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Tilmicosin liposome injection and preparation method thereof

A technology of tilmicosin and injection, which is applied in the field of tilmicosin liposome injection and its preparation, can solve the problems of negative cardiac effect, few injections, and large side effects, so as to reduce toxic and side effects , The preparation process is simple, and the effect of increasing the blood drug concentration

Active Publication Date: 2012-01-25
河南省帝一方生物制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Tilmicosin has the following disadvantages: 1. The injection is absorbed quickly, but not completely; 2. The side effects are large, and the target organ of its toxic effect is the heart, which can cause negative cardiac effects and cause death
Due to these shortcomings of tilmicosin, most of the clinically used oral preparations are rarely used for injection.

Method used

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  • Tilmicosin liposome injection and preparation method thereof
  • Tilmicosin liposome injection and preparation method thereof
  • Tilmicosin liposome injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] For tilmicosin liposome injection, each 100ml injection contains the following components: 20ml propylene glycol, 3g soybean lecithin, 1.5g cholesterol, 1g Span 80, 1g Tween-80, 5g tilmicosin, the balance For injection water.

[0016] Dosing: Take 20ml of propylene glycol, add 3g of soybean lecithin, 1.5g of cholesterol, 1g of Span 80, 1g of Tween-80, 5g of tilmicosin, heat until dissolved, then add water to 100ml, stir while adding, until into an emulsified solution, added to a colloid mill to grind to a fine liquid, potted and sterilized to obtain tilmicosin liposome injection for animals.

[0017] Quality inspection: the obtained injection is a light yellow milky liquid; the content of tilmicosin is 5g / 100ml, and all inspections are in line with the provisions of the Chinese Veterinary Pharmacopoeia on emulsions, and the injection is valid for 2.43 years.

Embodiment 2

[0019] The tilmicosin liposome injection contains the following components per 100ml injection: 20ml oleic acid, 3g soybean lecithin, 1.5g cholesterol, 2g Tween-80, 6g tilmicosin, and the balance is water for injection.

[0020] Dosing: Take 20ml of oleic acid, add 3g of soybean lecithin, 1.5g of cholesterol, 2g of Tween-80, and 6g of tilmicosin, heat until dissolved, then add water to 100ml, and stir while adding until it becomes a milky solution. Add it into a colloid mill to grind to a fine liquid, potting and sterilizing to obtain the tilmicosin liposome injection for veterinary use.

[0021] Quality inspection: the obtained injection is a light yellow milky liquid; the content of tilmicosin is 6g / 100ml, and all inspections are in line with the provisions of the Chinese Veterinary Pharmacopoeia on emulsions, and the validity period of the injection is 2.36 years.

Embodiment 3

[0023] For tilmicosin liposome injection, every 100ml injection contains the following components: 20ml propylene glycol, 4g soybean lecithin, 2g cholesterol, 2g glycerol monostearate, 8g tilmicosin, and the balance is water for injection.

[0024] Dosing: Take 20ml of propylene glycol, add 4g of soybean lecithin, 2g of cholesterol, 2g of glyceryl monostearate, and 8g of tilmicosin, heat until dissolved, then add water to 100ml, and stir while adding until it becomes a milky solution. Add it into a colloid mill to grind to a fine liquid, potting and sterilizing to obtain the tilmicosin liposome injection for veterinary use.

[0025] Quality inspection: the obtained injection is a light yellow milky liquid; the content of tilmicosin is 8g / 100ml, and all inspections are in line with the provisions of the Chinese Veterinary Pharmacopoeia on emulsions, and the injection is valid for 2.47 years.

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Abstract

The invention belongs to the technical field of veterinary drugs, and particularly relates to a tilmicosin liposome injection and a preparation method thereof. The particle diameter of the tilmicosin liposome injection is 7-10mu m, and every 100ml of injection contains the following components: 5-10g of tilmicosin, 3-5g of soya bean lecithin, 1.5-2.5g of cholesterol, 2g of non-ionic surfactant, 20ml of solvent and the balance of water for injection. The tilmicosin liposome injection provided by the invention greatly reduces the toxic and side effects of the tilmicosin, and can improve the body immunity in use.

Description

technical field [0001] The invention belongs to the technical field of veterinary medicine, and in particular relates to a tilmicosin liposome injection and a preparation method thereof. Background technique [0002] Tilmicosin is a semi-synthesized antibiotic for livestock and poultry by a hydrolyzate of tylosin. Tilmicosin is a semi-synthetic macrolide compound with a large volume of distribution in the body, especially in the lung tissue And breast tissue showed higher drug concentration, mainly concentrated in alveolar macrophages, fibroblasts, bronchial mucosa, etc. It was first introduced into China by Eli Lilly and Company of the United States, and its greatest role is to treat respiratory diseases and mastitis in animals. In 2004, experiments abroad have proved that it can effectively control PRRS. The drug accumulates in porcine alveolar macrophages, and the drug concentration inside the cells is as high as 50 times that outside the cells. Alveolar macrophages are...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K9/10A61K31/706A61K47/28A61K47/34A61P11/00A61P15/14A61P31/04A61P31/14
Inventor 马改云张亚
Owner 河南省帝一方生物制药有限公司
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