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Cefquinome sulfate lipidosome and preparation method thereof

A technology of cefquinol sulfate and quinol ester, which is applied in the direction of liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., and can solve the problems of low solubility, limited use and drug efficacy of cefquinol sulfate. Poor chemical stability and other problems, to achieve the effect of improving lung targeting, obvious lung targeting function, and low production cost

Active Publication Date: 2014-05-14
江西派尼生物药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Cefquinol sulfate has low solubility, poor chemical stability, and hygroscopicity
At present, the commonly used dosage form in clinical practice is mainly cefquinol sulfate suspension, and the existing dosage form limits its use and drug efficacy.
There is no report about cefquinol sulfate liposome

Method used

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  • Cefquinome sulfate lipidosome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1   preparation example 1

[0038] Cefquinol Sulfate Liposomal Prescription

[0039] Cefquinol Sulfate 100g

[0040] Egg Yolk Lecithin 300g

[0041] Cholesterol 150g

[0042] Vitamin E 10g

[0043] Sorbitol 50g

[0044] Cefquinol sulfate liposome preparation method is as follows

[0045] (1) Micronize cefquinol sulfate and pass through a 100-300 mesh sieve;

[0046] (2) Weigh egg yolk lecithin, cholesterol, and vitamin E in the prescribed amount, add 1500 mL of chloroform, stir in a water bath at 70°C, stir to dissolve, and evaporate on a rotary evaporator to make the chloroform solution of egg yolk lecithin, cholesterol, and vitamin E Form a film on the wall, and remove chloroform under reduced pressure;

[0047] (3) Weigh the prescribed amount of micronized cefquinol sulfate, fully dissolve it in 1000 mL of phosphate buffer with a pH value of 7.0, add the prescribed amount of sorbitol, and mix well;

[0048] (4) Add the product obtained in step (3) to the product obtained in step (2), rotate and...

Embodiment 2   preparation example 2

[0050] Cefquinol Sulfate Liposomal Prescription

[0051] Cefquinol Sulfate 100g

[0052] Soy Lecithin 600g

[0053] Cholesterol 200g

[0054] Vitamin E 15g

[0055] Tween 80 100g

[0056] Cefquinol sulfate liposome preparation method is as follows

[0057] (1) Powder cefquinol sulfate and pass through a 100-300 mesh sieve;

[0058] (2) Weigh the prescribed amount of soybean lecithin, cholesterol and vitamin E, add 1500mL of absolute ethanol, stir in a water bath at 80°C to dissolve, and rotate on a rotary evaporator to make soybean lecithin, cholesterol and vitamin E The water-ethanol solution forms a film on the wall, and the absolute ethanol is removed under reduced pressure;

[0059] (3) Weigh the prescribed amount of micronized cefquinol sulfate, fully dissolve it in 1500 mL of phosphate buffer with a pH value of 7.0, add the prescribed amount of Tween 80, and mix well;

[0060] (4) Add the product obtained in step (3) to the product obtained in step (2), rotate and...

Embodiment 3   preparation example 3

[0062] Cefquinol Sulfate Liposomal Prescription

[0063] Cefquinol Sulfate 80g

[0064] Egg Yolk Phosphatidylglycerol 200g

[0065] Cholesterol 100g

[0066] Vitamin E 3g

[0067] Trehalose 30g

[0068] Cefquinol sulfate liposome preparation method is as follows

[0069] (1) Powder cefquinol sulfate and pass through a 100-300 mesh sieve;

[0070] (2) Weigh egg yolk phosphatidylglycerol, cholesterol, and vitamin E, add 1500mL of acetone, stir in a water bath at 65°C to dissolve, and rotate on a rotary evaporator to make egg yolk phosphatidylglycerol, cholesterol, and vitamin E in acetone The solution forms a film on the wall, and the acetone is removed under reduced pressure;

[0071](3) Weigh the prescribed amount of micronized cefquinol sulfate, fully dissolve it in 1000 mL of phosphate buffer with a pH value of 7.4, add the prescribed amount of trehalose, and mix well;

[0072] (4) Add the product obtained in step (3) to the product obtained in step (2), rotate and st...

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Abstract

The invention relates to a cefquinome sulfate lipidosome and a preparation method thereof. The cefquinome sulfate lipidosome consists of cefquinome sulfate, phospholipid, cholesterol, vitamin E and a freeze-drying supporting agent. The preparation method comprises the following steps: adding phospholipid, cholesterol and vitamin E into an organic solvent to dissolve; dissolving cefquinome sulfate in a buffer liquid; and mixing, stirring and filtrating the products by a membrane obtained by the two steps to obtain the cefquinome sulfate lipidosome. The cefquinome sulfate lipidosome provided by the invention has good stability and encapsulation efficiency, and has a remarkable slow release effect after being delivered to animals.

Description

technical field [0001] The invention relates to a cefquinol sulfate liposome and a preparation method thereof. Background technique [0002] Cefquinol sulfate (Cefquinome sulfate), also known as cefquinome sulfate and cefquinome sulfate, is a fourth-generation cephalosporin antibiotic for animals. Cefquinome sulfate has a broad antibacterial spectrum and strong antibacterial activity. Both gram-positive bacteria and gram-negative bacteria have a strong killing effect. Especially for members of Staphylococcus aureus, Streptococcus, Pseudomonas aeruginosa and Escherichia coli have lower inhibitory concentrations. After intramuscular injection of cefquinol sulfate, the absorption is rapid, the peak time is fast, and the half-life (t 1 / 2 ) are short and have high bioavailability in vivo. At present, it has been approved by the European Commission for Veterinary Medicines (CVMP) for the clinical treatment of respiratory bacterial infections in pigs and cattle and mastitis in d...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/546A61K47/24A61P31/04
Inventor 李振
Owner 江西派尼生物药业有限公司
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