Aztreonam liposomes freeze-dry preparations and method of preparing the same

A technology of liposome freeze-drying and aztreonam, which is applied in the field of medicine, can solve the problems of poor stability of aztreonam, and achieve the effects of high encapsulation rate, reduced toxic and side effects, and low cost

Inactive Publication Date: 2008-08-27
HAINAN LINGKANG PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] In view of the poor stability of aztreonam in aqueous solution, it is not suitable to make liquid preparations, the object of the present invention is to provide a kind of aztreonam liposome preparation for injection with stable quality

Method used

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  • Aztreonam liposomes freeze-dry preparations and method of preparing the same
  • Aztreonam liposomes freeze-dry preparations and method of preparing the same
  • Aztreonam liposomes freeze-dry preparations and method of preparing the same

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Aztreonam 100g

[0031] Lecithin Distearate 50g

[0032] Phosphatidylglycerol Distearate 0.5g

[0033] Cholesterol 2g

[0034] Vitamin E 50mg

[0035] Citric acid 5g

[0036] Anhydrous sodium carbonate 5g

[0037] Sucrose 200g

[0038] Glycine 200g

[0039] Water for injection 5000ml

[0040] Preparation Process

[0041] (1) According to the formula, dissolve lecithin distearate, phosphatidylglycerol distearate, cholesterol and vitamin E in chloroform and mix evenly, remove the solvent in the solution under reduced pressure with a rotary evaporator to form a lipid film, and prepare 0.25mol / L citric acid solution, use citric acid solution to hydrate the lipid film, and the hydration temperature is generally between 50°C and 60°C to obtain a blank liposome suspension.

[0042] (2) After hydration is complete, liposomes are prepared with a high-pressure particle homogenizer until the average particle size is controlled at 100-120 nm, and the particle size and unif...

Embodiment 2

[0047] Aztreonam 3000g

[0048] Hydrogenated Soy Lecithin 18000g

[0049] Dimyristate Phosphatidylglycerol 12000g

[0050] Cholesterol 9000g

[0051] Vitamin E 100g

[0052] Succinic acid 15000g

[0053] Sodium hydroxide 21000g

[0054] Lactose 2000g

[0055] Glycine 4000g

[0056] Water for injection 50000ml

[0057]Preparation process: operate with reference to the steps of Example 1, (1) use 0.3mol / L succinic acid solution to hydrate the lipid film; (3) use 0.5mol / L aqueous sodium hydroxide solution to adjust the blank lipid liposome suspension to pH 7.2; (4) prepare 4.5% lactose aqueous solution and add 1.0% glycine as liposome dispersion.

Embodiment 3

[0059] Aztreonam 500g

[0060] Lecithin Distearate 3200g

[0061] Phosphatidylglycerol Distearate 680g

[0062] Cholesterol 950g

[0063] Vitamin E 12g

[0064] Citric acid 5600g

[0065] Anhydrous sodium carbonate 8000g

[0066] Sucrose 1200g

[0067] Glycine 1250g

[0068] Water for injection 10000ml

[0069] Preparation process: operate with reference to the steps of Example 1, (1) use 0.25mol / L citric acid to hydrate the lipid film; (3) use 0.8mol / L anhydrous sodium carbonate aqueous solution to adjust the blank lipid Plastid suspension to 7.6; (4) prepare 9% sucrose aqueous solution and add 1.0% glycine as liposome dispersion.

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Abstract

The invention discloses a freeze-dried preparation of aztreonam liposomes, wherein aztreonam is encapsulated in antioxidant-containing liposomes made of neutral phospholipids, negative charge phospholipids and cholesterol. The freeze-dried preparation has stable quality. Additionally, the aztreonam is encapsulated to minimize toxicity and adverse effects without affecting drug effectiveness.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to aztreonam liposome preparation for injection and a preparation method thereof. Background technique [0002] Aztreonam, the 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-methylpropanoic acid. Highly active against most aerobic Gram-negative bacteria, including Escherichia coli, Klebsiella pneumoniae and Oxitoella sp., Bacillus aerogenes, Bacillus cloacae, Proteus sp., Serratia sp. , Citrobacter, Shigella and other Enterobacteriaceae bacteria, as well as influenza bacillus, Neisseria gonorrhoeae, meningococcus, etc., which also have a good antibacterial effect on Pseudomonas aeruginosa. Aztreonam inhibits cell wall synthesis by binding to penicillin-binding protein 3 (PBP3) on the cell membrane of sensitive aerobic Gram-negative bacteria. Unlike most β-lactam antibiotics, it...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/427A61P31/04
Inventor 朱正兵
Owner HAINAN LINGKANG PHARMA CO LTD
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