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Cefquinome sulfate lung-targeted liposome preparation and preparation method thereof

A technology of cefquinome sulfate and liposome preparation, which is applied in the field of medicine, can solve the problems of high preparation cost, damage to the injection site, and increased drug resistance of toxic and side effects, and achieve reliable curative effect and stable quality

Active Publication Date: 2015-08-12
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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  • Cefquinome sulfate lung-targeted liposome preparation and preparation method thereof
  • Cefquinome sulfate lung-targeted liposome preparation and preparation method thereof
  • Cefquinome sulfate lung-targeted liposome preparation and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] A cefquinome sulfate lung targeting liposome preparation consists of the following components in parts 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, dissolve them in 300ml of chloroform-methanol solution, place them in a reaction vessel, remove the organic solvent by rotary evaporation in a water bath at 35°C under reduced pressure, and form a uniform and transparent mixture on the wall of the vessel. film;

[0035] (2) Add 1gD-mannose and 20g cefquinome sulfate to 500ml water for injection, add 2mol / L sodium hydroxide solution until the drug dissolves, add 0.2mol / L phosphate buffer to adjust the pH to 6.5, add the solution to In the reaction vessel containing the liposome film obtained in step 1), stir, emulsify and hydrate for 30 minutes under normal pressure at 25 ° C, and the rotation speed is 300 r / min, then raise the temperature to 30 ° C and stir and emu...

Embodiment 2

[0039] A cefquinome sulfate lung targeting liposome preparation consists of the following components in parts by weight:

[0040]

[0041] Specific steps are as follows:

[0042] (1) Precisely weigh 180g of egg yolk lecithin, 50g of cholesterol, and 0.05g of BHA, dissolve them in 360ml of chloroform-methanol solution, put them in a reaction vessel, remove the organic solvent by rotary evaporation in a water bath at 35°C under reduced pressure, and form a uniform and transparent mixture on the wall of the vessel. film;

[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 to In the reaction vessel containing the liposome film obtained in step 1), stir, emulsify and hydrate for 30 minutes under normal pressure at 25 ° C, and the rotation speed is 300 r / min, then raise the temperature to 30 ° C and stir and ...

Embodiment 3

[0047] A cefquinome sulfate lung targeting liposome preparation consists of the following components in parts by weight:

[0048]

[0049]

[0050] Specific steps are as follows:

[0051] (1) Precisely weigh 20Kg egg yolk lecithin, 6Kg cholesterol, and 10g BHT, dissolve them in 40L chloroform-methanol solution, place them in a reaction vessel, remove the organic solvent by rotary evaporation in a water bath at 35°C under reduced pressure, and form a uniform and transparent layer on the wall of the vessel. 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, and add the solution to the step 1) In the reaction vessel containing the liposome film, stir, emulsify and hydrate for 30 minutes under normal pressure at 25°C, at a speed of 300r / min, then raise the temperature to 30°C and stir and emulsify for 1h to obtain ...

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Abstract

The invention belongs to the field of medicines, relates to a new veterinary drugpreparation and particularly relates to a cefquinome sulfate lung-targeted liposome preparation and a preparation method thereof. The cefquinome sulfate lung-targeted liposome preparation is good in targeting property, is stable in quality and is high in encapsulation efficiency, is convenient to use and has an active and passive targeting function. The preparation is concentrated at the targeted organ through injection and works, thereby reducing loss of the preparation, improving curative effects and reducing toxic and side effects on 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-targeting liposome preparation and a preparation method thereof. Background technique [0002] Cefquinoxime is the 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 wider antibacterial spectrum and 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 requires less dosage, has a strong sensitivity to treating bacteria, has a long plasma half-life, and is toxic to the kidneys. It has a strong killing effect on Staphylococcus aureus, Streptococcus, Pseudomonas aeruginosa, Enterobacteriaceae (Es...

Claims

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Application Information

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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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