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Stable aztreonam composition and preparation method thereof

A technology of aztreonam and composition, which is applied in the field of antibacterial drugs and its preparation, can solve problems such as failure to meet quality requirements, large changes in pH value, uneven mixing, etc., and achieve improved drug availability, simple preparation method, and easy prescription The effect of process simplification

Active Publication Date: 2012-03-28
AMICOGEN CHINA BIOPHARM CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] In order to overcome the deficiencies in the prior art, solve the problem that the two components of aztreonam and L-arginine in the preparation of aztreonam for injection in the prior art are easily layered and cause uneven mixing, and the problems of the current aztreonam preparation for injection Poor stability, long-term placement of related substances increases a lot, pH value changes greatly, and cannot meet the quality requirements within the validity period. The invention provides a stable aztreonam / arginine composition preparation and its preparation method , solved the above problems, and provided more reliable technical support for the use of aztreonam for injection

Method used

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  • Stable aztreonam composition and preparation method thereof
  • Stable aztreonam composition and preparation method thereof

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Embodiment 1

[0043] β-Aztreonam 100g

[0044]L-Arginine 70g

[0045] Hydroxypropyl-β-cyclodextrin (HP-β-CD) 120g

[0046] Water for injection 5000ml

[0047] Preparation Process:

[0048] Add sterile β-aztreonam to the reaction kettle at room temperature and suspend it in water for injection; add sterile L-arginine to adjust the pH value and dissolve it completely to obtain an aqueous solution of aztreonam / arginine; After adding, adjust the pH value to 6.0 to completely dissolve β-aztreonam; add hydroxypropyl-β-cyclodextrin (HP-β-CD) to the reaction kettle, stir and clathrate for 1.0 hour; add water for injection to dilute to the The mass concentration is required, then filtered through a 0.45 μm microporous membrane, and finally filtered through a 0.22 μm microporous membrane, subpackaged, and freeze-dried to obtain aztreonam freeze-dried powder for injection.

Embodiment 2

[0050] β-Aztreonam 100g

[0051] L-Arginine 75g

[0052] Hydroxypropyl-β-cyclodextrin (HP-β-CD) 150g

[0053] Water for injection 2500ml

[0054] Preparation Process:

[0055] Add sterile β-aztreonam to the reaction kettle at room temperature and suspend it in water for injection; add sterile L-arginine to adjust the pH value and dissolve it completely to obtain an aqueous solution of aztreonam / arginine; After adding, adjust the pH value to 6.5 to completely dissolve the sterile β-aztreonam; add hydroxypropyl-β-cyclodextrin (HP-β-CD) to the reaction kettle, stir and clathrate for 1.5 hours; add water for injection to dilute to the desired mass concentration, then filtered through a 0.45 μm microporous membrane, and finally filtered through a 0.22 μm microporous membrane, and then packaged to obtain aztreonam injection.

Embodiment 3

[0057] β-Aztreonam 200g

[0058] L-Arginine 120g

[0059] Hydroxypropyl-β-cyclodextrin (HP-β-CD) 200g

[0060] Water for injection 2000ml

[0061] Preparation Process:

[0062] Add sterile β-aztreonam to the reaction kettle at room temperature and suspend it in water for injection; add sterile L-arginine to adjust the pH value and dissolve it completely to obtain an aqueous solution of aztreonam / arginine; After adding, adjust the pH value to 7.0 to completely dissolve the sterile β-aztreonam; add hydroxypropyl-β-cyclodextrin (HP-β-CD) to the reaction kettle, stir and clathrate for 2.0 hours; add water for injection to dilute to the desired mass concentration, then filtered through a 0.45 μm microporous membrane, and finally filtered through a 0.22 μm microporous membrane, subpackaged, and freeze-dried to obtain aztreonam freeze-dried powder for injection.

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Abstract

The invention belongs to the field of drug synthesis and preparations thereof, relates to a preparation method of an antibacterial drug, and particularly relates to a stable aztreonam composition and a preparation method thereof. The preparation method comprises the following steps: directly suspending aseptic beta-aztreonam in water, adding aseptic L-arginine to regulate the pH value for complete dissolution to obtain an aztreonam / arginine water solution, adding hydroxypropyl-beta-cyclodextrin (HP-beta-CD) into the water solution for clathration, subpackaging, and freeze-drying to obtain aztreonam for injection. The preparation method provided by the invention is simple and suitable for industrial production. After the aztreonam / arginine salt is clathrated by HP-beta-CD, the water solubility and stability of aztreonam are improved, the toxic and side effects of aztreonam are reduced, and the availability of aztreonam is improved.

Description

technical field [0001] The invention relates to an antibacterial drug and a preparation method thereof, in particular to a stable aztreonam composition and a preparation method thereof. Background technique [0002] Aztreonam is the first fully synthetic monocyclic β-lactam antibiotic on the market. Its chemical name is: [2S-[2α, 3β(z)]]-2-[[[1-(2-amino- 4-thiazolyl)-2-[(2-methyl-4-oxo-1-sulfo-3-azetidinyl)amino]-2-oxoethylene]amino]oxo] -2-Methylpropionic acid, molecular formula C 13 h 17 N 5 o 8 S 2 , molecular weight 435.43. It was first developed by Squibb, and it was first listed in Italy in 1984, followed by many countries in Europe and America, and in Japan in 1987. Because aztreonam is well tolerated, there are few chances of side effects, and it does not have common allergic reactions to penicillins and cephalosporins, nor does it have cross-allergic reactions with penicillins and cephalosporins. Responsive, efficient, broad-spectrum β-lactam antibiotics hav...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/427A61K47/40A61P31/04
Inventor 赵新祥李树英
Owner AMICOGEN CHINA BIOPHARM CO LTD