Enrofloxacin nanosuspension and preparation method thereof

A nano-suspension and enrofloxacin technology, which is applied in liquid delivery, pharmaceutical formula, emulsion delivery, etc., can solve the problem of low bioavailability of solid granules, poor water solubility of enrofloxacin, and low drug content in emulsions, etc. problem, to achieve the effect of improving bioavailability, improving absorption and bioavailability, and high drug concentration

Active Publication Date: 2017-01-04
GUANGDONG WENS DAHUANONG BIOTECH +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Because enrofloxacin has poor water solubility, bitter taste, strong irritation and easy decomposition, it greatly limits its clinical application in veterinary medicine. At present, commonly used enrofloxacin preparations mainly include emulsion, solid granules and injections, etc., and Ordinary injections have a short half-life, rapid elimination in the body, and require multiple administrations, which is time-consuming and laborious; emulsions have low drug content and require a large number of multiple administrations; solid granules have low bioavailability, which is not conducive to large-scale administration

Method used

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  • Enrofloxacin nanosuspension and preparation method thereof
  • Enrofloxacin nanosuspension and preparation method thereof
  • Enrofloxacin nanosuspension and preparation method thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0033] A kind of enrofloxacin nano-suspension, the preparation method of this enrofloxacin nano-suspension comprises the steps:

[0034] 1) Weigh 4.2 g of enrofloxacin bulk drug and 0.1 g of hydroxyethyl starch sodium and dissolve them in 25 mL of sodium hydroxide solution (pH=8.1) to form a good solvent A;

[0035] 2) Weigh 0.65g of Poloxamer 188, 0.56g of Gelucire44 / 14, and 0.50g of polyethylene glycol 400 and dissolve them in 75mL of aqueous hydrochloric acid (pH=2.5) to form poor solvent B;

[0036] 3) Control the temperature at 10°C, drop the above-mentioned good solvent A into the poor solvent B at a dropping speed of 5mL / min, and control the ultrasonic frequency to 45KHz at the same time, and disperse with ultrasonic stirring. After the dropping is completed, continue ultrasonic dispersion for 0.5h, A primary nanosuspension with blue opalescence is formed;

[0037] 4) Put the obtained primary nanosuspension in a high-pressure homogenizer, and circulate it 5 times under...

Embodiment 2

[0040] A kind of enrofloxacin nano-suspension, the preparation method of this enrofloxacin nano-suspension comprises the steps:

[0041] 1) Weigh 4.5g of enrofloxacin bulk drug and 0.1g of sodium hydroxyethyl starch, dissolve in 25mL of sodium hydroxide solution (pH=8.2) to form good solvent A;

[0042] 2) Weigh 0.85g soybean lecithin and 0.60g Labrasol, dissolve in 75mL phosphoric acid aqueous solution (pH=2.1) to form poor solvent B;

[0043] 3) Control the temperature at 8°C, drop the above-mentioned good solvent A into the poor solvent B at a rate of 2.5mL / min, and control the ultrasonic frequency to 45KHz at the same time, and disperse with ultrasonic stirring. A primary nanosuspension with blue opalescence is formed;

[0044] 4) Put the obtained initial nano-suspension in a high-pressure homogenizer, and circulate 10 times under a pressure of 500 bar to obtain the enrofloxacin nano-suspension;

[0045]The enrofloxacin nanosuspension was detected by a laser nanometer pa...

Embodiment 3

[0047] A kind of enrofloxacin nano-suspension, the preparation method of this enrofloxacin nano-suspension comprises the steps:

[0048] 1) Weigh 4.05g of enrofloxacin bulk drug and 0.15g of hydroxyethyl starch sodium and dissolve in 25mL of phosphate buffer (pH=8.5) to form good solvent A;

[0049] 2) Dissolve 0.82g of Labrasol and 0.49g of polyethylene glycol 400 in 75mL of phosphoric acid aqueous solution (pH=2.8) to form poor solvent B;

[0050] 3) Control the temperature at 2°C, drop the above-mentioned good solvent A into the poor solvent B at a dropping speed of 10mL / min, and control the stirring speed at 200r / min at the same time, stir and disperse with a high-shear emulsifier, and the dropping is completed. Continue stirring for 2h to form an initial nanosuspension;

[0051] 4) Put the gained initial nano-suspension in a high-pressure homogenizer, and circulate it 4 times under 1000 bar pressure to obtain the enrofloxacin nano-suspension;

[0052] The enrofloxacin n...

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Abstract

The invention discloses an enrofloxacin nanosuspension and a preparation method thereof. The enrofloxacin nanosuspension is prepared from enrofloxacin and a stablizer at a mass ratio of 1:(0.1-10); the stablizer is one or more selected from tween 80, soya bean lecithin, polyvinyl pyrrolidone K30, poloxamer 188, poloxamer 407, hydroxypropyl methylcellulose, sodium deoxycholate, sodium hydroxyethyl starch, glycerin monostearate, polyethylene glycol 400, octyl / decyl mono and diglycerides, gelucire and caprylic / capric triglyceride. The invention also provides a preparation method. The enrofloxacin nanosuspension is high in medicine concentration, good in absorption, long in action time and good in stability, and is also capable of improving the bioavailability.

Description

technical field [0001] The invention belongs to the field of veterinary preparations, and in particular relates to an enrofloxacin nano-suspension and a preparation method thereof. Background technique [0002] Enrofloxacin (ENR), also known as ethyl ciprofloxacin, is a third-generation quinolone antibacterial drug specially used for animals. Its mechanism of action is to achieve antibacterial effect by inhibiting bacterial DNA helicase, and its metabolism in animals mainly Is off ethyl and become ciprofloxacin. Enrofloxacin is a spectrum bactericidal drug, effective against Mycoplasma, Escherichia coli, Klebsiella, Salmonella, Proteus, Pseudomonas aeruginosa, Haemophilus, Pasteurella multocida, Pasteurella hemolyticus, Staphylococcus aureus, Streptococcus, etc. all have bactericidal effect, have the advantages of broad bactericidal spectrum, wide distribution in the body, and no cross-resistance with other drugs. In veterinary medicine, it is mainly used to prevent and tre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K47/24A61K47/32A61K47/34A61K47/38A61K47/28A61K47/36A61K47/14A61K31/496A61P31/04
CPCA61K9/10A61K31/496A61K47/10A61K47/14A61K47/24A61K47/26A61K47/28A61K47/32A61K47/36A61K47/38
Inventor 陈良柱方炳虎潘志坤陈明余鹏灵
Owner GUANGDONG WENS DAHUANONG BIOTECH
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