Tilmicosin film-controlled enteric-coated sustained release preparation and preparation method thereof

Abstract

The invention belongs to the field of pharmaceutical preparations and particularly relates to a tilmicosin film-controlled enteric-coated sustained release preparation. The preparation comprises an inner core layer and a film coating layer. The inner core layer comprises raw tilmicosin powder and an inner core layer auxiliary material. The inner core layer auxiliary material comprises two or more of starch, dextrin, sucrose, microcrystalline cellulose, povidone, methylcellulose, hydroxypropyl methylcellulose, hydroxyethylcellulose, xanthan gum, chitin and sodium alginate. The preparation method has a low material loss and a high yield. The tilmicosin film-controlled enteric-coated sustained release preparation masks the bitter taste of tilmicosin, greatly improves the palatability of tilmicosin, cannot be dissolved in a stomach dissolution rate determination test, only collapses and releases in an alkaline environment in the intestine, significantly improves the drug efficacy and reduces the clinical dosage of drugs.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a tilmicosin preparation, in particular to a tilmicosin film-controlled enteric-coated slow-release preparation and a preparation method thereof. Background technique [0002] Tilmicosin is a semi-synthesized macrolide antibiotic for livestock and poultry with a hydrolyzate of tylosin as the precursor. It was first successfully developed by the British Elanco animal health products company in the 1980s. Tilmicosin has a strong antibacterial effect, excellent pharmacokinetic characteristics, and a broad antibacterial spectrum, and has inhibitory effects on all Gram-positive bacteria and some Gram-negative bacteria, mycoplasma, mycoplasma, spirochetes, etc. , especially in the treatment of livestock and poultry respiratory tract infection effect is more obvious. [0003] Tilmicosin tastes extremely bitter, has poor palatability, is irritating to the gastric mucosa, and aff...

AI Technical Summary

Problems solved by technology

Ordinary granules are simply mixed and granulated with tilmicosin raw materials and excipients, which cannot mask the bitter taste and affect animal feeding, or some coated granules are unstable in the stomach, easy to degrade and irritating to the gastric mucosa

There are also studies on film-controlled enteric-coated tilmicosin preparations, such as publication numbers CN103083281A (a kind of enteric-coated tilmicosin sustained-release microcapsule preparation and its preparation method) and CN106176680A (a kind of enteric-coated tilmicosin slow-release microcapsule preparation) release microcapsule and its preparation method) respectively disclose a membrane-controlled enteric-coated tilmicosin sustained-release microcapsule, although it can also cover up the bitter taste of tilmicosin to a certain extent, but because it is micro Capsule preparations, the waste produced is not conducive to recycling and reuse, and the yield is low ("Application Progress of Microencapsulation Technology in Pharmaceutical Preparations", Li Rong et al., "Frontiers of Medicine", October 24, 2012)

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