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Lung-targeting sparfloxacin microsphere for animal and birds and its preparing method

The technology of sparfloxacin and microspheres is applied in the field of sparfloxacin microspheres and their preparation, and can solve the problems of increased drug residues, increased drugs, and decreased drug treatment effects.

Inactive Publication Date: 2007-06-27
TIANJIN RINGPU BIO TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, due to long-term and extensive use, many pathogenic bacteria have developed a certain resistance to this type of drug, which leads to a reduction in the therapeutic effect of the drug.
For example, in the treatment of lung diseases, to make the drug reach an effective concentration in the lung tissue, it is necessary to increase the dose of the drug, which will easily cause the increase of the drug residue in other tissues and produce some harmful side effects to the body

Method used

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  • Lung-targeting sparfloxacin microsphere for animal and birds and its preparing method

Examples

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Effect test

Embodiment 1

[0016] Example 1: Take 0.8kg of gelatin, put it into 8L of purified aqueous solution [10% gelatin solution], swell completely in a warm water bath at 60°C, dissolve 0.4kg of sparfloxacin in the gelatin-containing solution and mix evenly, then slowly drop Add 1.05L sorbitan oleate and 60L liquid paraffin (1.75% concentration) into a 200L stirring container, stir evenly in a water bath at the same temperature, and the stirring speed is 1000r / min, continue to stir for a certain period of time until milky white, emulsified The time is 15 minutes. Cool rapidly in an ice bath to below 5°C, add 6L of glutaraldehyde in a thin stream and continue stirring for 30 minutes to cross-link and solidify. Dehydrate and stir with isopropanol 60L for 10 min, and filter with suction. Wash with a little isopropanol and diethyl ether to remove the glutaraldehyde, wash off the liquid paraffin on the surface of the microspheres with petroleum ether, and dry in vacuum at room temperature for 24 hours...

Embodiment 2

[0017] Example 2: The prepared sparfloxacin lung-targeting preparation was used to treat livestock and poultry infections caused by Gram-positive and negative bacteria, mycobacteria, anaerobic bacteria, mycoplasma, and chlamydia. The way of administration is mixing or drinking water, 0.001-0.004g / kg body weight of livestock and poultry, twice a day, 3-5 days as a course of treatment.

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Abstract

The present invention belongs to the field of veterinary medicine technology, and is especially lung targeting sparfloxacin microsphere for animal and its preparation process. The sparfloxacin microsphere is prepared with sparfloxacin as medicine component and gelatin as carrier in the weight ratio of 1 to 2, and through dissolving sparfloxacin in gelatin solution and adding Span-80 and liquid paraffin through stirring to obtain emulsion; cooling in icy bath to below 5deg.c and adding glutaraldehyde through stirring for cross-linking and curing; dewatering with isopropyl alcohol and suction filtering; washing with isopropyl alcohol and ethyl ether to eliminate glutaraldehyd, washing with petroleum ether to eliminate liquid paraffin in the surface of microsphere and vacuum drying at room temperature to obtain sparfloxacin microsphere. The medicine has raised tissue selectivity, delayed release, raised curative effect and lowered toxic side effect.

Description

technical field [0001] The invention belongs to the technical field of veterinary medicine, and the invention relates to the preparation of a lung-targeting preparation—sparfloxacin microspheres and a preparation method thereof using sparfloxacin as a raw material. Background technique [0002] Quinolones antibiotics are a class of antibacterial drugs that are widely used in modern clinical practice. The chemical name of sparfloxacin is 5-amino-1-cyclopropyl-7-(cis-3,5-dimethyl-1 -piperazinyl)-6,8-difluoro-1,4-dihydro-4-oxo-quinoline-3-carboxylic acid. Calculated as dry product, including C 19 h 22 f 2 N 4 o 3 It should be 98.5%-102.0%, and the molecular formula is as follows: [0003] [0004] This product is slightly soluble in chloroform, slightly soluble in acetonitrile, methanol or ethyl acetate, very slightly soluble in ethanol, almost insoluble in water; soluble in 0.1mol / L sodium hydroxide solution, slightly soluble in glacial acetic acid . [0005] Sparfl...

Claims

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Application Information

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IPC IPC(8): A61K31/496A61K9/16A61K47/42A61P31/04A61P11/00
Inventor 李旭东鲍恩东苏建东
Owner TIANJIN RINGPU BIO TECH
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