Preparation method of malic acid and tilmicosin compound salt

Abstract

The invention discloses a preparation method of malic acid and tilmicosin compound salt. The preparation method comprises the following steps of (1) dissolving the malic acid into an organic solvent, stirring, and heating and dissolving under the anhydrous condition, so as to prepare an organic solution of the malic acid; (2) dissolving crude drug of tilmicosin which is equimolar with the malic acid into the organic solvent, and dissolving under the anhydrous condition, so as to prepare an organic solution of the tilmicosin; (3) mixing the organic solution of the malic acid and the organic solution of the tilmicosin, heating to react under the anhydrous condition, controlling the reaction temperature to 50 to 70 DEG C, cooling a reaction liquid after reaction is complete, filtering the undissolved matter, performing rotary evaporation on filtrate, and recycling the organic solvent, so as to obtain a solid product, namely the malic acid and tilmicosin compound salt. The preparation method has the advantages that the technology is simple, the production cost is low, the water dissolvability of the prepared malic acid and tilmicosin compound salt is good, the dissolvability is good, the preparation property is good, and the mouth feel is proper.

Description

technical field [0001] The invention belongs to the field of drug synthesis, and in particular relates to a preparation method of tilmicosin malate double salt. Background technique [0002] Tilmicosin is a special macrolide antibiotic for poultry and animals. It was successfully developed by Elanco Animal Health Products Company in the UK in the 1980s. Tilmicosin is generally semi-synthesized from tylosin and has the same It has a similar antibacterial spectrum to gram-positive bacteria and some gram-negative bacteria, mold-type bacteria, spirochetes, etc., especially against Actinobacillus pleuropneumoniae, Pasteurella and animal mold-type bacteria. Tylosin has stronger antibacterial activity, and there is no cross-resistance with other antibiotics commonly used in clinic. [0003] Tilmicosin has a macrocyclic lactone structure, and the hydroxyl group on the ring is linked with sugar or substituted sugar in the form of glycosidic bonds, which reduces the tension of the ma...

AI Technical Summary

Problems solved by technology

In order to solve this problem in the prior art, the use of expensive special solvents has greatly increased its use cost

Although there have been reports on the preparation of new technologies such as nanoemulsions, liposomes, and soluble powders in recent years, their clinical application has been largely limited due to their complex preparation process and poor preparation stability.

Its phosphate is commonly used in veterinary clinics, but because of the poor palatability of existing tilmicosin phosphate preparations, it affects animals foraging, thereby reducing the curative effect on diseases

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