monocrystal and pharmaceutically acceptable carriers, preferably injection; the cefathiamidine monocrystal disclosed by the invention can be used for preparing medicines for treating respiratory tract infection, biliary tract infection, urinary tract infection, wound and surgical infection, skin and soft tissue infection, gynaecological infection, ear-nose-throat infection, endocarditis, blood poisoning, pneumonia and meningitis.
Description
【Technical field】 [0001] The present invention relates to the field of chemical pharmacy, in particular, the present invention relates to cefathiamidine single crystal, its preparation method, its composition and its application in the field of pharmacy. 【Background technique】 [0002] Cefathiamidine, the chemical name is (6R,7R)-3-[(acetyl)methyl]-7-[α-(N,N'-diisopropylamidinothio)-acetylamino]-8- Oxo-5-thia-1-azabicyclo[4,2,0]-oct-2-ene-2-carboxylate betaine, molecular formula C 19 h 28 N 4 o 6 S 2 , its structural formula is as follows: [0003] [0004] Cefathiamidine belongs to the first-generation β-lactam antibiotics, and its antibacterial spectrum is similar to that of cephalothin. It has antibacterial activity against Gram-positive bacteria and some negative bacteria, especially against Gram-positive cocci. It has good antibacterial effect on Streptococcus viridans, Hemolytic Streptococcus, Non-hemolytic Streptococcus, Bacillus diphtheriae, Clostridium per...
Claims
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