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A kind of aztreonam compound and preparation thereof

A technology of aztreonam and its compounds, applied in the field of aztreonam compounds and their preparations, can solve problems such as low industrialization efficiency, unsuitability for industrialization, and affecting product purity, and achieve increased solubility and dissolution speed, good stability, and flow sex good effect

Active Publication Date: 2018-03-06
SHANDONG LUOXIN PHARMA GRP CO LTD +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although this method has been improved and can carry out sterile filtration, triethylamine hydrochloride impurities are produced in the finished product, which affects the purity of the product
[0007] 3) adding a binder to a dipolar aprotic solvent (such as acetonitrile) to treat the α crystal form aztreonam to obtain a solution of aztreonam binding derivatives; then add ethanol to obtain the β crystal form aztreonam crystals, The yield of this method is very low
This method has low solubility in ethanol of α crystal form aztreonam at low temperature, a large amount of ethanol, low industrialization efficiency, and long-term low-temperature stirring, and is not suitable for industrialization

Method used

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  • A kind of aztreonam compound and preparation thereof
  • A kind of aztreonam compound and preparation thereof
  • A kind of aztreonam compound and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0051] The preparation of embodiment 1 aztreonam monohydrate

[0052] 1. Grind the α crystal form of aztreonam, pass through a 300-mesh sieve, add it into 95% methanol solution, and heat up to 40-45°C while stirring; the weight ratio of aztreonam crude product to methanol solution is 1:30 ; Stirring speed is 240 rev / min; Add activated carbon, stir for 10 minutes and filter aseptically;

[0053] 2. Add ethyl acetate while stirring, and lower the temperature to 0°C at the same time; the stirring speed is 120 rpm; the weight of ethyl acetate is twice the weight of the methanol solution of aztreonam, and the adding speed is 80 ml / min; the cooling speed 1~2℃ / hour;

[0054] 3. After adding the mixed solvent, the obtained crystals were left to stand for crystallization; filtered, washed, and vacuum-dried for 8 hours to obtain aztreonam monohydrate.

[0055] The compound crystal is detected by high-performance liquid chromatography, and the purity is 99.95%, and the yield is 90.6%; ...

Embodiment 2

[0056] The preparation of embodiment 2 aztreonam monohydrate

[0057] 1. Grind the β crystal form of aztreonam, pass through a 300-mesh sieve, add to 90% methanol solution, and heat up to 45°C while stirring; the weight ratio of aztreonam crude product to methanol solution is 1:25; Stirring speed is 360 rpm; add activated carbon, stir for 120 minutes and then sterile filter;

[0058] 2. Add ethyl acetate while stirring, and lower the temperature to -2°C at the same time; the stirring speed is 180 rpm; the weight of ethyl acetate is 3 times the weight of the methanol solution of aztreonam, and the adding speed is 70 ml / min; cool down The speed is 2°C / hour;

[0059] 3. After adding the mixed solvent, the obtained crystals were left to stand for crystallization; filtered, washed, and vacuum-dried for 6 hours to obtain aztreonam monohydrate.

[0060] The compound crystal is detected by high-performance liquid chromatography, and the purity is 99.90%, and the yield is 92.6%; the ...

Embodiment 3

[0061] The preparation of embodiment 3 aztreonam monohydrate

[0062] 1. Grind the α crystal form of aztreonam, pass through a 200-mesh sieve, add to 93% methanol solution, and heat up to 43°C while stirring; the weight ratio of aztreonam crude product to methanol solution is 1:25; Stirring speed is 360 rpm; add activated carbon, stir for 15 minutes and then sterile filter;

[0063] 2. Add ethyl acetate while stirring, and lower the temperature to 2°C at the same time; the stirring speed is 180 rpm; the weight of ethyl acetate is 3 times the weight of the methanol solution of aztreonam, and the adding speed is 70 ml / min; the cooling speed 1.5°C / hour;

[0064] 3. After adding the mixed solvent, the obtained crystals were left to stand for crystallization; filtered, washed, and vacuum-dried for 7 hours to obtain aztreonam monohydrate.

[0065] The compound crystal is detected by high-performance liquid chromatography, and the purity is 99.91%, and the yield is 90.3%; the X-ray...

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Abstract

The invention relates to the field of medicines and concretely relates to an aztreonam monohydrate and a preparation thereof. The aztreonam monohydrate has a structure shown in the formula (I). The invention also relates to a dosage form of the aztreonam monohydrate. The dosage form of the pharmaceutical composition is an injection preparation or an inhaled preparation. A stability test proves that the aztreonam monohydrate has good stability and especially has higher stability after matching and is suitable for clinical application.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an aztreonam compound and its preparation. Background technique [0002] The chemical name of aztreonam is [2S-[2α,3β(Z)]-2-[[[1-(2-amino-4-thiazolyl)-2-[(2-methyl-4 -generation-1-sulfo-3-azetidinyl)amino]-2-oxoethylene]amino]oxo]-2-methylpropionic acid, {[2S-[2,3( Z)]]-2-[[[1-(2-amino-4-thiazolyl)-2-[(2-methyl-4-oxo-1-sulfo-3-azetidinyl)amino]-2-oxoethylene]amino ]oxy]-2-methyl propanoic acid}. In 1978, it was first discovered from the culture medium of Chromobacterium violaceum, a soil bacterium in New Jersey, USA. It was the first new lactam antibiotic of Monobactams used in clinical practice. It kills bacteria mainly by inhibiting the synthesis of bacterial cell walls. effect on G - The penicillin-binding protein 3 (PBP-3) on the bacterial cell membrane has a high affinity, which hinders the division of bacterial cells and forms filaments, which leads to the dissolution and death ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D417/12A61K31/427A61K47/18A61K9/14A61K9/72A61K9/08A61K9/19A61P31/04
CPCA61K9/0019A61K9/0073A61K9/08A61K9/145A61K9/19A61K31/427A61K47/183C07B2200/13C07D417/12
Inventor 武玉梅孙涛刘新泉朱丽萍
Owner SHANDONG LUOXIN PHARMA GRP CO LTD
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