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Water-soluble marbofloxacin as well as preparation method and application thereof

A marbofloxacin and water-soluble technology, applied in the field of water-soluble marbofloxacin and its preparation, can solve the problems of unstable preparation solvent, poor solubility of marbofloxacin, poor solubility of sodium carbonate, etc. Drug route, low cost, and the effect of solving water insoluble

Active Publication Date: 2017-12-08
JIANGXI AOXIN BIOTECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Marbofloxacin has poor solubility in water. In the above-mentioned patent, sodium carbonate is used as co-solvent to prepare marbofloxacin soluble powder, which is prone to uneven mixing, which leads to the risk of unstable solubility of the preparation in water, that is, the content of sodium carbonate is too high The part with good solubility, the part with low sodium carbonate content has poor solubility

Method used

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  • Water-soluble marbofloxacin as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 1

[0031] Add 400g of lactic acid to 600g of water and mix evenly, heat to 60°C, then add 200g of marbofloxacin coarse powder (purchased from Zhejiang Guobang Medicine Liquid Co., Ltd.) to dissolve, adjust the pH value to 3.0 with ethanolamine, and keep warm for 1h. Add 5 g of activated carbon and stir for 30 min, filter through a 0.22 micron filter column, concentrate and dry under reduced pressure (-0.1 MPa, 60° C.), and obtain a coarse water-soluble marbofloxacin powder.

[0032] Take the above-mentioned water-soluble marbofloxacin coarse powder, add anhydrous glucose, filter through a 0.22 micron filter column, concentrate, dry and pulverize the filtrate under reduced pressure to obtain a soluble powder with a mass fraction of marbofloxacin of 10%, and set aside.

[0033] Clinical trials with the prepared soluble powder:

[0034] A total of 40 lactating sows were selected in a pig farm in Jinggangshan City and randomly divided into two groups—the blank group and the test grou...

Embodiment 2

[0039] Take 150g of gluconolactone and add it to 1000g of water and mix evenly, heat to 60°C, then add 200g of marbofloxacin coarse powder (purchased from Zhejiang Guobang Medicine Liquid Co., Ltd.) to dissolve, adjust with 1mol / L NaOH solution The pH value is 3.5, heat preservation for 1 h, add 5 g of activated carbon and stir for 30 min, filter with a 0.22 micron filter column, and spray dry (60° C.) to obtain a coarse water-soluble marbofloxacin powder.

[0040]Take 500ml of water for injection, add 2g of sodium metabisulfite, 0.5g of disodium edetate, stir to dissolve, add the above-mentioned water-soluble powder (containing 100g of marbofloxacin), stir to completely dissolve, then add 1g of activated carbon, and stir for 10 Minutes, filter with a 0.22 micron filter column, add water for injection to the filtrate, set the volume to 1000ml, adjust the pH value to 4.5 with 1mol / L NaOH solution or 1mol / L gluconolactone solution, filter with a 0.22 micron filter column, pour P...

Embodiment 3

[0047] Take 100g of phosphoric acid and add it to 900g of water, mix evenly, heat to 60°C, then add 100g of marbofloxacin coarse powder (purchased from Zhejiang Guobang Medicine Liquid Co., Ltd.) to dissolve, adjust the pH value with 1mol / L NaOH solution 3.0, keep warm for 1 hour, add 5g of activated carbon and stir for 30 minutes, filter with a 0.22 micron filter column, add 1900g of anhydrous glucose, stir to dissolve completely, spray granulate to make marbofloxacin granules, and set aside.

[0048] Clinical trials were carried out with the prepared marbofloxacin granules:

[0049] A total of 50 farrowing sows were selected from a pig farm in Jinggangshan City and randomly divided into two groups—the blank group and the test group, with 25 pigs in each group, to verify the preventive effect of the above-mentioned marbofloxacin soluble powder on mastitis in sows. The blank group was fed normally without adding any drugs; the test group was fed in the same way as the control ...

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Abstract

The invention relates to water-soluble marbofloxacin as well as a preparation method and application thereof. The preparation method comprises the following steps: adding an acidic substance into water for dissolution, heating to 50-70 DEG C, adding a marboxacin coarse powder, dissolving, subsequently adjusting a pH value to 3.0-4.0 with an alkaline substance, performing heat preservation for 1-2.5 hours, then adding a solid adsorbent, stirring and mixing, then filtering, concentrating and drying; the prepared water-soluble marbofloxacin is used for treating respiratory tract infection, digestive canal infection and urogenital tract infection or mammitis of breeding animals and pets. Compared with the prior art, the water-soluble marbofloxacin provided by the invention has the benefits that the water is taken as a solvent in the preparation process, so that the use of DMF, methylbenzene, dichloromethane and other organic solvents is avoided, and pollution to the environment is reduced; the process steps are simple, the cost is low, the problem that the marbofloxacin is insoluble in water is effectively solved, the administration route of the marbofloxacin is increased, the clinical medication is convenient, and the application prospect is good.

Description

technical field [0001] The invention belongs to the field of veterinary drug preparations, and relates to a water-soluble marbofloxacin and a preparation method and application thereof. Background technique [0002] Marbofloxacin is a new quinolone antibacterial drug. Quinolones are divided into first, second, third, and fourth generations according to their invention and antibacterial properties: the first generation of quinolones has antibacterial effects only on Escherichia coli, Shigella, Klebsiella, and a small number of Proteus. Specific varieties include nalidixic acid and pyrrole acid, etc., which are rarely used because of poor curative effect. The second-generation quinolones have expanded antibacterial spectrum, and have certain antibacterial effects on Enterobacter, Citrobacter, Pseudomonas aeruginosa, and Serratia. Pipemidic acid is the main domestic application variety, and abroad there are neooxic acid and methoxquinic acid. The third-generation quinolones ...

Claims

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Application Information

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IPC IPC(8): C07D498/06A61K31/5395A61P31/04
CPCC07D498/06
Inventor 王庆福戴多亮肖丽萍刘文礼吴有林梁世仁
Owner JIANGXI AOXIN BIOTECH CO LTD
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