Ceftiofur lung targeting microsphere used for beasts and birds and preparation method thereof

A ceftiofur and lung targeting technology, applied in the field of lung targeting microspheres and preparation of ceftiofur, can solve the problems of increasing drug toxicity and side effects, insignificant curative effect, large drug resistance, etc., and improve tissue selection. The effect of reducing the concentration, reducing the toxicity and side effects

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

[0006] The invention provides a lung-targeted microsphere of ceftiofur for livestock and poultry and a preparation method thereof, which can solve the problems 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 the occurrence of The problem of high potential for drug resistance

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] A preparation method of ceftiofur-targeted microspheres for livestock and poultry is as follows:

[0028] 1) Preparation of microspheres

[0029] Accurately weigh 1g of gelatin to swell completely in 5ml of 50°C water, weigh 0.5g of ceftiofur and add it to the gelatin solution, and ultrasonically disperse it completely; at the same time, measure 150ml of liquid paraffin into a Erlenmeyer flask, add 3ml of emulsifier Span80, set Disperse completely in a water bath at 50°C; add the gelatin solution dissolved in ceftiofur into the Erlenmeyer flask dropwise, stir and emulsify at 50°C for 20 minutes at 1900 rpm, and then transfer to an ice bath for emulsification for 45 minutes; add 4.5ml of 7% (volume ratio) The glutaraldehyde solution was solidified for 0.5h; add the corresponding concentration of glycine solution to react for 40min, shield the unreacted aldehyde group in glutaraldehyde; add 25ml isopropanol to dehydrate for 50min; add acetone 30ml after suction filtration...

Embodiment 2

[0042] Accurately weigh 0.5g of gelatin to swell completely in 10ml of 40°C water, weigh 0.025g of ceftiofur and add it to the gelatin solution, and ultrasonically disperse it completely; at the same time, measure 100ml of liquid paraffin into the Erlenmeyer flask, add 2ml of emulsifier Span80, Disperse completely in a water bath at 40°C; add the gelatin solution containing the drug dropwise into the Erlenmeyer flask, stir and emulsify at 40°C for 15 minutes at 700 rpm, and then transfer to an ice bath for emulsification for 25 minutes; add 4.5ml of 1% (volume ratio) Glutaraldehyde solution was solidified for 1 hour; glycine solution of corresponding concentration was added to react for 20 minutes to shield unreacted aldehyde groups in glutaraldehyde; 200ml of isopropanol was added for dehydration for 20 minutes; after suction filtration, 60ml of acetone was added to remove liquid paraffin; After re-dispersion, the microspheres were selected by sample sieving, filtered by sucti...

Embodiment 3

[0045]Accurately weigh 1g of gelatin to swell completely in 5ml of 50°C water, weigh 0.25g of ceftiofur and add it to the gelatin solution, and ultrasonically disperse it completely; at the same time, measure 100ml of liquid paraffin in a Erlenmeyer flask, add 2ml of emulsifier Span80, set Disperse completely in a water bath at 50°C; add the gelatin solution containing the drug dropwise into the Erlenmeyer flask, stir and emulsify at 50°C for 15 minutes at 1700 rpm, and then transfer to an ice bath for emulsification for 30 minutes; add 4.5ml of 3% (volume ratio) Glutaraldehyde solution was solidified for 1 hour; glycine solution of corresponding concentration was added to react for 30 minutes to shield unreacted aldehyde groups in glutaraldehyde; 25ml of isopropanol was added for dehydration for 30 minutes; after suction filtration, 20ml of acetone was added to remove liquid paraffin; After re-dispersion, the microspheres were selected by sample sieving, filtered by suction an...

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Abstract

The invention provides a ceftiofur lung targeting microsphere used for beasts and birds and a preparation method thereof, which can solve the problems of waste of a large amount of medicine, indistinctive curative effect, medicine toxic and side effect enhancement and high possibility of generating medicine resistance caused by few reached targeting parts in the prior art. The invention has the technical scheme that ceftiofur is used as raw materials, gelatin is used as carriers, and the weight ratio of the ceftiofur to the gelatin is 1 / 0.5 to 20. The invention also provides a preparation method of the lung targeting microsphere. Both the medicine carrying rate and the encapsulation rate of the microsphere are high, the encapsulation rate can reach more than 60 percent, and more than 94 percent of sorted microspheres have the grain diameter between 7 and 30 mum, so the requirement of the lung targeting microsphere on the grain diameter is met, the tissue selectivity of the medicine is improved, the effect of lung targeting is reached, the concentration of the medicine in other tissues is lowered, the toxic and side effect is reduced, and thus, pulmonary infection of animals can be treated at high efficiency.

Description

technical field [0001] The invention belongs to the technical field of antibiotic preparations for livestock and poultry, and in particular relates to a lung-targeting microsphere of ceftiofur and a preparation method thereof. Background technique [0002] Ceftiofur (ceftiofur) is the first cephalosporin antibiotic for animals. Due to its outstanding advantages such as broad antibacterial spectrum, strong antibacterial activity, less drug residue, less toxic and side effects, and difficult to pass through the blood-brain barrier, it is widely used by veterinarians at home and abroad. Clinical application is becoming more and more extensive. [0003] At present, the most widely used preparations of ceftiofur are mainly powder and ceftiofur sodium injection. After administration, the drug is evenly distributed in the blood and tissues, and only a small amount can reach the target site, which not only causes a lot of waste of the drug, but also increases the cost of the drug. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/16A61K31/546A61K47/42A61P31/04
Inventor 郝智慧肖希龙王艳玲
Owner QINGDAO VLAND BIOTECH INC
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