Aztreonam composition freeze-dried powder for injection

Abstract

The invention provides an aztreonam composition freeze-dried powder for injection, relating to the technical field of drugs and drug preparation. The aztreonam composition freeze-dried powder comprises the following raw material components in parts by weight: 9.47-11.58 parts of aztreonam, 4.74-5.79 parts of chitosan nanoparticles and 75.79-92.63 parts of water for injection. The aztreonam composition freeze-dried powder has the advantages: (1) a composition composed of aztreonam and chitosan nanoparticles according to the proportion of 1:0.5 not only can be used for improving the solubility of aztreonam in water, but also can be used for shortening the dissolving time of aztreonam so as to be beneficial for clinical application; (2) the composition can be used for remarkably enhancing the antibacterial effect of aztreonam and can be used for clinically reducing the dosage and adverse reaction of aztreonam, and an in-vitro experiment proves that 0.2g of aztreonam containing the chitosan nanoparticles has the same antibacterial effect with 0.4g of aztreonam not containing the chitosan nanoparticles; (3) the chitosan nanoparticles can be used as a freeze-dried skeleton agent of the freeze-dried powder for injection to replace arginine, so that the activation effect of arginine to human bodies is eliminated.

Description

Technical field:

[0001] The invention relates to the technical field of medicine and medicine manufacture, in particular to a freeze-dried powder injection of aztreonam composition for injection. Background technique:

[0002] Aztreonam is a synthetic monocyclic β-lactam antibiotic. Its antibacterial mechanism is that it can quickly pass through the outer membrane wall of Gram-negative aerobic cells, and has a high affinity for penicillin-binding protein 3 (PBP-3). By acting on PBP-3, it inhibits the synthesis of bacterial cell walls, resulting in Cell lysis and death. Aztreonam has a high degree of antibacterial activity against most aerobic Gram-negative bacteria, including Escherichia coli, Klebsiella pneumoniae and Oxitoella, Bacillus aerogenes, Bacillus cloacae, Serratia, Enterobacteriaceae such as Citrobacter and Shigella, as well as influenza bacilli, Neisseria gonorrhoeae, Neisseria meningitidis, etc., also have good antibacterial effects on Pseudomonas aeruginosa....

Examples

Embodiment 1

[0030] Embodiment 1. Preparation of aztreonam composition freeze-dried powder for injection, in 1000 vials.

[0031] prescription:

[0032] Aztreonam 250g

[0033] Chitosan Nanoparticles 100g

[0034] Water for injection 2000ml

[0035] 2. Preparation process:

[0036] (1) Weigh 250g of chitosan nanoparticles and slowly add them to 2000ml of water for injection, and stir until dissolved while adding.

[0037] (2) Add 500g of aztreonam and stir to dissolve until clear.

[0038] (3) Adjust the pH to 5.1 with buffer salts of sodium dihydrogen phosphate and disodium hydrogen phosphate, add 0.1% activated carbon and stir for 30 minutes, filter out the activated carbon, and filter the liquid through 0.45 μm and 0.22 μm microporous membranes to detect The intermediate content is calculated as 0.5g per bottle based on aztreonam.

[0039] (4) Fill according to the testing requirements, put it into a freeze dryer after half-tamping, cool down to -40°C, keep warm for 2 hours, slowl...

Embodiment 2

[0040] Example 2: Preparation of aztreonam composition freeze-dried powder for injection, in 1000 vials.

[0041] 1. Prescription:

[0042] Aztreonam 250g

[0043] Chitosan Nanoparticles 125g

[0044] Water for injection 2000ml

[0045] 2. Preparation process:

[0046] (1) Weigh 250g of chitosan nanoparticles and slowly add them to 2000ml of water for injection, and stir until dissolved while adding.

[0047] (2) Add 500g of aztreonam and stir to dissolve until clear.

[0048] (3) Adjust the pH to 5.1 with buffer salts of sodium dihydrogen phosphate and disodium hydrogen phosphate, add 0.1% activated carbon and stir for 30 minutes, filter out the activated carbon, and filter the liquid through 0.45 μm and 0.22 μm microporous membranes to detect The intermediate content is calculated as 0.5g per bottle based on aztreonam.

[0049] (4) Fill according to the testing requirements, put it into a freeze dryer after half-tamping, cool down to -40°C, keep warm for 2 hours, slowl...

Embodiment 3

[0050] Example 3: Preparation of aztreonam composition freeze-dried powder for injection, in 1000 vials.

[0051] prescription:

[0052] Aztreonam 250g

[0053] Chitosan Nanoparticles 150g

[0054] Water for injection 2000ml

[0055] 2. Preparation process:

[0056] (1) Weigh 300g of chitosan nanoparticles and slowly add to 2000ml of water for injection, stir until dissolved while adding.

[0057] (2) Add 500g of aztreonam and stir to dissolve until clear.

[0058] (3) Adjust the pH to 5.1 with buffer salts of sodium dihydrogen phosphate and disodium hydrogen phosphate, add 0.1% activated carbon and stir for 30 minutes, filter out the activated carbon, and filter the liquid through 0.45 μm and 0.22 μm microporous membranes to detect The intermediate content is calculated as 0.5g per bottle based on aztreonam.

[0059] (4) Fill according to the inspection requirements, and send it into the freeze dryer after half-tamping, and leave the box after freeze-drying, with good for...

Technical field:

[0001] The invention relates to the technical field of medicine and medicine manufacture, in particular to a freeze-dried powder injection of aztreonam composition for injection. Background technique:

[0002] Aztreonam is a synthetic monocyclic β-lactam antibiotic. Its antibacterial mechanism is that it can quickly pass through the outer membrane wall of Gram-negative aerobic cells, and has a high affinity for penicillin-binding protein 3 (PBP-3). By acting on PBP-3, it inhibits the synthesis of bacterial cell walls, resulting in Cell lysis and death. Aztreonam has a high degree of antibacterial activity against most aerobic Gram-negative bacteria, including Escherichia coli, Klebsiella pneumoniae and Oxitoella, Bacillus aerogenes, Bacillus cloacae, Serratia, Enterobacteriaceae such as Citrobacter and Shigella, as well as influenza bacilli, Neisseria gonorrhoeae, Neisseria meningitidis, etc., also have good antibacterial effects on Pseudomonas aeruginosa....

Examples

Embodiment 1

[0030] Embodiment 1. Preparation of aztreonam composition freeze-dried powder for injection, in 1000 vials.

[0031] prescription:

[0032] Aztreonam 250g

[0033] Chitosan Nanoparticles 100g

[0034] Water for injection 2000ml

[0035] 2. Preparation process:

[0036] (1) Weigh 250g of chitosan nanoparticles and slowly add them to 2000ml of water for injection, and stir until dissolved while adding.

[0037] (2) Add 500g of aztreonam and stir to dissolve until clear.

[0038] (3) Adjust the pH to 5.1 with buffer salts of sodium dihydrogen phosphate and disodium hydrogen phosphate, add 0.1% activated carbon and stir for 30 minutes, filter out the activated carbon, and filter the liquid through 0.45 μm and 0.22 μm microporous membranes to detect The intermediate content is calculated as 0.5g per bottle based on aztreonam.

[0039] (4) Fill according to the testing requirements, put it into a freeze dryer after half-tamping, cool down to -40°C, keep warm for 2 hours, slowl...

Embodiment 2

[0040] Example 2: Preparation of aztreonam composition freeze-dried powder for injection, in 1000 vials.

[0041] 1. Prescription:

[0042] Aztreonam 250g

[0043] Chitosan Nanoparticles 125g

[0044] Water for injection 2000ml

[0045] 2. Preparation process:

[0046] (1) Weigh 250g of chitosan nanoparticles and slowly add them to 2000ml of water for injection, and stir until dissolved while adding.

[0047] (2) Add 500g of aztreonam and stir to dissolve until clear.

[0048] (3) Adjust the pH to 5.1 with buffer salts of sodium dihydrogen phosphate and disodium hydrogen phosphate, add 0.1% activated carbon and stir for 30 minutes, filter out the activated carbon, and filter the liquid through 0.45 μm and 0.22 μm microporous membranes to detect The intermediate content is calculated as 0.5g per bottle based on aztreonam.

[0049] (4) Fill according to the testing requirements, put it into a freeze dryer after half-tamping, cool down to -40°C, keep warm for 2 hours, slowl...

Embodiment 3

[0050] Example 3: Preparation of aztreonam composition freeze-dried powder for injection, in 1000 vials.

[0051] prescription:

[0052] Aztreonam 250g

[0053] Chitosan Nanoparticles 150g

[0054] Water for injection 2000ml

[0055] 2. Preparation process:

[0056] (1) Weigh 300g of chitosan nanoparticles and slowly add to 2000ml of water for injection, stir until dissolved while adding.

[0057] (2) Add 500g of aztreonam and stir to dissolve until clear.

[0058] (3) Adjust the pH to 5.1 with buffer salts of sodium dihydrogen phosphate and disodium hydrogen phosphate, add 0.1% activated carbon and stir for 30 minutes, filter out the activated carbon, and filter the liquid through 0.45 μm and 0.22 μm microporous membranes to detect The intermediate content is calculated as 0.5g per bottle based on aztreonam.

[0059] (4) Fill according to the inspection requirements, and send it into the freeze dryer after half-tamping, and leave the box after freeze-drying, with good for...

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