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

A technology of cephradine and microspheres, which is applied in the field of cephradine microspheres and its preparation, and can solve the problems of reduced therapeutic effect of drugs, increased drug residues, toxic and side effects, etc.

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 produced certain drug resistance to cephradine, resulting in the reduction of drug therapeutic effect.
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

[0016] Embodiment 1: get gelatin 0.8kg, put in the purified aqueous solution 8L [gelatin solution of 10% concentration], swell completely in 60 DEG C of warm water baths, cephradine 0.4kg is dissolved in the solution containing gelatin and mix well, then slowly dropwise add Have in the 200L stirring vessel of 1.05L sorbitan oleate and 60L liquid paraffin (1.75% concentration), stir evenly in the same temperature water bath, stirring speed is 1000r / min, continues stirring certain hour to milky white, emulsification time is 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. Then 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 vacuum-dry at room temperature for 24 hours to obtain t...

Embodiment 2

[0017] Example 2: The prepared cephradine lung-targeting preparation is used to treat bacterial infections in livestock and poultry caused by Staphylococcus, Escherichia coli, influenza bacillus and other bacteria. The administration method is mixing or drinking water administration, poultry 0.02-0.04g / kg body weight, livestock 0.01-0.03g / kg body weight, 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 cefradine microsphere for animal and its preparation process. The cefradine microsphere is prepared with cefradine as medicine component and gelatin as carrier in the weight ratio of 1 to 2, and through dissolving cefradine in gelatin solution and adding Span-80 and liquid paraffin through stirring to obtain emulsion; cooling in icy bath to below 5 deg.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 cefradine 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—cephradine microspheres and a preparation method thereof—using cephradine as a raw material. Background technique [0002] Cephalosporin antibiotics are the most widely used class of antibacterial drugs in modern times. The chemical name of cephradine is (6R, 7R)-7-[(R)-2-amino-2-(1,4-cyclohexyl alkenyl)acetylamino]-3-methyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid. Calculated as anhydrous matter, containing C 16 h 19 N 3 o 4 S must not be less than 90.0%. [0003] The properties of the drug are white or off-white crystalline powder; slight odor. Slightly soluble in water, almost insoluble in ethanol, chloroform or ether. [0004] Its antibacterial effect is stronger than that of cephalexin, and it has bactericidal effect on Staphylococcus, Escherichia coli, influenza bacillus and ot...

Claims

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Application Information

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IPC IPC(8): A61K31/545A61K9/16A61K47/42A61P31/04
Inventor 李旭东鲍恩东苏建东
Owner TIANJIN RINGPU BIO TECH
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