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Lung targeting microsphere of veterinary ceftiofur hydrochloride and preparation method

A ceftiofur hydrochloride and lung-targeting technology, which is applied in the field of ceftiofur hydrochloride lung-targeting microspheres and its preparation, can solve the problems of poor drug treatment effect, toxic side effects, and increased concentration, and achieve Reduce concentration, reduce toxic and side effects, delay drug release effect

Active Publication Date: 2010-09-15
江西派尼生物药业有限公司
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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, which can solve the problem in the prior art that the concentration of the drug in other tissues is increased due to the low tissue selectivity of the drug, thereby causing adverse effects on the body. The problem of harmful side effects and poor therapeutic effect of drugs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] A preparation method of veterinary ceftiofur hydrochloride lung targeting microspheres is as follows:

[0029] 1) Preparation of microspheres

[0030] Accurately weigh 1g of gelatin to swell completely in 5ml of 50°C water, weigh 0.33g of ceftiofur hydrochloride and add it to the gelatin solution to dissolve it completely; at the same time, measure 150ml of liquid paraffin into the Erlenmeyer flask, add 2ml of emulsifier Span80 , placed in a 50°C water bath to disperse completely; add the gelatin solution dissolved with ceftiofur hydrochloride dropwise into the Erlenmeyer flask, stir and emulsify at 50°C for 20min at 1900rpm, and then transfer to an ice bath for emulsification for 45min; add 4.5ml7 % (volume ratio) glutaraldehyde solution was solidified for 0.5h; add corresponding concentration of glycine solution to react for 40min to shield the unreacted aldehyde groups in glutaraldehyde; add 100ml of isopropanol to dehydrate for 20min; add 30ml of acetone to remove t...

Embodiment 2

[0043]Accurately weigh 0.25g of gelatin to swell completely in 5ml of 40°C water, weigh 0.0083g of ceftiofur hydrochloride and add it to the gelatin solution until it is completely dissolved; at the same time, measure 50ml of liquid paraffin into the Erlenmeyer flask, add 1ml of emulsifier Span80 , placed in a 40°C water bath to disperse completely; add the gelatin solution containing the drug dropwise into the Erlenmeyer flask, stir and emulsify at 40°C for 10 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 2 hours; glycine solution of corresponding concentration was added to react for 20 minutes to shield unreacted aldehyde groups in glutaraldehyde; 25ml of isopropanol was added for dehydration for 50min; after suction filtration, 30ml of acetone was added to remove liquid paraffin; After the acetone was re-dispersed, the microspheres were selected by sieving with...

Embodiment 3

[0046] Accurately weigh 0.5g of gelatin to swell completely in 2.5ml of 50°C water, weigh 0.1g of ceftiofur hydrochloride and add it to the gelatin solution until it is completely dissolved; at the same time, measure 50ml of liquid paraffin into the Erlenmeyer flask, add 1ml of emulsifier Span80, placed in a 50°C water bath to disperse completely; add the gelatin solution containing the drug dropwise into the Erlenmeyer flask, 1700rpm, 50°C stirring and emulsifying for 15min, and then transfer to an ice bath for emulsifying for 30min; add 4.5ml of 2% (volume ratio ) glutaraldehyde solution was solidified for 1 hour; added glycine solution of corresponding concentration to react for 30 minutes to shield unreacted aldehyde groups in glutaraldehyde; added 20ml of isopropanol for dehydration for 30 minutes; After re-dispersing with acetone, the microspheres were selected by separate sieving, filtered with suction and dried at room temperature.

[0047] For the microspheres prepare...

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Abstract

The invention provides a lung targeting microsphere of veterinary ceftiofur hydrochloride and a preparation method and can solve the problems of harmful toxic and side effects on a tissue due to the increased concentrations of other tissues caused by the low tissue selectivity of medicaments and poor therapeutic effect of the medicaments in the prior art. The lung targeting microsphere adopts the technical scheme of taking ceftiofur hydrochloride as a raw material and glutin as a carrier, wherein the weight ratio of the ceftiofur hydrochloride to the glutin is 1:3 to 30. The invention further provides the preparation method of the lung targeting microsphere. The lung targeting microsphere has the advantages of higher medicament loading rate and encapsulation rate of over 60 percent; after separation, the grain diameter of over 92 percent of the microsphere is between 7 and 30 mu m, so that the lung targeting microsphere meets the grain diameter requirement, improves the tissue selectivity, targets to the lung, reduces the concentrations of the medicaments in other tissues and toxic and side effects, and efficiently treats the pulmonary infection of animals.

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 ceftiofur hydrochloride and a preparation method thereof. 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. Due to the above-mentioned...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/546A61K47/42A61P31/04
Inventor 郝智慧肖希龙王艳玲
Owner 江西派尼生物药业有限公司
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