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Method for preparing veterinary tilmicosin microspheres

A technology of tilmicosin and microspheres, which is applied in the field of preparation of tilmicosin microspheres for veterinary use, can solve the problems of tilmicosin limitation, animal death, negative mental force and the like, achieves low toxicity, reduced side effects, Low-cost effects of preparation

Active Publication Date: 2012-09-19
ZHENGZHOU HOUYI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Tilmicosin is irritating to a certain extent, and sometimes causes allergic reactions. In severe cases, it is very toxic to the heart. When injected intravenously or intramuscularly in too large a dose, it may cause negative heart force and cause animal death
Therefore, tilmicosin is mainly administered by oral administration or subcutaneous injection, which limits the clinical promotion of tilmicosin in veterinary medicine.

Method used

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  • Method for preparing veterinary tilmicosin microspheres

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The preparation method of the tilmicosin microspheres of the present embodiment comprises the steps:

[0030] Prepare the solution:

[0031] A Weigh 1g of dextran and 1g of tilmicosin, first add dextran to 5ml of distilled water and heat to dissolve to prepare a 20% dextran aqueous solution, then add tilmicosin into the dextran aqueous solution and stir well dissolved to obtain an aqueous phase;

[0032] B Take 50ml of castor oil with 10 times the volume of water added in A, add 0.6ml of Span-80, heat in a water bath and quickly stir to dissolve to obtain the oil phase;

[0033] Microsphere preparation:

[0034] 1) Preheat the water phase and oil phase prepared above to 60°C, add the water phase to the oil phase drop by drop under continuous stirring, then keep the temperature at 60°C and continue stirring for 10 minutes to obtain an emulsion;

[0035] 2) Place the emulsion in a cold water bath, stir quickly to cool down, when the temperature drops to 5°C, add pre-co...

Embodiment 2

[0038] The preparation method of the tilmicosin microspheres of the present embodiment comprises the steps:

[0039] Prepare the solution:

[0040] A Weigh 0.9g dextran and 0.7g tilmicosin, first add dextran to 5ml distilled water and heat to dissolve to prepare 18% dextran aqueous solution, then add tilmicosin to dextran aqueous solution Stir to fully dissolve to obtain the water phase;

[0041] B Take 40ml of castor oil with 8 times the volume of water added in A, add 0.6ml of Span-80, heat in a water bath and quickly stir to dissolve to obtain the oil phase;

[0042] Microsphere preparation:

[0043] 1) Preheat the water phase and oil phase prepared above to 65°C, add the water phase to the oil phase drop by drop under continuous stirring, then keep the temperature at 65°C and continue stirring for 10 minutes to obtain an emulsion;

[0044] 2) Put the emulsion in a cold water bath, stir rapidly to cool it down, when the temperature drops to 10°C, add pre-cooled acetone f...

Embodiment 3

[0047] The preparation method of the tilmicosin microspheres of the present embodiment comprises the steps:

[0048] Prepare the solution:

[0049] A Weigh 0.75g dextran and 0.38g tilmicosin, first add dextran to 5ml distilled water and heat to dissolve to prepare 15% dextran aqueous solution, then add tilmicosin to dextran aqueous solution Stir to fully dissolve to obtain the water phase;

[0050] B Take 45ml of castor oil with 9 times the volume of water added in A, add 0.45ml of Tween-80, heat in a water bath and quickly stir to dissolve to obtain the oil phase;

[0051] Microsphere preparation:

[0052] 1) Preheat the water phase and oil phase prepared above to 55°C, add the water phase to the oil phase drop by drop under constant stirring, then keep the temperature at 55°C and continue stirring for 10 minutes to obtain an emulsion;

[0053] 2) Place the emulsion in a cold water bath, stir quickly to cool it down, when the temperature drops to 7°C, add pre-cooled isopro...

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Abstract

The invention discloses a method for preparing veterinary tilmicosin microspheres, which prepares the microspheres by using glucosan to encapsulate a tilmicosin medicament and comprises the following steps of: firstly, preparing a water phase containing the glucosan and tilmicosin and an oil phase containing an emulsifying agent, and mixing the water phase and the oil phase uniformly at the temperature of between 55 and 65 DEG C; secondly, reducing the temperature of the mixed solution to between 5 and 10 DEG C; thirdly, adding a dehydrating agent into the mixed solution; and finally, stirring and filtering the mixture to obtain uncrosslinked microspheres, and performing crosslinking on the microspheres in a crosslinking agent to obtain the tilmicosin microspheres. The tilmicosin microspheres prepared by the method are mainly centralized at the lung in an animal body after being taken, have very good targeting performance, can treat bacterial infections at the lung of an animal, and have a very good curative effect; besides, the preparation method is simple, has low energy consumption, small toxicity and high safety and needs no special equipment, and the finally-prepared tilmicosin microspheres have high encapsulation efficiency and low preparation cost, and are suitable for mass production.

Description

technical field [0001] The invention relates to a preparation method of tilmicosin microspheres for animals, belonging to the technical field of veterinary medicines. Background technique [0002] Tilmicosin is a broad-spectrum antibacterial drug with similar antibacterial activity to other macrolides, and it can inhibit all Gram-positive bacteria and some Gram-negative bacteria, mycoplasma, spirochetes, etc. Especially against Actinobacillus pleuropneumoniae, Pasteurella hemolytica, Pasteurella multocida and mycoplasma, it has stronger antibacterial activity than tylosin. Moreover, it absorbs rapidly in the body, has a long elimination half-life, has good tissue penetration ability, and has a large distribution volume. It has high drug concentration in milk and lung and is eliminated slowly. Tilmicosin is irritating to a certain extent, and sometimes causes allergic reactions. In severe cases, it is very toxic to the heart. When it is injected intravenously or intramuscula...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/16A61K31/706A61K47/44A61P31/04
Inventor 吴红云陈卓董晓盈陈玮斌
Owner ZHENGZHOU HOUYI PHARMA
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