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

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...