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Enrofloxacin gelatine microball and its preparation method

A technology of enrofloxacin and gelatin, which is applied in the directions of pharmaceutical formulations, medical preparations containing active ingredients, and bulk delivery, can solve the problems of reduced drug treatment effect, increased drug residues, toxic and side effects, etc., and achieves a round shape. , good dispersion, less adhesion effect

Inactive Publication Date: 2008-01-09
北京中农大动物保健品技术研究院
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  • Summary
  • Abstract
  • Description
  • Claims
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Problems solved by technology

[0003] With the generation of drug resistance, the therapeutic effect of drugs will be reduced, and quinolones are widely distributed in the body. Therefore, when treating respiratory infections such as pneumonia and bronchitis in animals, it is necessary to increase the effective concentration of drugs in lung tissue. The dose of the drug, which is likely to cause increased drug residues in other tissues and produce some toxic side effects

Method used

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  • Enrofloxacin gelatine microball and its preparation method

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preparation example Construction

[0027] The preparation method of enrofloxacin gelatin microspheres proposed by the present invention, the specific steps are as follows: take gelatin and add double distilled water or phosphate buffer solution, completely swell in a warm water bath, then add enrofloxacin to mix and dissolve, and then drop Add it into a beaker containing Span 80 (or Span 60) and liquid paraffin, stir evenly in a water bath at the same temperature, continue to stir for a certain period of time until it becomes milky white, cool down rapidly in the ice bath to below 5°C and continue to emulsify, then add pentadiene The aldehyde continued to stir to cross-link and solidify, dehydrated and stirred with isopropanol, and filtered with suction. Then wash with a little isopropanol, wash off the glutaraldehyde, wash off the liquid paraffin on the surface of the microspheres with petroleum ether, and dry in vacuum to obtain a slightly yellowish microsphere powder with good roundness;

[0028] In this met...

Embodiment 1

[0034] Get 0.4g of gelatin, add 4mL of double-distilled aqueous solution (to make a gelatin solution with a weight volume concentration of 10%), swell completely in a warm water bath at 60°C, then add 0.2g of enrofloxacin, mix and dissolve (enrofloxacin in water The weight-volume concentration in the oil phase is 5%), and then added dropwise to the 100mL beaker filled with 0.6mL Span 80 and 30mL liquid paraffin (Span 80 is 2.0% in the oil phase by volume concentration). The medium electromagnetic stirring is even, the stirring speed is 1000r min -1 , stirred for 15 minutes until milky white, cooled rapidly in an ice bath to below 5°C, continued to stir and emulsify for 15 minutes, added 3 mL of glutaraldehyde in a thin stream, continued to stir for cross-linking and solidification for 30 minutes, dehydrated with 30 mL of isopropanol and stirred for 10 minutes, and suction filtered. Then wash with a little isopropanol to remove the glutaraldehyde, wash off the liquid paraffin o...

Embodiment 2

[0037] Take 0.4g of gelatin, add 0.9mol·L -1 pH 5.0 phosphate buffer solution 4mL (prepared 10wt% gelatin solution), swell completely in a warm water bath at 60°C, then add 0.4g enrofloxacin, mix and dissolve, then dropwise add 0.6mL Span 80 and 30mL In a 100mL beaker of liquid paraffin (Span 80 volume concentration 2.0%), electromagnetically stir evenly in a water bath at the same temperature, and the stirring speed is 700r min -1 , stirred for 15 minutes until milky white, cooled rapidly in an ice bath to below 5°C and continued to emulsify for 15 minutes, added 3 mL of glutaraldehyde in a thin stream and continued to stir for cross-linking and solidification for 30 minutes, dehydrated with 30 mL of isopropanol and stirred for 10 minutes, and filtered with suction. Then wash with a little isopropanol to wash away the glutaraldehyde, wash off the liquid paraffin on the surface of the microspheres with petroleum ether, and dry in vacuum overnight to obtain a yellowish microsp...

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Abstract

The present invention relates to an enrofloxacin gelatin microsphere and its preparation method. It is characterized by that it uses type A gelatin as carrier, uses enrofloxacin as medicine to be carried and adopts an emulsification-condensation process to prepare the invented gelatin microsphere which can take the lung as target organ after intravenous injection. The average grain size of said microspheres is 12 micrometers.

Description

technical field [0001] The invention belongs to the field of animal medicines, and in particular relates to an improved preparation of enrofloxacin, a fluoroquinolone antibacterial drug specially used for veterinary medicine, and a preparation method thereof. Background technique [0002] Enrofloxacin (ENR) is a third-generation fluoroquinolone antibacterial drug specially used for veterinary medicine. Bacteria in stationary phase and growth phase are effective, and its bactericidal activity depends on concentration. Clinically, it is mainly used for various infections caused by various animal sensitive bacteria. [0003] With the generation of drug resistance, the therapeutic effect of drugs will be reduced, and quinolones are widely distributed in the body. Therefore, when treating respiratory infections such as pneumonia and bronchitis in animals, it is necessary to increase the effective concentration of drugs in lung tissue. The dose of the drug is likely to increase ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61K9/16A61P31/04
Inventor 肖希龙周友中李锐
Owner 北京中农大动物保健品技术研究院
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