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

A technology of fleroxacin and microspheres, applied in the field of veterinary medicine, which can solve the problems of increased drug residues, toxic and side effects, and reduced drug therapeutic effect

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

[0005] However, due to long-term and extensive use, many pathogenic bacteria have developed a certain resistance to fleroxacin, resulting in 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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] 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 fleroxacin in the gelatin-containing solution and mix evenly, then slowly add it dropwise In a 200L stirring container containing 1.05L sorbitan oleate and 60L liquid paraffin (1.75% concentration), stir evenly in a water bath at the same temperature, at a stirring speed of 1000r / min, continue stirring for a certain period of time until milky white, emulsification time 15min. 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 h...

Embodiment 2

[0016] Example 2: The prepared fleroxacin lung-targeting preparation was used to treat respiratory tract, urinary tract, abdominal cavity, bone and joint infections caused by Gram-negative bacteria and certain Gram-positive bacteria in livestock and poultry. The way of administration is mixing or drinking water, 0.005g / kg body weight of livestock and poultry, twice a day, 3-5 days as a course of treatment.

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PUM

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Abstract

The present invention belongs to the field of veterinary medicine technology, and is especially lung targeting fleroxacin microsphere for animal and its preparation process. The fleroxacin microsphere is prepared with fleroxacin as medicine component and gelatin as carrier in the weight ratio of 1 to 2, and through dissolving fleroxacin 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 fleroxacin 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 lung-targeting preparation—fleroxacin microspheres and a preparation method thereof using fleroxacin 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 fleroxacin is 6,8-difluoro-1-(2-fluoroethyl)-1,4-dihydro-7-(4 -methyl-1-piperazinyl)-4-oxo-3-quinolinecarboxylic acid. Calculated as dry product, including C 17 h 18 f 3 N 3 o 3 Should be 98.5%-102.0%. The properties of the drug are white to slightly yellow crystalline powder; odorless; slightly bitter taste; slightly soluble in chloroform, very slightly soluble in water or methanol, almost insoluble in ethyl acetate; easily soluble in glacial acetic acid Soluble, slightly soluble in sodium hydroxide test solution. [0003] This drug is a third-generation ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K9/16A61K47/42A61P31/04
Inventor 李旭东鲍恩东苏建东
Owner TIANJIN RINGPU BIO TECH