Process for preparing tilmicosin enteric-coated pellet by centrifuge method

Abstract

The invention discloses a process for preparing a tilmicosin enteric-coated pellet by a centrifuge method. The tilmicosin enteric-coated pellet is prepared from the following raw materials in percentage by mass: 21-26% of tilmicosin, 10-20% of an adhesive, 23-30% of microcrystalline cellulose and 10-20% of a coating material, and is prepared through the following steps: performing centrifugal pelleting on the raw materials, and coating the pellet obtained through centrifugal pelleting. The tilmicosin enteric-coated pellet is high in encapsulation efficiency, can mask the bitter taste of tilmicosin well, is dissolved out in an intestinal environment, can be used as an enteric-coated sustained-release reagent, solves the adverse reaction caused after the tilmicosin enteric-coated pellet is absorbed in stomach, is simple in preparation process, and is suitable for industrial large-scale production, thereby having a very wide application prospect; besides, the raw materials are cheap and easy to obtain.

Description

technical field [0001] The invention relates to a process for preparing tilmicosin enteric-coated pellets by a centrifugation method, and belongs to the technical field of veterinary drug preparation. Background technique [0002] Tilmicosin is a derivative of tylosin after acid hydrolysis. It is a semi-synthetic macrolide antibiotic for animals. Its molecular formula is C 46 h 80 N 2 o 13 , with a molecular weight of 869.15, which has been approved for clinical use in Australia, Brazil, France, Malaysia, Italy, Spain, the United States and other countries. Tilmicosin has similar antibacterial activity to macrolides, and is effective against Gram-positive bacteria, some Gram-negative bacteria and mycoplasma. Especially for Actinobacillus pleuropneumoniae, Pasteurella, Staphylococcus aureus, Streptococcus pyogenes, Streptococcus pneumoniae, Corynebacterium pyogenes and mycoplasma of livestock and poultry, the activity is stronger than tylosin. Clinically, it is mainly us...

AI Technical Summary

Problems solved by technology

Because the injection is not taken orally, there is no problem of poor palatability, but due to the complicated clinical application and relatively high toxicity and side effects, tilmicosin cannot actually exert its maximum effect during a large-scale outbreak of the disease; other preparations such as oral liquid, Premixes, etc. are all conventional oral preparations, which fail to solve the problem of poor palatability of tilmicosin

[0004] Most of the existing tilmicosin pelleting methods adopt the extrusion spheronization process, which is not only cumbersome to operate and high in cost, but also the prepared granules are in the shape of rice with slightly pointed ends, and the true sphericity is far inferior to the granules produced by the centrifugal pelletizing process , resulting in poor coating efficiency, uneven coating thickness on the surface of the particles, easy to be degraded and absorbed in the stomach after oral administration, and irritating to the stomach (the coated particles are required not to dissolve in the stomach, but to dissolve in the intestinal tract)

In addition, the granules prepared by the extrusion spheronization process are difficult to completely dissolve and release in the small intestine due to high-intensity extrusion, resulting in most of the raw materials being excreted from the body, causing environmental pollution, which is also a very serious problem

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