Veterinary enrofloxacin solid lipid nanosuspension and preparation method thereof

A technology of solid lipid nanometer and enrofloxacin, which is applied in medical preparations with non-active ingredients, medical preparations containing active ingredients, and liquid delivery, etc. Low drug dosage and other problems, to achieve the effect of reducing clinical drug dosage, improving absorption, and improving bioavailability

Active Publication Date: 2018-05-04
HUAZHONG AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Studies have reported that myristic acid, palmitic acid and stearic acid solid lipid nanoparticles prepared by hot-melt emulsification ultrasonography can improve the in vivo absorption and circulation time of enrofloxacin in mice, but the three fatty acid solid lipid nanocapsules The sealing rate is lower than 70%, and the drug loading is lower than 7.3%, which limits the possibility of its wide clinical application (Xie et al., 2011)

Method used

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  • Veterinary enrofloxacin solid lipid nanosuspension and preparation method thereof
  • Veterinary enrofloxacin solid lipid nanosuspension and preparation method thereof
  • Veterinary enrofloxacin solid lipid nanosuspension and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0059] The formula of enrofloxacin solid lipid nanosuspension for veterinary use is shown in Table 1, and the preparation method is as follows:

[0060] (1) Weigh 12g of behenic acid in a test tube heated in an oil bath at 120°C, add 2g of enrofloxacin raw material to it after heating to melt, and form a transparent enrofloxacin solution under constant stirring;

[0061] (2) Weigh 0.2g of sodium lauryl sulfate and sodium bisulfite and add them to 30mL of sterilized water to make a solution;

[0062] (3) The solution prepared in step (2) is heated in an oil bath at 120°C and added to the enrofloxacin solution prepared in step (1) at a stirring speed of 3000-5000 r / min to form an oil-in-water colostrum;

[0063] (4) Disperse the colostrum prepared in step (3) for 2 to 5 minutes to form an oil-in-water emulsion;

[0064] (5) Quickly pour the emulsion prepared in step (4) into 30 mL of sterilized water at 4° C. to obtain a suspension of enrofloxacin particles;

[0065] (6) Use a high-pressu...

Embodiment 2

[0070] The formula of enrofloxacin solid lipid nanosuspension for veterinary use is shown in Table 2. The preparation method is as follows:

[0071] (1) Weigh 12g of behenyl alcohol into a test tube heated in an oil bath at 120°C, add 2g of enrofloxacin raw material to it after heating to melt, and form a transparent enrofloxacin solution under constant stirring;

[0072] (2) Weigh 0.5g poloxamer 188, 0.2g sodium sulfoxylate formaldehyde and 3.5g dimethyl dioctadecyl ammonium chloride and add them to 30mL sterile water to make a solution;

[0073] (3) The solution prepared in step (2) is heated in an oil bath at 120°C and added to the enrofloxacin solution prepared in step (1) at a stirring speed of 3000-5000 r / min to form an oil-in-water colostrum;

[0074] (4) Disperse the colostrum prepared in step (3) for 2 to 5 minutes to form an oil-in-water emulsion;

[0075] (5) Quickly pour the emulsion prepared in step (4) into 20 mL of sterilized water at 4° C. to obtain a suspension of enro...

Embodiment 3

[0081] The formula of enrofloxacin solid lipid nanosuspension for veterinary use is shown in Table 3. The preparation method is as follows:

[0082] (1) Weigh 20g of behenyl alcohol and 15g of behenic acid into a test tube heated in an oil bath at 120°C, add 6g of enrofloxacin raw material to it after heating to melt, and form transparent enrosha under constant stirring. Star solution

[0083] (2) Weigh 2g polyvinylpyrrolidone K separately 15 Add 1g formaldehyde and sodium hyposulfite to 40mL sterile water to make a solution;

[0084] (3) The solution prepared in step (2) is heated in an oil bath at 120°C and added to the enrofloxacin solution prepared in step (1) at a stirring speed of 3000-5000 r / min to form an oil-in-water colostrum;

[0085] (4) Disperse the colostrum prepared in step (3) for 2 to 5 minutes to form an oil-in-water emulsion;

[0086] (5) Quickly pour the emulsion prepared in step (4) into 15 mL of sterilized water at 4° C. to obtain a suspension of enrofloxacin par...

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Abstract

The invention belongs to the technical field of preparation of veterinary drugs and particularly relates to a veterinary enrofloxacin solid lipid nanosuspension and a preparation method thereof. The technological production of a preparation is implemented with a high-pressure homogenization technique. In terms of W / V, a suspension injection is prepared from 12%-35% of a solid lipid substrate, 2%-6% of crude enrofloxacin, 0.2%-4% of an active agent, 0.2%-1% of an antioxidant and the balance of sterile water. The solid lipid substrate is good in physiological compatibility and biodegradable, theencapsulation efficiency and drug loading capacity of nanoparticles are high, the preparation method is simple, the production cost is low, and large-scale industrial production is easy. The solid lipid nanosuspension has an obvious slow-release effect, in-vivo absorption and in-cell intake of active molecules can be increased, clinical administration times can be reduced, and the nanosuspensionis non-irritant to target animals and can be used for preventing and treating bacterial digestive tract and respiratory diseases of pigs and chicken.

Description

Technical field [0001] The invention belongs to the field of preparation of veterinary drug preparations, and specifically relates to an enrofloxacin solid lipid nano suspension for veterinary use and a preparation method thereof. Background technique [0002] Enrofloxacin is a synthetic animal-specific fluoroquinolone antibacterial drug, which can achieve antibacterial effect by inhibiting bacterial DNA helicase. It has a broad antibacterial spectrum, strong bactericidal activity, wide distribution in the body, small toxic and side effects, and other antibacterial The drug has no cross-resistance and other characteristics, and is mainly used to treat animal bacterial infectious diseases. Although enrofloxacin has strong antibacterial activity, its weak ability to accumulate in cells results in limited clinical treatment of intracellular infections. The poor solubility and bitterness of enrofloxacin cause greater changes in its absorption in animals, which affects the clinical t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/496A61K47/10A61K47/12A61P31/04
CPCA61K9/0019A61K9/0053A61K9/10A61K31/496A61K47/10A61K47/12
Inventor 袁宗辉谢书宇杨飞陶燕飞瞿玮潘源虎陈冬梅黄玲利程古月刘振利谢长清
Owner HUAZHONG AGRI UNIV
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