Cefquinome liposome

A technology of cefquinoxime and liposome, applied in the field of pharmacy, can solve the problems of difficult preparation and low solubility of cefquinoxime, and achieve the effects of prolonging circulation time, reducing toxic reactions and reducing adverse reactions

Active Publication Date: 2014-08-27
HENAN SOAR VETERINARY PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, the solubility of cefquinome in water is extremely low, so there are certain difficulties when it is prepared into a preparation

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] The cefquinome liposome is mainly made of the following raw materials in parts by weight: 50 mg of cefquinome, 500 mg of lecithin, and 40 mg of cholesterol. It is a liquid preparation, prepared by thin film dispersion method: put cefquinome, lecithin, and cholesterol into an eggplant-shaped bottle, add 20ml of ethanol: acetone volume ratio = 2:1 mixed solvent, and ultrasonically dissolve the raw materials; The eggplant-shaped bottle was placed in a constant temperature water bath at 40°C for decompression and rotary evaporation to remove the organic solvent, and a layer of lipid film was formed on the inner wall of the bottle; slowly add 10ml of phosphate buffer (pH7.0), hydrate, vortex, and make The lipid film on the eggplant-shaped bottle is completely dissolved; the mixed solution is ultrasonically dispersed at room temperature (ultrasonic power 600W) for 30min, and the cefquinome liposome liquid preparation is obtained.

[0021] After testing, the average particle s...

Embodiment 2

[0023] Cefquinome liposome is mainly made of the following raw materials in parts by weight: 50 mg of cefquinome, 200 mg of soybean lecithin, 50 mg of cephalin, 20 mg of soybean isoflavone glucoside, 10 mg of vitamin E (additional agent), sodium cholate (additional agent) 0.15mg. It is a liquid preparation prepared by injection method: accurately weigh cefquinome, soybean lecithin, cephalin, soybean isoflavone glucoside and vitamin E, add 10ml of ethanol to dissolve it, and make a lipid solution; draw the Slowly inject the lipid solution into 30ml of physiological saline containing 0.5% sodium cholate (aqueous medium, 40°C). After the injection, use an electronic constant-speed stirrer to stir at a speed of 2000r / min until the ethanol is completely removed, and then homogenize under high pressure. (Homogeneous pressure 10000psi) treatment 5 times, promptly obtains cefquinome liposome liquid preparation, puts 4 ℃ of refrigerators and preserves for subsequent use.

[0024] ...

Embodiment 3

[0026]Cefquinome liposome is mainly made of the following raw materials in parts by weight: 100mg of cefquinome, 2000mg of hydrogenated lecithin, 50mg of cardiolipin, 800mg of soybean saponol, 50mg of stearic acid (additive), poloxamer 188 (addition) 100mg, glycerin (addition) 400mg, vitamin C (addition) 100mg. It is a liquid preparation prepared by melting method: accurately weigh cefquinome, hydrogenated lecithin, cardiolipin, soybean saponol and stearic acid, add it to a Erlenmeyer flask and heat it to 75°C to melt to obtain a lipid melt, Standby: Dissolve 100mg of poloxamer 188, 400mg of glycerol, and 100mg of vitamin C in 20ml of 5% glucose solution, heat to 75°C, add to the lipid melt, mix with high-speed shear, and homogenize under high pressure (homogeneous pressure 15000psi) to process 3 times to obtain the cefquinome liposome liquid preparation.

[0027] After testing, the average particle diameter of the liposomes in the liquid preparation was 47 nm, and the partic...

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Abstract

Cefquinome liposome, which belongs to the field of pharmaceutics, has a particle size of less than 1000 nm, and is mainly prepared from the following raw materials by weight: 1 part of cefquinome, 1-40 parts of phospholipid, 0-15 parts of sterol or soy isoflavone glucoside or soyasapogenol, and 0-15 parts of additives. The cefquinome liposome can be prepared into a liquid preparation, and can also be prepared into a solid preparation by adding a proper amount of a support agent. The cefquinome liposome or cefquinome long circulating liposome prepared in the invention contains no irritant substances, and can relieve anaphylactic reaction; the obtained preparation has good stability, has an average liposome particle size of less than 1000 nm, and has encapsulation efficiency of more than 80%. The preparation method is mature in process, simple, practical, and suitable for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a novel cefquinome preparation - cefquinome liposome. Background technique [0002] Cefquinome (English name: Cefquinome) is the fourth-generation cephalosporin antibiotics for animals. Its properties are white, off-white to light yellow powder. Its characteristics are: 1) Highly stable to β-lactamase; 2) Its intrinsic antibacterial properties The activity is stronger than the third-generation cephalosporin ceftiofur. Compared with the third-generation cephalosporin, the plasma half-life of the fourth-generation cephalosporin is longer and has no nephrotoxicity; 3) It has strong antibacterial activity against Staphylococcus aureus, streptococcus, Pseudomonas aeruginosa and Enterobacteriaceae (Escherichia coli, Salmonella, Klebsiella, Citrobacter, Serratia marcescens) have a strong killing effect on many methicillin-resistant staphylococci and Enterobacter also has a good kill...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/546A61P31/04
Inventor 孙江宏蒋增海郭建军张军强
Owner HENAN SOAR VETERINARY PHARMA
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