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Preparation method of tilmicosin phosphate microsphere specifically for use on animals

A technology of tilmicosin phosphate and microspheres, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve problems such as poor palatability, and achieve improved encapsulation efficiency and stability The effect of good performance and good industrial application prospect

Active Publication Date: 2014-03-12
长沙施比龙动物药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] In view of the deficiencies in the prior art, the object of the present invention is to provide a preparation method for animal-specific tilmicosin phosphate microspheres, which uses light yellowish brown to light reddish brown granular tilmicosin phosphate bulk drug White tilmicosin phosphate microspheres with moderate drug loading and high encapsulation efficiency were obtained after specific coating, which solved the problem of poor palatability of the drug and better met production needs

Method used

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  • Preparation method of tilmicosin phosphate microsphere specifically for use on animals
  • Preparation method of tilmicosin phosphate microsphere specifically for use on animals
  • Preparation method of tilmicosin phosphate microsphere specifically for use on animals

Examples

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Effect test

Embodiment 1

[0024] A preparation method for animal-specific tilmicosin phosphate microspheres, the steps are as follows:

[0025] (1) Weigh 1.11g of acrylic resin RSPO and dissolve in 10mL of absolute ethanol to obtain solution A;

[0026] (2) Weigh 0.5g of tilmicosin phosphate crude drug, add it to 1.25g of soybean oil, stir well to obtain mixture B;

[0027] (3) Add solution A to mixture B, and mix thoroughly by ultrasonication for 1 min to obtain mixture C;

[0028] (4) Mix 0.75g SP-80, 0.5g silicon dioxide and 50mL liquid paraffin and place it in a water bath at 40°C. Stir at a speed of 900r / min, add the mixture C dropwise, and continue stirring in a water bath at 40°C after the drop is complete 1.0h, let absolute ethanol volatilize completely, obtain mixture D;

[0029] (5) Wash the mixture D with petroleum ether 3 times, each time with 20 mL of petroleum ether, discard the solution after shaking and centrifuging to wash away the liquid paraffin, then carry out vacuum filtration, a...

Embodiment 2

[0032] A preparation method for animal-specific tilmicosin phosphate microspheres, the steps are as follows:

[0033] (1) Weigh 0.53g of acrylic resin RSPO and dissolve in 10mL of absolute ethanol to obtain solution A;

[0034] (2) Weigh 0.25g of tilmicosin phosphate crude drug, add it to 0.625g of soybean oil, stir well to obtain mixture B;

[0035] (3) Add solution A to mixture B, and mix thoroughly by ultrasonication for 1 min to obtain mixture C;

[0036] (4) Mix 0.45g SP-80, 0.5g silicon dioxide and 50mL liquid paraffin and place it in a water bath at 40°C. Stir at a speed of 900r / min, add the mixture C dropwise, and continue stirring in a water bath at 40°C after dropping 1.5h, let the absolute ethanol volatilize completely, and obtain the mixture D;

[0037] (5) Wash the mixture D with petroleum ether 3 times, each time with 20 mL of petroleum ether, discard the solution after shaking and centrifuging to wash away the liquid paraffin, then carry out vacuum filtration,...

Embodiment 3

[0040] A preparation method for animal-specific tilmicosin phosphate microspheres, the steps are as follows:

[0041] (1) Weigh 1.11g of acrylic resin RSPO and dissolve in 10mL of absolute ethanol to obtain solution A;

[0042] (2) Weigh 0.375g of tilmicosin phosphate crude drug, add it to 0.625g of soybean oil, stir well to obtain mixture B;

[0043] (3) Add solution A to mixture B, and mix thoroughly by ultrasonication for 1 min to obtain mixture C;

[0044] (4) Mix 0.6g SP-80, 0.4g silicon dioxide and 40mL liquid paraffin and place it in a water bath at 40°C. Stir at a speed of 900r / min, add the mixture C dropwise, and continue stirring in a water bath at 40°C after dropping 2.0h, let the absolute ethanol volatilize to obtain the mixture D;

[0045] (5) Wash the mixture D with petroleum ether 3 times, each time with 20 mL of petroleum ether, discard the solution after shaking and centrifuging to wash away the liquid paraffin, then carry out vacuum filtration, and dry the ...

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Abstract

The invention belongs to the technical field of preparation of animal drugs, and particularly discloses a preparation method of a tilmicosin phosphate microsphere specifically for use on animals. The preparation method comprises the steps of: solving acrylic resin into absolute ethyl alcohol to make up a solution with a certain concentration; adding the soybean oil solution of the tilmicosin phosphate to obtain uniformly mixed phase; slowly dropping the mixed phase into liquid paraffin comprising Span 80 (SP80) and silicon dioxide; bathing in water and stirring at 40 DEG C to fully volatilize the absolute ethyl alcohol so as to form cured microsphere; centrifuging; removing the liquid paraffin on the surface of the microsphere through washing for many times by use of few petroleum ether, and drying at 40 DEG C to obtain the tilmicosin phosphate microsphere specifically for use on animals. The preparation method of tilmicosin phosphate microsphere specifically for use on animals has the advantages of simple operation in preparation technology and low requirement on preparation equipment and conditions. The prepared microsphere better solves the problem of drug palatability.

Description

technical field [0001] The invention belongs to the technical field of preparation of animal medicines, and in particular relates to a preparation method of special macrolide antibacterial drug tilmicosin phosphate microspheres for animals. Background technique [0002] Tilmicosin (tilmicosin) is a semi-synthesized antibiotic for livestock and poultry with tylosin as the precursor. It was developed by the British Elanco company in the 1980s. It has strong antibacterial activity, broad antibacterial spectrum, and resistance to It has low drug resistance and has inhibitory effects on all Gram-positive bacteria and some Gram-negative bacteria, spirochetes, mycoplasma, etc. Its phosphate is commonly used in veterinary clinics, but the palatability of the existing tilmicosin phosphate preparations is generally poor, which affects the feed intake of animals, thereby reducing the efficacy of the drug on diseases. Contents of the invention [0003] In view of the deficiencies in ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/706A61K47/44A61K47/32A61P31/04
Inventor 张卫元肖飞刘国庆陈翠兰崔海港张永丹李荣吴言术向光强
Owner 长沙施比龙动物药业有限公司
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