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Method for preparing marbofloxacin nanoparticles

A technology of marbofloxacin and nanoparticles, which is applied in the field of preparation of marbofloxacin nanoparticles, can solve the problems of no nano dosage form, unfavorable animal drug use, poor solubility, etc., and achieve increased solubility, good application prospects, The effect of increasing water solubility

Inactive Publication Date: 2019-08-20
SICHUAN AGRI UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there are problems of sensitivity to light, poor solubility, and a certain odor, which is not conducive to the drug use of animals
At present, the drug preparation has a single variety, mainly injections and oral solutions of lactic acid or hydrochloride, and its application field is relatively narrow, mainly used in pets
There are few reports on the new dosage form of the drug, Jiang Yingxin [Jiang Yingxin, Zheng Libin, Hou Zhongke, et al. Preparation method of Mabaofloxacin microcapsules [J]. Fine Chemical Intermediates, 2015,45(03):14-16.] There have been related studies on its microcapsule formulations, but there are no reports related to nano formulations

Method used

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  • Method for preparing marbofloxacin nanoparticles
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  • Method for preparing marbofloxacin nanoparticles

Examples

Experimental program
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Effect test

Embodiment 1

[0023] The present embodiment provides a kind of preparation method of marbofloxacin nanoparticles, comprising the following steps:

[0024] Step 1, after chitosan and volume concentration are 1% glacial acetic acid solution mix homogeneously, add Mabaofloxacin crude drug stirring and dissolving, wherein the mass ratio of chitosan and Mabaofloxacin is 3.3:1, stirring speed Be 500rpm, stirring time is 40min, get Mabaofloxacin-chitosan solution;

[0025] Step 2, after adjusting the pH value of the Mabaofloxacin-chitosan solution with 1% sodium hydroxide to 5.0, add dropwise the sodium polyphosphate solution with a concentration of 1.5mg / mL under stirring at 500rpm, wherein the sodium polyphosphate The mass ratio with Mabaofloxacin is preferably 0.8:1, and the rate of addition is 1 drop / s to obtain Mabaofloxacin-chitosan nanoparticle colloidal solution;

[0026] Step 3. Centrifuge the mabofloxacin-chitosan nanoparticle colloidal solution in a high-speed freezer with a centrifuga...

Embodiment 2

[0028] The present embodiment provides a kind of preparation method of marbofloxacin nanoparticles, comprising the following steps:

[0029] Step 1, after chitosan and the glacial acetic acid solution that volume concentration is 3% are mixed evenly, add the marbofloxacin raw material drug stirring and dissolving, wherein the mass ratio of chitosan and marbofloxacin is 2:1, stirring speed Be 500rpm, stirring time is 40min, get Mabaofloxacin-chitosan solution;

[0030] Step 2, after adjusting the pH value of Mabaofloxacin-chitosan solution with 1% sodium hydroxide to be 5.5, it is the sodium polyphosphate solution of 2mg / mL that drip concentration is 2mg / mL under stirring at 500rpm, wherein sodium polyphosphate and The mass ratio of Mabaofloxacin is preferably 1:1, and the rate of addition is 1 drop / s to obtain Mabaofloxacin-chitosan nanoparticle colloidal solution;

[0031] Step 3. Centrifuge the mabofloxacin-chitosan nanoparticle colloidal solution at 10000 rpm and a centrif...

Embodiment 3

[0033] The present embodiment provides a kind of preparation method of marbofloxacin nanoparticles, comprising the following steps:

[0034] Step 1, after chitosan and the glacial acetic acid solution that volume concentration is 4% are mixed evenly, add the marbofloxacin crude drug stirring and dissolving, wherein the mass ratio of chitosan and marbofloxacin is 4:1, stirring speed Be 550rpm, stirring time is 30min, obtains Mabofloxacin-chitosan solution;

[0035] Step 2, after adjusting the pH value of the Mabaofloxacin-chitosan solution with 1% sodium hydroxide to be 4.5, under stirring at 550rpm, dropwise add the sodium polyphosphate solution with a concentration of 3mg / mL, wherein the sodium polyphosphate and The mass ratio of Mabaofloxacin is preferably 0.6:1, and the rate of addition is 1 drop / s to obtain Mabaofloxacin-chitosan nanoparticle colloidal solution;

[0036] Step 3. Centrifuge the mabofloxacin-chitosan nanoparticle colloidal solution at 10000 rpm and a centri...

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Abstract

The invention provides a method for preparing marbofloxacin nanoparticles. The method comprises the following steps: 1, uniformly mixing chitosan and a glacial acetic acid solution, adding a marbofloxacin raw material drug into the mixture, and performing stirring and dissolving to obtain a marbofloxacin-chitosan solution; 2, adjusting the pH value of the marbofloxacin-chitosan solution to be acidic, dropwise adding a sodium polyphosphate solution into the acidic solution under a stirring state to obtain a marbofloxacin-chitosan nanoparticle colloidal solution; and 3, performing high-speed refrigerated centrifugation on the marbofloxacin-chitosan nanoparticle colloidal solution to obtain the marbofloxacin nanoparticles. The marbofloxacin-chitosan nanoparticles have high encapsulation efficiency, high drug loading capacity and stable property, can overcome the problem that marbofloxacin is sensitive to light, can be used for improving the solubility of marbofloxacin to a certain extentto cover the undesirable odor of the drug, and has an excellent application prospect.

Description

technical field [0001] The invention belongs to the technical field of marbofloxacin pharmaceutical preparations, and in particular relates to a preparation method of marbofloxacin nanoparticles. Background technique [0002] Marbofloxacin, also known as marbofloxacin, exhibits bactericidal activity by inhibiting the topoisomerase required for bacterial DNA replication. It is another first after enrofloxacin, ofloxacin, difloxacin, etc. The third-generation quinolone antibacterial drugs for animals have strong antibacterial activity against most Gram-positive bacteria, are more sensitive to Gram-negative bacteria, and have higher activity than ofloxacin against most anaerobic bacteria. In particular, the positive bacillus and some pathogenic bacteria that are partially resistant to drugs such as lincomycin, doxycycline and sulfonamide are still sensitive to marbofloxacin. The drug has a long elimination half-life and is only approved for dogs and cats to treat deep and supe...

Claims

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Application Information

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IPC IPC(8): A61K9/51A61K47/36A61K31/5395A61P31/04
CPCA61K9/5161A61K31/5395A61P31/04
Inventor 舒刚王晓雪唐子婷黄远玲李琪徐丹冉崇霖靳振坤刘建成赵小玲符华林朱庆
Owner SICHUAN AGRI UNIV
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