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
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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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