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A kind of ceftaroning nano-suspension freeze-dried powder and preparation method thereof

A nano-suspension, cefuroxime technology, applied in the field of cefuroxime preparations, can solve the problems of cefuroning insoluble in water, high organic solvent content, unfavorable popularization and application, etc., to improve chemical stability, stable Good performance, easy to popularize and apply

Active Publication Date: 2020-08-21
SOUTH CHINA AGRI UNIV +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Because ceftaroline is insoluble in water and oil, and easy to decompose, it greatly limits its clinical application in veterinary medicine
At present, the preparation of ceftaroning mainly includes ophthalmic ointment and breast infusion (oily suspension), and the shortcoming of oily suspension is that organic solvent content is high, and toxicity is bigger, and production cost is high, is unfavorable for popularizing and applying

Method used

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  • A kind of ceftaroning nano-suspension freeze-dried powder and preparation method thereof
  • A kind of ceftaroning nano-suspension freeze-dried powder and preparation method thereof
  • A kind of ceftaroning nano-suspension freeze-dried powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] A kind of preparation method of ceftaroning nano-suspension freeze-dried powder, comprises the steps:

[0036] 1) Accurately weigh 0.1g of hydroxypropyl methylcellulose (HPMC), add it into 100g of deionized water, and after fully dissolving, add 0.3g of soybean lecithin, ultrasonicate for 5 minutes to make it evenly mixed, and then add 3g of cefuroxime raw material, High-speed shearing at 12000 rpm for 10 min to obtain a coarse suspension. Then the coarse suspension is circulated 3 times at 200bar in a high-pressure homogenizer, 10 times at 500bar, and 15 times at 1000bar to obtain the cefuroxime nanosuspension.

[0037] 2) Take 5ml of the prepared ceftaroning nanosuspension and place it in a 15ml vial, add 0.25g of mannitol, stir evenly, place it in a -80°C ultra-low temperature refrigerator for pre-freezing for 24 hours, and transfer it quickly after taking it out Put it in a freeze dryer, freeze-dry at -70°C and 0.3mbar for 36-48h, and obtain the freeze-dried powder...

Embodiment 2

[0040] A kind of preparation method of ceftaroning nano-suspension freeze-dried powder, comprises the steps:

[0041] 1) Precisely weigh 0.5g of gum arabic powder, add it into 100g of deionized water, fully dissolve it, add 0.3g of soybean lecithin, mix it evenly by ultrasonication for 5min, then add 3g of cefuroxime raw material, and shear at 12000rpm for 10min, A coarse suspension was prepared. Then the coarse suspension is circulated 3 times at 200bar in a high-pressure homogenizer, 10 times at 500bar, and 15 times at 1000bar to obtain the cefuroxime nanosuspension.

[0042] 2) Take 5ml of the prepared ceftaroning nanosuspension and place it in a 15ml vial, add 0.25g of mannitol, stir evenly, place it in a -80°C ultra-low temperature refrigerator for pre-freezing for 24 hours, and transfer it quickly after taking it out Put it in a freeze dryer, freeze-dry at -70°C and 0.3mbar for 36-48h, and obtain the freeze-dried powder of cefuroxime nano-suspension.

[0043] The obtai...

Embodiment 3

[0045]A kind of preparation method of ceftaroning nano-suspension freeze-dried powder, comprises the steps:

[0046] 1) Accurately weigh 0.1g of hydroxypropyl methylcellulose (HPMC), add 100g of deionized water, fully dissolve, add 0.3g of glycine, and ultrasonically mix for 5min, then add 3g of cefuroxime raw material, 12000rpm high speed Cut for 10 min to obtain a coarse suspension. Then the coarse suspension is circulated 3 times at 200bar in a high-pressure homogenizer, 10 times at 500bar, and 15 times at 1000bar to obtain the cefuroxime nanosuspension.

[0047] 2) Take 5ml of the prepared ceftaroning nanosuspension and place it in a 15ml vial, add 0.25g of mannitol, stir evenly, place it in a -80°C ultra-low temperature refrigerator for pre-freezing for 24 hours, and transfer it quickly after taking it out Put it in a freeze dryer, freeze-dry at -70°C and 0.3mbar for 36-48h, and obtain the freeze-dried powder of cefuroxime nano-suspension.

[0048] The obtained freeze-d...

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Abstract

The invention discloses cefalonium nanosuspension freeze-dried powder and a preparation method of the cefalonium nanosuspension freeze-dried powder. The cefalonium nanosuspension freeze-dried powder is prepared from the following components in parts by weight: 1-5 parts of cefalonium raw drug, 0.1-0.5 part of a surfactant, 0.1-0.5 part of a suspending aid, and 1-10 parts of a freeze-drying protective agent. The cefalonium nanosuspension freeze-dried powder prepared by adopting the preparation method disclosed by the invention has good stability, and is uniform in particle size distribution and good in redispersibility, and the solubility and bioavailability of cefalonium can be improved; an organic solvent is not used in a formula, the use of auxiliary materials is little, the toxic and side effects are small, a preparation process is simple, and the popularization and application are convenient. The cefalonium nanosuspension freeze-dried powder disclosed by the invention has good inhibitory activity for clinical isolates of staphylococcus aureus, streptococcus and escherichia coli.

Description

technical field [0001] The invention relates to a preparation of cefuroxime, in particular to a cefuroxime nano-suspension freeze-dried powder and a preparation method thereof. Background technique [0002] The molecular formula of ceftaroline is C 20 h 18 N 4 o 5 S 2 , with a molecular weight of 458.5. Cefalonine belongs to the first generation of semi-synthetic cephalosporin broad-spectrum antibiotics. It is a specific drug for the prevention and treatment of mastitis in dry milk cows. It has the advantages of broad antibacterial spectrum, strong bactericidal power, less allergic reactions, and low toxicity. Its mechanism of action is to lose its activity by binding to one or more penicillin-binding proteins located on the cell wall of sensitive bacteria, thereby hindering the synthesis of the cell wall of the bacteria, changing the permeability of the cell wall, increasing the osmotic pressure of the cells in the bacteria, and breaking the cell membrane. Body lysis ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K9/10A61K31/546A61K47/32A61K47/24A61K47/40A61K47/44A61K47/10A61K47/36A61K47/38A61K47/26A61P31/04
CPCA61K9/10A61K9/19A61K31/546A61K47/10A61K47/24A61K47/26A61K47/32A61K47/36A61K47/38A61K47/40A61K47/44Y02A50/30
Inventor 方炳虎王琴陈良柱余鹏灵潘志坤
Owner SOUTH CHINA AGRI UNIV
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