Pulmonary targeting microsphere of veterinary ceftiofur hydrochloride and preparation method thereof

A technology of ceftiofur hydrochloride and lung targeting, which is applied to medical preparations containing no active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas, etc. Large drug resistance and other problems, to achieve the effect of significant drug effect, uniform particle size, and delayed release

Active Publication Date: 2010-07-14
QINGDAO VLAND BIOTECH INC +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The invention provides a lung-targeting microsphere of veterinary ceftiofur hydrochloride and a preparation method thereof, which can solve the problems in the prior art that a large amount of me

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0026] Weigh 1.8g PLGA (molecular weight is 5000Da, the ratio of lactic acid to glycolic acid is 85:15), dissolve in 12.86ml of the mixed solution of dichloromethane and methanol, the volume ratio of dichloromethane to methanol is 7:3, weigh Add 0.9g of ceftiofur hydrochloride into the solution, and after it is completely dissolved, adjust the parameters of the spray dryer so that the inlet temperature is 50°C, the air flow rate is 900%, and the injection rate is 40% (that is, 11.5ml / min) , the compressed air pressure is 0.4kPa, and the microspheres are prepared by spray drying with a spray dryer.

[0027] Microsphere Morphology and Particle Size

[0028] For the microspheres prepared by the above method, the average particle diameter of the microspheres measured by the dynamic light scattering method is 10.12 μm, and more than 89% of the particle diameters of the microspheres are between 7 and 30 μm, and the electron microscope shows that it is a regular spherical structure; ...

Embodiment 2

[0039] Weigh 1.8g of PLGA (molecular weight is 75000Da, the ratio of lactic acid to glycolic acid is 50:50), dissolve in 360ml of mixed solution of dichloromethane and methanol, the volume ratio of dichloromethane to methanol is 9:1, weigh 0.18 g ceftiofur hydrochloride was added to the solution, and after it was completely dissolved, the parameters of the spray dryer were adjusted so that the inlet temperature was 35°C, the air flow rate was 600%, the injection rate was 50% (ie 20ml / min), and the air The compression pressure is 0.4kPa, and the microspheres are prepared by spray drying with a spray dryer.

[0040] The average particle size of the PLGA microspheres prepared by the above method is 17.48 μm, and more than 91% of the particle sizes of the microspheres are between 7 and 30 μm. The electron microscope shows that it is a regular spherical structure, and the drug loading reaches 8.94%. The encapsulation efficiency It can reach 89.52%, and the drug loading effect is ve...

Embodiment 3

[0043] Weigh 1.8g PLGA (molecular weight is 20000Da, the ratio of lactic acid to glycolic acid is 75:25), dissolve in 30ml of dichloromethane and methanol mixed solution, the volume ratio of dichloromethane and methanol is 8:2, weigh 0.45 g ceftiofur hydrochloride was added to the solution, after it was completely dissolved, adjust the parameters of the spray dryer so that the inlet temperature was 40°C, the air flow rate was 700%, and the injection rate was 45% (i.e. 15.5ml / min), The compressed air pressure is 0.4kPa, and the microspheres are prepared by spray drying with a spray dryer.

[0044] The average particle size of the PLGA microspheres prepared by the above method is 13.34 μm, and more than 90% of the particle sizes of the microspheres are between 7 and 30 μm. The electron microscope shows that it is a regular spherical structure, and the drug loading reaches 17.59%. The encapsulation efficiency It can reach 87.95%, and the drug loading effect is better. Assay meth...

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Abstract

The invention provides a pulmonary targeting microsphere of veterinary ceftiofur hydrochloride and a preparation method thereof, which solves the problems of the prior art that the quantity of microspheres reaching the target site is small, thereby causing a large amount of drug waste, the therapeutic effect is no significant, the side effects of drugs are increased, and the possibility for generating drug resistance is high. In the technical scheme of the pulmonary targeting microsphere of veterinary ceftiofur hydrochloride, ceftiofur hydrochloride is used as a main component, poly-lactic-co-glycolic acid is used as a carrier material, and the mass ratio of the ceftiofur hydrochloride and the poly-lactic-co-glycolic acid is 1:1-1:50. The preparation method adopts the spray drying method. The particle sizes of the microspheres prepared in the method are relatively uniform, the large-scale preparation can be realized, the drug loading capacity and the encapsulation efficiency are both high, more than 89 percent of the particle sizes of the microspheres are all between 7mum and 30mum, thereby meeting the requirements of the pulmonary targeting microspheres for the particle sizes, and the microspheres can be concentrated in the lung, thereby enhancing the therapeutic effect.

Description

technical field [0001] The invention belongs to the technical field of veterinary antibiotic preparations, and in particular relates to a lung-targeting microsphere of veterinary ceftiofur hydrochloride and a preparation method. Background technique [0002] Ceftiofur, also known as Ceftiofur, is a cephalosporin antibiotic with broad antibacterial spectrum and strong antibacterial activity. It is the first ceftiofur antibiotic for animals created by Pharmacia Upjohn in the United States. Since it was approved by the FDA in 1988 for the treatment of respiratory infections in cattle, due to its excellent antibacterial activity and dynamic process in vivo, it is now widely used in veterinary clinics at home and abroad. [0003] Ceftiofur is an acid-base amphoteric compound, which can react with sodium hydroxide and hydrochloric acid to form acid-soluble salts and alkaline-soluble salts. The dry powder of its sodium salt and hydrochloride is very stable. Because ceftiofur has m...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/546A61K47/34A61P31/04A61P11/00
Inventor 郝智慧肖希龙王艳玲
Owner QINGDAO VLAND BIOTECH INC
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