Compound tilmicosin solid dispersing agent and preparation method thereof

A technology of solid dispersant and tilmicosin, which is applied in the field of compound tilmicosin solid dispersant and its preparation, can solve problems affecting pig feed intake, micosin instability, easy degradation of gastric mucosa, etc., and achieve The effect of restoring the immune activity of macrophages, improving bioavailability, and mediating immune function

Inactive Publication Date: 2017-05-10
WUHAN XINLIANDA BIOLOGY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although tilmicosin has the above advantages, tilmicosin itself is irritating to a certain extent and can cause allergic reactions. In severe cases, it has great toxicity to the heart. Sexual stress, leading to animal death, so tilmicosin is mainly administered orally or subcutaneously
[0004] At present, there are many tilmicosin preparations on the market at home and abroad, but most of them are powders, which are too bitter to be used according to the recommended dose in the Pharmacopoeia (200-400g / ton of feed, calculated according to the active substance of tilmicosin). Seriously affect the feed intake of pigs
When administered orally, because tilmicosin tastes extremely bitter and has an odor, the palatability is poor; on the other hand, micosin is unstable in the stomach, easily degraded and irritating to the gastric mucosa It will cause adverse symptoms such as anorexia, nausea, and vomiting in livestock and poultry, and even some animals will refuse to eat when they smell the smell of tilmicosin, resulting in the failure of drug administration.

Method used

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  • Compound tilmicosin solid dispersing agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] The preparation method of the compound tilmicosin solid dispersant comprises the following steps: dissolving Eudragit L-100 in 10 times the weight of ethanol according to 1.0% of the total solid dispersant, stirring for 30 minutes to present a clear solution, Add respectively 0.2% sodium bisulfite and 10% tilmicosin according to the total amount of solid dispersant, dissolve, and shear in a high-speed shear homogenizer for 30 minutes, then transfer to a vacuum drying oven, and keep the temperature at 60°C to dry, take out, grind and pulverize through 80-mesh sieve to obtain carrier core layer. Then drop into respectively the povidone by 2% of the total amount of solid dispersant, 0.5% lysozyme by the total amount of solid dispersant, 0.5% aperidin and anhydrous glucose by the total amount of solid dispersant, mix After uniformity, granulate with purified water, the amount of pure water accounts for 2% of the total weight of the granular compound amoxicillin solid disper...

Embodiment 2

[0034] A kind of compound tilmicosin solid dispersion, its component and corresponding weight percentage are: tilmicosin 20%, lysozyme 0.8%, terme B 0.8%, Eudragit L-100 1.5%, hydrogen sulfite Sodium 0.4%, povidone 3%, the balance is anhydrous glucose;

[0035] Eudragit L-100 was dissolved in 20 times the weight of ethanol, and the amount of the above-mentioned pure water accounted for 3% of the total weight of the granular compound amoxicillin solid dispersion, and the other steps were the same as in Example 1.

Embodiment 3

[0037]A compound tilmicosin solid dispersant, the components and corresponding weight percentages are: tilmicosin 20%, lysozyme 1.0%, termicosin 1.0%, Eudragit L-100 1.5%, sodium bisulfite 0.4%, povidone 3%, the balance is anhydrous glucose;

[0038] Dissolve Eudragit L-100 in 30 times the weight of ethanol, and the stirring time is 40 minutes; the amount of the above-mentioned pure water accounts for 4% of the total weight of the granular compound amoxicillin solid dispersion, other steps and examples 1 is the same.

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Abstract

The invention discloses a compound tilmicosin solid dispersing agent and a preparation method thereof. The compound tilmicosin solid dispersing agent comprises, by weight percentage, 1.0-2.0% of Eudragit L-100, 0.2-0.5% of sodium bisulfite, 10-30% of tilmicosin, 0.5-1% of lysozyme, 0.5-1% of aesculetin, 2-5% of polyvidone and the balance anhydrous dextrose. The solid dispersing agent prepared by the method has the advantages that the medicine effect of the tilmicosin is kept, bioavailability is increased evidently, good palatability is achieved, gastrointestinal tract irritation is avoided, cure rate can be increased greatly, controlled-release absorption is formed in the intestinal tract, plasma concentration is kept at the therapeutic dose for a long time, and the highest medicine utilization rate is achieved; in addition, the dispersing agent has an immunoregulation function and can recover macrophage immune activity.

Description

technical field [0001] The invention belongs to the technical field of veterinary medicine, and in particular relates to a compound tilmicosin solid dispersion and a preparation method thereof. Background technique [0002] Tilmicosin is a macrolide antibiotic specially used for livestock and poultry, with a broad antibacterial spectrum and strong antibacterial activity. It has inhibitory effect on Gram-positive bacteria and some Gram-negative bacteria, mycoplasma, spirochetes, etc. It is mainly used to treat infection diseases caused by sensitive bacteria in cattle, goats, sheep, dairy cows, pigs, chickens and other animals. [0003] Although tilmicosin has the above advantages, tilmicosin itself is irritating to a certain extent and can cause allergic reactions. In severe cases, it has great toxicity to the heart. Therefore, tilmicosin is mainly administered orally or subcutaneously. [0004] At present, there are many tilmicosin preparations on the market at home and ab...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/47A61K47/32A61K9/16A61P31/04A61P31/14A61P11/06A61P11/10A61P11/00A61K31/706A61K31/366
CPCA61K38/47A61K9/1635A61K31/366A61K31/706C12Y302/01017A61K2300/00
Inventor 童庆平黄恒袁林
Owner WUHAN XINLIANDA BIOLOGY
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