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Lung-targeting ceftiofur microsphere and preparation method thereof

A ceftiofur, lung targeting technology, applied in pharmaceutical formulations, medical preparations with non-active ingredients, and medical preparations containing active ingredients, etc. problem, achieve good biocompatibility, solve the effect of insignificant curative effect, and delay the release

Active Publication Date: 2010-06-30
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 ceftiofur microsphere and a preparation method thereof, which can solve the problems existing in the prior art that a large amount of medicine is wasted due to a small amount of reaching the target site, the curative effect is not significant, the side effects of the medicine are increased, and drug resistance is produced. likely problem

Method used

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  • Lung-targeting ceftiofur microsphere and preparation method thereof
  • Lung-targeting ceftiofur microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A preparation method for lung targeting ceftiofur microspheres, comprising the steps of:

[0028] Preparation of microspheres

[0029] Accurately weigh 0.9g PLA (molecular weight: 5000Da) and dissolve it in 2.25ml of dichloromethane. After it is completely dissolved, add 0.45g of ceftiofur; use a probe-type ultrasonic pulverizer to sonicate for 3 minutes to fully disperse the ceftiofur, then emulsify to In the PVA aqueous solution with a concentration of 1% (mass / volume), emulsify at a speed of 9000rpm for 3 minutes; add the above-mentioned emulsion to a PVA aqueous solution with a concentration of 0.3% (mass / volume), stir at room temperature for 7 hours at a low speed, so that the dichloromethane is completely Volatile and clean; centrifuge at 2500rpm for 20min to collect the microspheres; wash with distilled water three times until the PVA is completely washed, freeze-dry to obtain the microspheres.

[0030] Microsphere Morphology and Particle Size

[0031] The morp...

Embodiment 2

[0042] Accurately weigh 0.9g PLA (molecular weight: 75,000Da) and dissolve it in 18ml of dichloromethane. After it is completely dissolved, add 0.09g of ceftiofur; use a probe type ultrasonic pulverizer to sonicate for 5 minutes to fully disperse the ceftiofur, and emulsify at high speed to the concentration In a 5% (mass / volume) PVA aqueous solution, emulsify at a speed of 10000rpm for 0.5min; add the above-mentioned emulsion into a 0.1% (mass / volume) PVA aqueous solution, and stir at a low speed at room temperature for 4h, so that the dichloromethane is completely Volatile and clean; centrifuge at 5500rpm for 5min to collect the microspheres; wash with distilled water three times until the PVA is completely washed, and freeze-dry to obtain the microspheres.

[0043] According to the method of Example 1, the indicators of the PLA microspheres prepared by the above method were measured. It can be seen that the average particle size of the microspheres is 13.39 μm, and the parti...

Embodiment 3

[0045] Accurately weigh 0.9g PLA (molecular weight: 20000Da) and dissolve it in 4.5ml of dichloromethane. After it is completely dissolved, add 0.18g of ceftiofur; use a probe-type ultrasonic pulverizer to sonicate for 5 minutes to fully disperse the ceftiofur, then emulsify to In the PVA aqueous solution with a concentration of 2% (mass / volume), emulsify at a speed of 9000rpm for 1min; add the above-mentioned emulsion to a PVA aqueous solution with a concentration of 0.25% (mass / volume), stir at room temperature for 5 hours at a low speed, so that the dichloromethane is completely Volatile and clean; centrifuge at 4000rpm for 10min to collect the microspheres; wash with distilled water three times until the PVA is completely washed, and freeze-dry to obtain the microspheres.

[0046] According to the method of Example 1, the indicators of the PLA microspheres prepared by the above method were measured. It can be seen that the average particle size of the microspheres is 19.39 ...

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Abstract

The invention provides a lung-targeting ceftiofur microsphere and a preparation method thereof, aiming at solving the problems that less medicine can reach the target part in the prior art, so that a great deal of medicine is wasted, the treatment effect is not remarkable, the toxic and side effect of the medicine is increased, and the probability of generating drug resistance is high. The technical scheme comprises: the microsphere takes ceftiofur as raw material and PLA as carrier material, and the weight ratio between the ceftiofur and the PLA is 1:0.5-10. The invention also provides the method for preparing the microsphere by emulsification. The microsphere prepared by the method has round appearance and shape, even grain fineness distribution, the average grain diameter of about 20mu m and higher medicine-loading rate. The microsphere can be used for treating lung infection of livestock and poultry with high effect, and leads the ceftiofur to be made into the lung-targeting microsphere so as to improve the concentration of the medicine at the lung tissues of animals and lead the medicine effect to be more remarkable, thus achieving the aims of slow release, long-term effect and target.

Description

technical field [0001] The invention belongs to the technical field of veterinary antibiotic preparations, and in particular relates to a lung-targeting ceftiofur microsphere and a preparation method. Background technique [0002] Bacterial infectious diseases have always been one of the main diseases that endanger the aquaculture industry, causing serious economic losses to the aquaculture industry. At present, antibacterial drugs are mainly used clinically for the treatment of bacterial infectious diseases, and good results have also been achieved. However, in recent years, the serious problem of antibacterial drugs is the emergence of drug resistance, which leads to the reduction of the therapeutic effect of drugs. For example, in the treatment of lung diseases, it is necessary to increase the concentration of drugs in the lungs to achieve the therapeutic effect. Therefore, it is easy to cause the increase of drug residue in other tissues and produce some harmful side ef...

Claims

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Application Information

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