A kind of microporous membrane controlled-release coating tilmicosin pellets and preparation method thereof

Abstract

The invention discloses a micro-porous membrane release-controlling coating tilmicosin pellet and a preparation method thereof. The micro-porous membrane release-controlling coating tilmicosin pellet comprises a pill-containing core and a release-controlling coating layer in turn from inner to outer, wherein the pill-containing core is composed of a main ingredient and an auxiliary material in the proportion of 10-30%: 70-90%; the main ingredient is composed of tilmicosin phosphate with excellent solubility and indissolvable tilmicosin alkali in the proportion of 25-100:0-75%; the auxiliary material comprises one or more of microcrystalline cellulose, starch, lactose, dextrin, sodium carboxymethyl starch and sodium carboxymethylcellulose; the release-controlling coating layer is composed of insoluble polymer in gastrointestinal tract, dissoluble or falling pore-foaming agent, plasticizer and anti-plastering reagent in the proportion of 80-85%: 3-5%:0.3%-0.5%:10-15%. The micro-porous membrane release-controlling coating tilmicosin pellet can cover bitter taste and can dissolve out the effective constituent; the constant long-acting blood concentration is ensured; the defect of discharging drug before completely releasing is overcome.

Description

Technical field [0001] The invention relates to the field of animal drug preparations, and more specifically, to a microporous membrane controlled release coated tilmicosin pellets and a preparation method thereof. Background technique [0002] Tilmicosin is an animal-specific macrolide antibiotic with strong antibacterial activity. It has been widely used in the prevention and treatment of infectious diseases in pigs, cattle, sheep, chickens and other animals. However, Tilmicosin tastes extremely bitter. The existing oral solid dosage forms at home and abroad, such as soluble powder, premix, etc., generally suffer from the problem of bitter taste and strong irritation which lead to animal refusal to eat. For example: 20% Tilmicosin premix is ​​given to pigs by mixing. When the dose concentration is higher than 200ppm, the feed intake of the pigs will drop immediately or even directly refuse to feed. The recommended dosage of Tilmicosin on pigs is as high as 200-400ppm. That is...

AI Technical Summary

Problems solved by technology

However, glyceryl monostearate, animal wax, vegetable wax, fat powder, etc. all have such defects: their thermal melting points are low, and they begin to melt when they reach 60°C. Thermal melting precipitation may occur due to temperature rise during processing; in addition, this type of carrier is a bioerodible material, and the dissolution in the body is slow, which may cause the problem of slow drug release

However, studies have shown that tilmicosin is stable at pH 2-7.4, that is, in gastric acid environment, and the idea of ​​improving bioavailability by making enteric-coated preparations lacks a theoretical basis

At the same time, because the preparation does not dissolve in the stomach, it starts to release when it reaches the small intestine. It takes a time for the drug to reach the small intestine from the stomach, which will inevitably lead to a delay in the onset of the drug. At present, there is no research data to prove that tilmicosin is digested in pigs. Wh