Veterinary danofloxacin mesylate slow-release microsphere preparation as well as preparation method and application of veterinary danofloxacin mesylate slow-release microsphere preparation

Abstract

The invention relates to a veterinary danofloxacin mesylate slow-release microsphere preparation as well as a preparation method and application of the veterinary danofloxacin mesylate sow-release microsphere preparation. The veterinary danofloxacin mesylate slow-release microsphere preparation comprises effective components in percentage by weight: 11.45-21.01 percent of danofloxacin mesylate and 78.99-88.55 percent of sodium alginate polysaccharide cross-linking polymer as a carrier. The veterinary danofloxacin mesylate slow-release microsphere preparation is prepared by adopting an emulsion chemical cross-linking method. The preparation method comprises the following steps of: firstly, mixing the danofloxacin mesylate, sodium alginate and an antioxidant to form an aqueous phase solution; dropping a cross-linking agent under the condition of emulsification and curing to form microsphere; and secondly, carrying out washing, centrifuging, filtering and drying to obtain the danofloxacin mesylate slow-release microsphere preparation of which the average particle size is 8-9mum. The preparation process of the preparation is simple and feasible; raw materials used for the preparation have better biocompatibility, biodegradability and stability; the prepared danofloxacin mesylate slow-release microsphere preparation has the characteristics of safety, no toxicity, high drug-loading rate (11.45-21.01 percent), high encapsulation rate (59.54-88.20 percent), long-acting effect, slow release and the like; after the danofloxacin mesylate slow-release microsphere preparation is injected in swine muscle, the effective concentration can be maintained for several days; and the veterinary danofloxacin mesylate slow-release microsphere preparation is suitable for treating respiratory tract and digestive tract infection of livestock caused by sensitive bacteria.

Description

technical field [0001] The invention relates to the technical field of preparation of new dosage forms of veterinary drugs, in particular to a veterinary dafloxacin mesylate sustained-release microsphere preparation and a preparation method and application thereof. Background technique [0002] Danofloxacin mesylate is a special fluoroquinolone drug for animals. It was successfully developed and launched by Pfizer of the United States in 1988 and has been widely used in the world. Dafloxacin mesylate has a wide antibacterial spectrum, strong bactericidal activity, low toxicity, good water solubility, wide distribution in the body, no cross-resistance with other antibacterial drugs, can be administered in multiple ways, absorbs rapidly, and has high bioavailability high. The drug shows strong antibacterial activity against Gram-positive bacteria, Gram-negative bacteria, intracellular pathogens, mycoplasma and some drug-resistant strains, and is often used in the treatment of...

AI Technical Summary

Problems solved by technology

The average particle size of dafloxacin mesylate microspheres prepared by this patent application is 10~11 μm, which can meet the requirements of intramuscular injection, but the drug loading (2.0~6.3wt%) and encapsulation efficiency (8.1%~ 16.5%) is low, and used a large amount of organic reagents such as isopropanol, ether, sherwood oil, liquid paraffin, formaldehyde, glutaraldehyde etc. in the preparation process, and these reagents all have certain toxic and side effects to people and animals, ether , Petroleum ether and other reagents are flammable, explosive, and volatile. There are potential safety hazards when used and pollute the environment.

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