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A cefquinome sulfate lung targeting liposome preparation and preparation method thereof

A technology of cefquinoxime sulfate and liposome preparation, applied in the field of medicine, can solve the problems of injection site damage, high preparation cost, drug waste and the like, and achieve the effects of stable quality and reliable curative effect

Active Publication Date: 2017-11-10
AMICOGEN CHINA BIOPHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The cefquinome sulfate preparation currently on the market is an oil injection, which is thicker and difficult to pass through the needle. It will cause pain to the animal during injection and may cause damage to the injection site, resulting in local tissue necrosis, and only a small amount of medicine can Reaching the lesion site will cause waste of drugs, increase the possibility of toxic side effects and drug resistance, and the preparation cost is high

Method used

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  • A cefquinome sulfate lung targeting liposome preparation and preparation method thereof
  • A cefquinome sulfate lung targeting liposome preparation and preparation method thereof
  • A cefquinome sulfate lung targeting liposome preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] A cefquinome sulfate lung-targeted liposome preparation is composed of the following components by weight:

[0032]

[0033] Specific steps are as follows:

[0034] (1) Precisely weigh 150g of egg yolk lecithin, 30g of cholesterol, and 0.02g of PG in 300ml of chloroform-methanol solution, and place them in a reaction vessel. The organic solvents will be removed by rotary evaporation under reduced pressure in a water bath at 35°C to form a uniform and transparent surface 的膜;

[0035] (2) Add 1g D-mannose and 20g cefquinome sulfate to 500ml water for injection, add 2mol / L sodium hydroxide solution until the drug is dissolved, add 0.2mol / L phosphate buffer to adjust the pH to 6.5, add the solution Go to the reaction vessel containing liposome film obtained in step 1), stir and emulsify and hydrate for 30 minutes at 25°C under normal pressure at a speed of 300r / min, then heat up to 30°C and stir and emulsify for 1 hour to obtain a liposome solution. 5g of sucrose is dissolved in ...

Embodiment 2

[0039] A cefquinome sulfate lung-targeted liposome preparation is composed of the following components by weight:

[0040]

[0041] Specific steps are as follows:

[0042] (1) Precisely weigh 180g egg yolk lecithin, 50g cholesterol, and 0.05g BHA in 360ml chloroform-methanol solution, place them in a reaction vessel, and remove the organic solvents by rotary evaporation under reduced pressure in a water bath at 35°C, forming a uniform and transparent surface on the vessel wall 的膜;

[0043] (2) Add 2g D-mannose and 25g cefquinome sulfate to 500ml water for injection, add 2mol / L sodium hydroxide solution until the drug is dissolved, add 0.2mol / L phosphate buffer to adjust the pH to 6.5, add the solution Go to the reaction vessel containing liposome film obtained in step 1), stir and emulsify and hydrate for 30 minutes at 25°C under normal pressure at a speed of 300r / min, then heat up to 30°C and stir and emulsify for 1 hour to obtain a liposome solution. 8g of mannitol was dissolved i...

Embodiment 3

[0047] A cefquinome sulfate lung-targeted liposome preparation is composed of the following components by weight:

[0048]

[0049]

[0050] Specific steps are as follows:

[0051] (1) Precisely weigh 20Kg egg yolk lecithin, 6Kg cholesterol, and 10g BHT in 40L chloroform-methanol solution, and place them in a reaction vessel. The organic solvent is removed by rotary evaporation under reduced pressure in a water bath at 35°C, forming a uniform and transparent surface on the wall film;

[0052] (2) Add 300g mannitol and 3Kg cefquinome sulfate to 50L water for injection, add 2mol / L sodium hydroxide solution until the drug is dissolved, add 0.2mol / L phosphate buffer to adjust the pH to 6.5, add the solution to the step 1) In the resulting reaction vessel containing the liposome film, stir emulsify and hydrate for 30 minutes at 25°C under normal pressure at a speed of 300r / min, and then heat to 30°C, stir and emulsify for 1 hour, to obtain liposome solution, and then add 1Kg of seaweed ...

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Abstract

The invention belongs to the field of medicine, and relates to a new dosage form of veterinary medicine, in particular to a cefquinome sulfate lung-targeting liposome preparation and a preparation method thereof. The cefquinome sulfate lung-targeting liposome preparation provided by the invention has the advantages of good targeting, stable quality, high encapsulation efficiency and the like. The cefquinome sulfate lung-targeted liposome provided by the present invention is easy to use, has active and passive targeting effects, and the drug concentrates in the target organ after injection to take effect, reduces the loss of the drug, improves the curative effect, and reduces the effect on the Toxic side effects in other organs.

Description

Technical field [0001] The invention belongs to the field of medicine, and relates to a new dosage form of veterinary medicine, in particular to a cefquinome sulfate lung-targeted liposome preparation and a preparation method thereof. Background technique [0002] Cefquinome is a fourth-generation cephalosporin antibiotic for animals. It is a broad-spectrum and highly effective cephalosporin antibiotic. Compared with the third-generation cephalosporin, it has a broader antibacterial spectrum and a stronger bactericidal effect. Its intrinsic antibacterial activity is stronger than that of the first three generations of cephalosporins. Compared with the first three generations of cephalosporins, the fourth generation of cephalosporins has a small dosage, strong sensitivity to bacteria, long plasma half-life and five nephrotoxicity. It has strong killing effect on Staphylococcus aureus, Streptococcus, Pseudomonas aeruginosa, Enterobacteriaceae (E. coli, Salmonella, Citrobacter Klebs...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K31/546A61K47/26A61P11/00
Inventor 胡维智李建国杨申永王玲
Owner AMICOGEN CHINA BIOPHARM CO LTD
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