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Aztreonam anhydrous crystal compound and preparation method thereof

An anhydrous crystalline compound technology, applied in the field of aztreonam anhydrous crystalline compound and its preparation, can solve the problems of poor antibacterial effect and no antibacterial activity

Active Publication Date: 2010-09-15
HAINAN HULUWA PHARMA GRP CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Aztreonam has a high degree of antibacterial activity against most aerobic Gram-negative bacteria, including Escherichia coli, Klebsiella pneumoniae and Oxytobacter, aerogenes, cloacae, Proteus, sand Enterobacteriaceae such as Chrysobacterium, Citrobacter, and Shigella, as well as Influenza bacilli, Neisseria gonorrhoeae, and Neisseria meningitidis, etc., also have good antibacterial effects on Pseudomonas aeruginosa. Pseudomonas and Acinetobacter have poor antibacterial activity except for Pseudomonas aeruginosa, and have no antibacterial activity against aerobic Gram-positive bacteria such as Staphylococcus and Streptococcus and anaerobic bacteria

Method used

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  • Aztreonam anhydrous crystal compound and preparation method thereof
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  • Aztreonam anhydrous crystal compound and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0032] Example 1 : Preparation of aztreonam anhydrous crystal compound

[0033] Add 1 g of aztreonam into 5 mL of anhydrous acetonitrile, reflux and dissolve at 80° C. for 1 h, and stir and cool the filtrate at room temperature for 6 h to crystallize. Suction filtration was then performed, and the filter cake was washed with a small amount of anhydrous acetonitrile. The filter cake was vacuum dried at 60°C to constant weight. Obtained 0.80 g of a crystal compound sample.

[0034] Use the RigakuD / MAXRC diffractometer to measure the prepared crystalline compound samples. The system parameters are as follows: CuK 1 Wire Monochromatic radiation, 40kV, 200mA. The obtained X-ray powder diffraction pattern is shown in figure 1 .

Embodiment 2

[0035] Example 2 : Performance identification of aztreonam anhydrous crystal compound

[0036] Under laboratory conditions, the fluidity (measurement of the angle of repose) of the aztreonam anhydrous crystal compound powder prepared in Example 1 was detected.

[0037] Basis: The angle of repose was measured by the fixed funnel method to investigate the fluidity of the anhydrous crystal compound of aztreonam.

[0038] Method: Gently and evenly drop the predicted material into the center of the disc to make the powder form a cone, stop feeding when the material falls freely from the inclined edge of the powder along the edge of the disc, and measure the angle of repose with a protractor (or Measure the radius of the disc and the height of the powder, and calculate the angle of repose, tgθ=height / radius). The smaller the angle of repose, the better the fluidity of the aztreonam anhydrous crystal compound.

[0039] Results: According to the above method, the measurement resul...

Embodiment 3

[0047] Example 3 : Preparation of aztreonam freeze-dried powder injection

[0048] The 24.2Kg aztreonam anhydrous crystal compound prepared by the method of Example 1 is mixed with 16.6Kg L-arginine powder, and 170.0Kg of water for injection is added under stirring and mixed until the powder is completely dissolved, and 1638.5g L-arginine is added to the solution. Arginine, adjust the pH of the solution to 5, and then add water for injection to adjust the final volume to 220L. The solution passes through a clarification filter and a sterile filter into a sterile tank. An aliquot of the resulting solution is poured into vials to obtain the following vial-filled medicinal solution:

[0049] Flushing volume Aztreonam potency / vial

[0050] 5mL 0.55g

[0051] 10mL 1.1g

[0052] 20mL 2.2g

[0053] A partially opened stopper with a catheter is placed over the vial and the contents are lyophilized.

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Abstract

The invention provides an aztreonam anhydrous crystal compound. An X-ray diffractive map comprises the following X-ray diffractive peaks: 18.2 degrees + / - 0.2 degree, 24.0degrees + / - 0.2 degree, 9.1 degrees + / - 0.2 degree, 4.1 degrees + / - 0.2 degree and 17.2 degrees + / - 0.2 degree disclosed by 2 theta angles. The invention also provides a method for preparing the aztreonam anhydrous crystal compound. The aztreonam anhydrous crystal compound has a sharp outline, can be perfectly reappeared, has powder flowbility, intrinsic dissolution rate, solid stability, and the like which are obviously better than that of the traditional aztreonam crystal compound and can be prepared into a medical composition for treating various types of infection caused by sensitive oxybiontic gram-negative bacteria.

Description

technical field [0001] The invention relates to a new crystal form compound of aztreonam and a preparation method thereof. The new crystal form compound and its pharmaceutically acceptable salt can be used for antibacterial purposes. Background technique [0002] Aztreonam (Aztreonam) is a fully synthetic monocyclic β-lactam antibiotic with the chemical name [3S-[3α(Z), 4β]]-3-[[2-amino-4-thiazolyl[1-carboxy- 1-methylethoxy]imino]acetyl]amino]-4-methyl-2-oxo-1azetidinesulfonic acid, its chemical structural formula is as follows: [0003] [0004] Aztreonam has a high degree of antibacterial activity against most aerobic Gram-negative bacteria, including Escherichia coli, Klebsiella pneumoniae and Oxytobacter, aerogenes, cloacae, Proteus, sand Enterobacteriaceae such as Chrysobacterium, Citrobacter, and Shigella, as well as Influenza bacilli, Neisseria gonorrhoeae, and Neisseria meningitidis, etc., also have good antibacterial effects on Pseudomonas aeruginosa. Except fo...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/12A61K31/427A61P31/04
Inventor 刘全国
Owner HAINAN HULUWA PHARMA GRP CO LTD
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