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Lung targeting ceftiofur microsphere and preparation method

A ceftiofur and lung-targeting technology, which is applied in medical formulas, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve the problem of increased drug side effects, insignificant curative effect, drug waste, etc. problem, to achieve the effects of significant efficacy, good appearance and delayed release

Active Publication Date: 2010-06-30
QINGDAO VLAND BIOTECH INC +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] 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

Examples

Experimental program
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Effect test

Embodiment 1

[0030] A preparation method for lung targeting ceftiofur microspheres, comprising the steps of:

[0031] Preparation of microspheres

[0032] Accurately weigh 0.9g PLGA (the molecular weight is 5000Da, the ratio of lactic acid to glycolic acid is 85:15) 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 3min, After the ceftiofur is fully dispersed, emulsify into a PVA aqueous solution with a concentration of 5% (mass / volume) at high speed, and emulsify at a speed of 8000rpm for 3 minutes; add the above emulsion into a PVA aqueous solution with a concentration of 0.3% (mass / volume) , stirring at low speed at room temperature for 7 hours to completely volatilize the dichloromethane; centrifuge at 5500 rpm for 5 minutes to collect the microspheres; wash with distilled water three times until the PVA is completely washed, and freeze-dry to obtain the microspheres.

[0033] ...

Embodiment 2

[0045] Accurately weigh 0.9g PLGA (the molecular weight is 75000Da, the ratio of lactic acid to glycolic acid is 50:50) 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 5min, so that After ceftiofur is fully dispersed, emulsify it into a PVA aqueous solution with a concentration of 1% (mass / volume) at a high speed, and emulsify at a speed of 10,000rpm for 0.5min; add the above emulsion into a PVA aqueous solution with a concentration of 0.1% (mass / volume) , stirring at low speed at room temperature for 4 hours to completely volatilize the dichloromethane; centrifuge at 2500 rpm for 20 minutes 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 various indicators of the PLGA microspheres prepared by the above method are measured. ...

Embodiment 3

[0048] Accurately weigh 0.6g of PLGA (molecular weight is 20000Da, the ratio of lactic acid to glycolic acid is 75:25) and dissolve it in 3ml of ethyl acetate. After it is completely dissolved, add 0.2g of ceftiofur; use a probe-type ultrasonic pulverizer to sonicate for 3min, so that After ceftiofur is fully dispersed, it is emulsified into a PVA aqueous solution with a concentration of 3% (mass / volume) at a high speed, and emulsified at 9000rpm for 1min; the above emulsion is added to a PVA aqueous solution with a concentration of 0.25% (mass / volume), Stir at room temperature at low speed for 5 hours to completely volatilize the dichloromethane; collect the microspheres by centrifuging at 4000 rpm for 10 minutes; wash with distilled water three times until the PVA is completely washed, and freeze-dry to obtain the microspheres.

[0049] According to the method of Example 1, the various indicators of the PLGA microspheres prepared by the above-mentioned method are measured. It...

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Abstract

The invention provides lung targeting ceftiofur microsphere and a preparation method which can solve the problems the prior art that few positions reach a target, so that a lot of medicine is wasted, the therapical effect is insignificant, the toxin and side effect of the medicine are improved and the chance of leading to medicine resistance is great. The technical scheme is as follows: the microsphere takes ceftiofur as the raw material, PLGA as the carrier material, and the weight ratio of ceftiofur to PLGA is 1:1 to 1:50. The invention also provides a method for preparing the microsphere through an emulsion process. The microsphere can treat the lung infection of animals with high efficiency; and the ceftiofur is prepared into lung targeting microsphere, thereby improving the concentration of the medicine in the animal lung tissue, so that the therapical effect is more significant. The microsphere prepared through the method has the advantages of very good morphology and very strong controllable particle size, can achieve high lung targeting property by optimizing the particle size, so that the particle size of more than 90 percent of microsphere is 7 to 30mu m, the encapsulation rate of the microsphere is more than 65 percent, the drug loading can reach 8 to 24 percent, and the microsphere has better releasing effect.

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, a series of serious problems have emerged in the use of antibacterial drugs: (1) The emergence of drug resistance, resulting in a decrease in the therapeutic effect of drugs. For example, in the treatment of lung diseases, the drug must reach an effective concentration in the lungs. To achieve the therapeutic effect, it is necessary to increase the dosage of the drug, so it is easy to cause the increas...

Claims

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Application Information

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