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Lung targeting clarithromycin microsphere for animal and birds and its preparing method

A technology for clarithromycin and veterinary drug clarithromycin, which is applied in the field of veterinary drugs 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

[0004] However, due to long-term and extensive use, many pathogenic bacteria have developed certain drug resistance to clarithromycin, 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

[0014] 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 clarithromycin 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 diethyl ether to wash off glutaraldehyde, wash off the liquid paraffin on the surface of the microspheres with petroleum ether, and vacuum dry at r...

Embodiment 2

[0015] Example 2: The prepared clarithromycin lung-targeted formulation was used to treat livestock and poultry infections caused by staphylococcus, streptococcus pneumoniae, streptococcus pyogenes, catarrhal bacteria, mycoplasma pneumoniae, and the like. The mode of administration is mixing or drinking water, 0.01 g / kg body weight for poultry and 0.006 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 clarithromycin microsphere for animal and its preparation process. The clarithromycin microsphere is prepared with clarithromycin as medicine component and gelatin as carrier in the weight ratio of 1 to 2, and through dissolving clarithromycin 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 clarithromycin 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 relates to the preparation of lung targeting preparations - clarithromycin microspheres by using clarithromycin as a raw material and a preparation method thereof. Background technique [0002] Macrolide antibiotics are a class of antibacterial drugs that are widely used clinically in modern times. Clarithromycin is 6-O-methyl erythromycin, calculated as anhydrous, containing C 38 H 69 NO 13 Not less than 94.0%; it is white or off-white crystalline powder; odorless, bitter in taste; the drug is easily soluble in chloroform, soluble in acetone or ethyl acetate, slightly soluble in methanol or ethanol, and slightly soluble in water Insoluble; and the antibacterial spectrum of the drug is similar to that of erythromycin, and has antibacterial effects on Staphylococcus, Streptococcus pneumoniae, Streptococcus pyogenes, Catarella, Mycoplasma pneumoniae, etc. Oral absorption is rapid...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K47/42A61K31/7056A61P31/04
Inventor 李旭东鲍恩东苏建东
Owner TIANJIN RINGPU BIO TECH