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

A technology of cefoperazone and microspheres, which is applied in the field of cefoperazone microspheres and its preparation, and can solve problems such as increased drug residues, increased drugs, and reduced therapeutic effects of drugs

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 certain drug resistance to cefoperazone, 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

[0016] Example 1: Take 0.8kg of gelatin, put it into 8L of purified aqueous solution [10% concentration of gelatin solution], swell completely in a warm water bath at 60°C, dissolve 0.4kg of cefoperazone in the gelatin-containing solution and mix well, then slowly drip Add 1.05L sorbitan oleate and 60L liquid paraffin (1.75% concentration) into a 200L stirring vessel, stir evenly in a water bath at the same temperature, stirring at a speed of 1000r / min, continue stirring for a certain period of time until milky white, emulsification The time is 15 minutes. The ice bath was rapidly cooled to below 5°C, and 6L of glutaraldehyde was added in a thin stream to continue stirring and crosslinking for 30min. It was dehydrated with 60 L of isopropanol, stirred for 10 min, and filtered with suction. Then wash with a little isopropanol and ether to wash off glutaraldehyde, wash off the liquid paraffin on the surface of the microspheres with petroleum ether, and dry in vacuum at room tem...

Embodiment 2

[0017] Example 2: The prepared cefoperazone lung-targeted preparation is used to treat respiratory tract, urinary tract, abdominal cavity, pleura, skin and soft tissue, bone and joint infections caused by Gram-negative bacteria in livestock and poultry. The mode of administration is mixing or drinking water, 0.04-0.11 g / kg body weight for poultry and 0.02-0.04 g / kg body weight for livestock, 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 cefoperazone microsphere for animal and its preparation process. The cefoperazone microsphere is prepared with cefoperazone as medicine component and gelatin as carrier in the weight ratio of 1 to 2, and through dissolving cefoperazone 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 cefoperazone 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 drugs, and relates to a preparation method for lung targeting preparation-cefoperazone microspheres by using cefoperazone as a raw material. Background technique [0002] Cephalosporin antibiotics are the most widely used antibacterial drugs in modern clinical practice. The chemical name of cefoperazone is (6R, 7R)-3-[[(1-methyl-1H-tetrazol-5-yl) sulfur ]methyl]-7-[(R)-2-(4-ethyl-2,3-dioxo-1-piperazinecarbonylamino)-2-p-hydroxyphenyl-acetamido]-8- Oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid. Calculated as anhydrous, containing C 25 H 27 N 9 O 8 S 2 Not less than 95.0%. [0003] The drug is white or off-white crystalline powder, odorless, slightly bitter in taste, and hygroscopic; soluble in acetone or dimethyl sulfoxide, slightly soluble in methanol or ethanol, and soluble in water or ethyl acetate Very slightly soluble; molecular formula is C 25 H 27 N 9 O 8 S 2 , th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/546A61K9/16A61P31/04
Inventor 李旭东鲍恩东苏建东
Owner TIANJIN RINGPU BIO TECH
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