Tilmicosin sustained release enteric-coated powder, preparation method and application thereof

A tilmicosin and enteric-coated technology, which is applied in the field of preparation of animal drugs, can solve the problems of fast release speed, poor palatability, and weak acid resistance, and achieve the effects of preventing premature release, convenient medication, and preventing burst release

Active Publication Date: 2017-07-07
SOUTH CHINA AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved in the present invention is to provide a slow release in the intestinal tract through an acid-resistant environment for the existing tilmicosin preparations, which are poor in palatability, weak in acid resistance, and too fast in the body of livestock and poultry. Good taste effect tilmicosin sustained-release enteric-coated powder

Method used

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  • Tilmicosin sustained release enteric-coated powder, preparation method and application thereof
  • Tilmicosin sustained release enteric-coated powder, preparation method and application thereof
  • Tilmicosin sustained release enteric-coated powder, preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] Follow the steps below to prepare tilmicosin sustained-release enteric-coated powder:

[0042] S1. Weigh 35% of cholesterol, 5% of tilmicosin raw material, and 60% of cellulose acetate phthalate according to the proportion, heat and melt the cholesterol at 80°C, and mix evenly to obtain a mixture;

[0043] S2. Add the tilmicosin raw material to the mixture described in step S1, and stir evenly to obtain the mixture;

[0044] S3. Add cellulose acetate phthalate to the mixture described in step S2, and stir evenly at 45° C. to obtain a mixture;

[0045] S4. The mixture described in step S3 is atomized, and cooled by a fluidized bed to make a powder, the temperature of the fluidized air is 28 ° C, and the linear velocity is 55 m / s;

[0046] S5. The powder described in step S4 is cooled, sieved, and collected to obtain 5% tilmicosin slow-release enteric-coated powder, with a particle size of about 100 mesh;

Embodiment 2

[0048] Follow the steps below to prepare tilmicosin sustained-release enteric-coated powder:

[0049] S1. Weigh 30% of glyceryl palmitate, 10% of tilmicosin raw material, 60% of hypromellose phthalate according to the proportion, heat and melt glyceryl palmitate at 80°C, and mix evenly to obtain a mixture;

[0050] S2. Add the tilmicosin raw material to the mixture described in step S1, and stir evenly to obtain the mixture;

[0051]S3. adding hypromellose phthalate to the mixture described in step S2, and stirring evenly at 45° C. to obtain a mixture;

[0052] S4. The mixture described in step S3 is atomized, cooled in a fluidized bed to make powder, the temperature of the fluidized air is 15°C, and the linear velocity is 75 m / s;

[0053] S5. The powder described in step S4 is cooled, sieved, and collected to obtain 10% tilmicosin slow-release enteric-coated powder, with a particle size of about 200 mesh;

Embodiment 3

[0055] Follow the steps below to prepare tilmicosin sustained-release enteric-coated powder:

[0056] S1. Weigh 25% of castor oil wax, 20% of tilmicosin raw material, 55% of No. Ⅱ polyacrylic acid resin according to the proportion, heat and melt castor oil wax at 100°C, and mix evenly to obtain a mixture;

[0057] S2. Add the tilmicosin raw material to the mixture described in step S1, and stir evenly to obtain the mixture;

[0058] S3. Add No. II polyacrylic acid resin to the mixture described in step S2, and stir evenly at 85° C. to obtain a mixture;

[0059] S4. Atomize the mixture described in step S3, and cool it in a fluidized bed to form a powder, the temperature of the fluidized air is 25°C, and the linear velocity is 95 m / s;

[0060] S5. The powder described in step S4 is cooled, sieved, and collected to obtain 20% tilmicosin slow-release enteric-coated powder, with a particle size of about 120 mesh;

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Abstract

The invention discloses a tilmicosin sustained release enteric-coated powder, a preparation method and application thereof. The tilmicosin sustained release enteric-coated powder comprises the following components by mass percentage: 5-40% of tilmicosin; 10-50% of a hydrophobic carrier; and 20-60% of an enteric material. Specifically, the hydrophobic carrier is one or more of cholesterol, palmitin or castor oil wax; the enteric material includes one or more of cellulose acetate phthalate, hydroxypropyl methyl cellulose phthalate or polyacrylic resin II. According to the tilmicosin sustained release enteric-coated powder provided by the invention, on the one hand, drugs are included in the hydrophobic carrier, and the palatability of enteric-coated powder is improved; and on the other hand, the acid resistance of the drugs is improved, so that drugs can be disintegrated and released after reaching the intestinal environment, the plasma concentration in livestock is relatively stable, the cardiotoxicity of tilmicosin is greatly reduced, at the same time, the effective plasma concentration maintenance time is significantly prolonged, the times of administration is reduced, and man power is saved.

Description

technical field [0001] The invention belongs to the technical field of preparation of animal medicines, in particular relates to a medicine for treating respiratory tract infection in livestock and poultry, more specifically relates to a tilmicosin slow-release enteric-coated powder and its preparation method and application. Background technique [0002] In the 1980s, the British Elanco Company synthesized the macrolide broad-spectrum antibiotic tilmicosin using the hydrolyzate of tylosin as a precursor. Tilmicosin is an animal-specific antibiotic, which is currently on the market in many countries including my country. It is mainly used to treat infectious diseases caused by sensitive bacteria in pigs, cattle, goats, sheep, broilers, turkeys and other animals, especially For respiratory infections in livestock and poultry. Tilmicosin has high antibacterial activity and special pharmacokinetic characteristics, making it sensitive to all Gram-positive bacteria, some Gram-neg...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/706A61K47/38A61K47/32A61K47/28A61K47/14A61K47/44A61P31/04A61P11/00
CPCA61K9/0002A61K9/145A61K9/146A61K31/706Y02A40/70
Inventor 黄显会魏开赟张申
Owner SOUTH CHINA AGRI UNIV
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