Tilmicosin premix with fragrance and preparation method of tilmicosin premix

A technology of tilmicosin and premix, which is applied to medical preparations with non-active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. It can solve the problem of affecting the use of tilmicosin and causing negative psychodynamic effects , Difficulty in taking animals, etc., to achieve the effect of improving drug efficacy, accelerating absorption, and improving bioavailability

Active Publication Date: 2016-06-29
宁波科瑞特动物药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, intravenous injection of tilmicosin is prohibited. A single intravenous injection of 5 mg / kg can kill cattle, and it is also easy to kill pigs, horses and primates. The target organ of its toxicity is the heart, which can cause negative cardiodynamic effects.
Moreover, because tilmicosin tastes extremely bitter and is irritating to the gastrointestinal tract, it can cause symptoms such as anorexia, nausea and vomiting in livestock and poultry, and it is quite difficult for animals to take it, which seriously affects the use of tilmicosin

Method used

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  • Tilmicosin premix with fragrance and preparation method of tilmicosin premix

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Embodiment approach

[0055] As a preferred embodiment of the present invention, the molar ratio of polyamino acid to cyclodextrin in the polyamino acid-cyclodextrin complex is 1:1-100, more preferably, the molar ratio of polyamino acid to cyclodextrin is 1 : 10-30.

[0056] As a preferred embodiment of the present invention, the polyamino acid is one or more of polyglutamic acid, polyaspartic acid, poly-L-lysine, polylysine, preferably, the The polyamino acid is polyaspartic acid.

[0057] As a preferred embodiment of the present invention, the cyclodextrin is one or more of α-cyclodextrin, β-cyclodextrin, and γ-cyclodextrin, preferably, the cyclodextrin is beta-cyclodextrin.

[0058] As a preferred embodiment of the present invention, the binder is starch slurry, polyvinyl alcohol, hydroxypropylmethylcellulose, carboxymethylcellulose, hydroxyethylcellulose, hydroxypropylcellulose, etc. One or more mixtures, preferably, the binder is hydroxypropyl methylcellulose.

[0059] As a preferred embod...

Embodiment 1

[0069] (1) In a 100mL three-necked bottle, add 0.1g of polyaspartic acid, 1-2g of β-cyclodextrin and 50mL of hexamethylphosphoric triamide, stir well at room temperature; After reacting for 15-48 hours, settling and filtering in absolute ethanol to obtain polyaspartic acid-β-cyclodextrin complex;

[0070] (2) 5% by weight of hydroxypropyl methylcellulose, 20% by weight of starch and dextrin mixture, and 15% by weight of polyaspartic acid-β-cyclodextrin complex are added to distilled water, Heat at 50-80°C to dissolve; stir evenly and cool to obtain mixture A;

[0071] (3) Add 20% by weight of tilmicosin to the solution mixture A obtained in step (1), stir for 30-40 minutes, make a soft material, granulate, dry, and sieve.

Embodiment 2

[0073] The preparation method of the polyaspartic acid-β-cyclodextrin complex is the same as in Example 1.

[0074] (1) 5% by weight of hydroxypropyl methylcellulose, 20% by weight of starch and dextrin mixture, and 20% by weight of polyaspartic acid-β-cyclodextrin complex are added to distilled water, Heat at 50-80°C to dissolve; stir evenly and cool to obtain mixture A;

[0075] (2) Add 20% by weight of tilmicosin to the solution mixture A obtained in step (1), stir for 30-40 minutes, make a soft material, granulate, dry, and sieve.

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Abstract

The invention discloses tilmicosin premix with fragrance. The tilmicosin premix is prepared from raw materials including tilmicosin type compounds, an adhesive, a diluent and a polyamino acid-cyclodextrin compound, wherein the polyamino acid-cyclodextrin compound is obtained by chemically modifying polyamino acid with cyclodextrin. The invention further discloses a method for preparing the tilmicosin premix.

Description

technical field [0001] The invention relates to the field of medicaments for livestock and poultry, in particular to a tilmicosin premix and a preparation method thereof. Background technique [0002] Timicosin is a semi-synthetic macrolide antibiotic for livestock and poultry developed in the 1980s, with a molecular weight of 869.15. Tylosin is reacted with 3,5-dimethylpiperidine to generate tilmicosin base, and phosphoric acid and water are added to form tilmicosin phosphate, which is a mixture of cis-trans isomers. Tilmicosin is a very active product obtained by the amination reaction of aldehyde groups after the desugaration of tylosin. The amination reaction uses the Wallach reaction with formic acid as a catalyst, and can obtain a high yield of Tilmicosin. As a special antibiotic for livestock and poultry, tilmicosin has inhibitory effect on gram-positive bacteria, some gram-negative bacteria, mycoplasma, spirochetes, etc.; stronger antibacterial activity. It is ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/706A61K47/40A61K47/18A61P31/04
CPCA61K9/1617A61K9/1652A61K31/706
Inventor 郭瑞忠
Owner 宁波科瑞特动物药业有限公司
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