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Preparation method of fenbendazole microspheres

A technology of fenbendazole microspheres and fenbendazole, which is applied in the direction of medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, which can solve the problem of increased coccidiosis outbreaks and few developments. Deworming drugs, high cost of coccidiosis control, etc., to achieve the effect of prolonging the elimination half-life, increasing drug loading, and non-immunogenicity

Inactive Publication Date: 2015-04-01
ZHENGZHOU HOUYI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Large western pharmaceutical companies have rarely developed new anthelmintic drugs because of drug residues and the concept of green breeding, and many excellent anthelmintic drugs have been criticized for their water solubility and cannot meet the requirements of modern large-scale production in clinical use. These have resulted in fewer and fewer coccidia drugs available in the Chinese market, an increase in the number of coccidia outbreaks in the same batch of chickens, and the cost of coccidia control is getting higher and higher

Method used

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  • Preparation method of fenbendazole microspheres

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Effect test

Embodiment 1

[0010] The preparation method of the fenbendazole microspheres of the present embodiment, make fenbendazole microspheres according to the following steps:

[0011] 1) Take 1g of gelatin, add distilled water to make 5mL gelatin solution, swell completely in a warm water bath at 50°C, and then add 2g

[0012] Fenbendazole, stirred evenly to obtain the water phase;

[0013] 2) Take 24mL of liquid paraffin and 1.0-2.0% Span-80 6mL and mix them to obtain 30mL of oil phase;

[0014] 3) Add the water phase obtained in step 1) to the oil phase obtained in step 2), and stir evenly at a speed of 500 r / min, cool to 5°C, add 2 mL of glutaraldehyde cross-linking agent for cross-linking and solidification , the curing time is 20 minutes;

[0015] 4) Wash off the excess cross-linking agent with isopropanol, then wash off the liquid paraffin on the surface of the microspheres with petroleum ether, and dry in vacuum to obtain fenbendazole microspheres. It was determined that the powder had ...

Embodiment 2

[0017] The preparation method of the fenbendazole microspheres of the present embodiment, make fenbendazole microspheres according to the following steps:

[0018] 1) Take 0.8g of gelatin, add distilled water to make 5mL of gelatin solution, swell completely in a warm water bath at 45°C, then add 1.5g of fenbendazole, stir evenly, and obtain the water phase;

[0019] 2) Take 25mL of liquid paraffin and 5mL of 1.0-2.0% Span-80 and mix them to obtain 30mL of oil phase;

[0020] 3) Add the water phase obtained in step 1) to the oil phase obtained in step 2), and stir evenly at a speed of 600 r / min, cool to 4°C, add 3 mL of glutaraldehyde cross-linking agent for cross-linking and solidification , the curing time is 30 minutes;

[0021] 4) Wash off the excess cross-linking agent with isopropanol, then wash off the liquid paraffin on the surface of the microspheres with petroleum ether, and dry in vacuum to obtain fenbendazole microspheres.

[0022] The microsphere powder with goo...

Embodiment 3

[0024] The preparation method of the fenbendazole microspheres of the present embodiment, make fenbendazole microspheres according to the following steps:

[0025] 1) Take 1.5g of gelatin, add distilled water to make 5mL of gelatin solution, swell completely in a warm water bath at 55°C, then add 1g of fenbendazole, stir evenly, and obtain the water phase;

[0026] 2) Take 30mL of liquid paraffin and 1.0-2.0% Span-80 5mL and mix them to obtain 35mL of oil phase;

[0027] 3) Add the water phase obtained in step 1) to the oil phase obtained in step 2), and stir evenly at a speed of 800 r / min, cool to 3°C, add 4 mL of glutaraldehyde cross-linking agent for cross-linking and solidification , the curing time is 40 minutes;

[0028] 4) Wash off the excess cross-linking agent with isopropanol, then wash off the liquid paraffin on the surface of the microspheres with petroleum ether, and dry in vacuum to obtain fenbendazole microspheres.

[0029] It has good roundness and good dispe...

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Abstract

The invention relates to a preparation method of fenbendazole microspheres, which comprises the following steps: (1) water phase preparation: taking gelatin and water, preparing a gelatin solution, heating to 45-55 DEG C, and adding fenbendazole until the gelatin concentration is 0.02-0.4 g / ml and the fenbendazole concentration is 0.01-0.5 g / ml; (2) oil phase preparation: taking liquid paraffin and 1.0-2.0 wt% Span 80, and mixing according to the volume ratio of (4-6):1; (3) adding the water phase in the step (1) into the oil phase in the step (2) according to the volume ratio of 1:(5-7), stirring, cooling to 5 DEG C below, and adding glutaric dialdehyde to perform crosslinking curing, wherein the volume ratio of the glutaric dialdehyde to the water phase in the step (3) is 1:(1-10); and (4) washing with isopropanol, washing with petroleum ether, and carrying out vacuum drying. The preparation method is simple to operate, has the advantages of cheap and accessible reagents, high simpleness and safety, environmental protection and lower preparation cost, and can easily implement popularization and application.

Description

technical field [0001] The invention relates to the technical field of veterinary medicine, in particular to a preparation method of fenbendazole microspheres. Background technique [0002] One of the bottlenecks in the treatment of coccidiosis today is that the drug resistance of coccidia is very serious, and the efficacy of the drugs continues to decline. The extensive use of anthelmintics has prompted the continuous emergence of drug-resistant strains. Large western pharmaceutical companies have rarely developed new anthelmintic drugs due to drug residues and the concept of green breeding, and many excellent anthelmintic drugs have been criticized due to their water solubility and cannot meet the requirements of modern large-scale production. These have resulted in fewer and fewer coccidiosis drugs available in the Chinese market, and the number of coccidia outbreaks in the same batch of chickens has increased, and the cost of coccidia control has become higher and highe...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/4184A61K47/42A61K47/44A61K47/26A61K47/08A61P33/02
Inventor 李亚娥张听盼王广霞
Owner ZHENGZHOU HOUYI PHARMA
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