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Water-soluble tilmicosin phosphate as well as preparation method and application thereof

A technology of tilmicosin phosphate and tilmicosin, which is applied to the preparation of sugar derivatives, chemical instruments and methods, sugar derivatives, etc., can solve the inconvenient anorexia animal drinking water administration, the operator's respiratory discomfort, and the impact Pig feed intake and other problems, to achieve the effect of convenient clinical drug use, uniform product quality, convenient preparation production and clinical use

Inactive Publication Date: 2017-11-24
JIANGXI AOXIN BIOTECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the tilmicosin preparation has the following defects in production and use: the first is that tilmicosin has a special bitter taste, which affects pigs' intake of food, and some individuals even refuse to eat feed mixed with tilmicosin; The tilmicosin has a special irritant, which can easily cause respiratory discomfort of the operator during production and operation, and even severe symptoms such as rhinitis, pharyngitis, systemic allergies, etc. Many sick animals are anorexic during the onset of the disease, and the feed intake decreases, which can be administered through drinking water)
The tilmicosin phosphate soluble powder preparation provided by the above patent has the risk of uneven mixing or incomplete dissolution

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Take 100g of phosphorus pentoxide and slowly add it to 1000g of water, stir to dissolve completely, heat to 50°C, then add 1000g of tilmicosin coarse powder (purchased from Ningxia Tairui Pharmaceutical Co., Ltd.) to dissolve, and use 1mol / L NaOH Adjust the pH of the solution to 5.0-8.0, keep it warm for 20 minutes, add 5g of activated carbon and stir for 5 minutes, filter through a 0.22 micron filter column, add 4000g of anhydrous glucose to the filtrate, stir to dissolve completely, and the mixed solution is spray-dried at 60°C to obtain tilmicol phosphate Star soluble powder, spare.

[0031] Clinical trials with the prepared soluble powder:

[0032] A total of 60 nursery pigs with a body weight of about 15kg were selected in a pig farm in Jinggangshan City, and they were randomly divided into three groups-blank group, low-dose test group and high-dose test group, with 20 pigs in each group, to verify the solubility of the above-mentioned tilmicosin phosphate The eff...

Embodiment 2

[0037] Add 200g of phosphoric acid to 1000g of water, heat to 60°C, then add 1000g of tilmicosin coarse powder (purchased from Ningxia Tairui Pharmaceutical Co., Ltd.) to dissolve, adjust the pH value to 5.0-8.0 with ethanolamine, keep it warm for 20min, add 5g of montmorillonite was stirred for 10min, filtered through a 0.22 micron filter column, and the filtrate was evenly sprayed on 9kg of corncob powder, boiled and dried to obtain tilmicosin phosphate premix, which was set aside.

[0038] Clinical trials with the prepared soluble powder:

[0039]A total of 90 nursery pigs with a body weight of about 25kg were selected in a pig farm in Jinggangshan City, and they were randomly divided into three groups-blank group, low-dose test group and high-dose test group, with 20 pigs in each group. The effect of the mixture on the prevention and control of respiratory diseases. The three groups were all raised in the same way. No medicine was added to the feed of the blank group. The...

Embodiment 3

[0044] The preparation method of the water-soluble tilmicosin phosphate in this embodiment is to add the phosphate-containing substance into water to dissolve, heat to 50° C., then add tilmicosin to dissolve, and then adjust the pH value to 5.0 with an alkaline substance. Keep warm for 15 minutes, then add solid adsorbent, after stirring, filter, concentrate, and dry under reduced pressure to obtain water-soluble tilmicosin phosphate.

[0045] Wherein, the mass ratio of tilmicosin to water is 1:1, and the molar ratio of phosphate radical-containing substance to tilmicosin is 1:1. The phosphate-containing substance is dihydrogen phosphate, the alkaline substance is ammonia solution, and the solid adsorbent is kaolin.

[0046] In the actual preparation process, after being concentrated, suitable auxiliary materials can be added, and then water can be prepared into solutions with different mass-volume ratio concentrations. It can also be prepared by dissolving a suitable filler ...

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PUM

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Abstract

The invention relates to water-soluble tilmicosin phosphate as well as a preparation method and application thereof. The preparation method comprises the steps of adding a substance containing a phosphate radical into water for dissolving, heating to 50-70 DEG C, adding tilmicosin for dissolving, adjusting the pH value to 5.0-8.0 by virtue of an alkaline substance, maintaining the temperature for 15-30 minutes, adding a solid adsorbent, stirring, filtering, concentrating, and drying, so as to obtain water-soluble tilmicosin phosphate. Prepared water-soluble tilmicosin phosphate is used for preventing and treating respiratory tract infection of animal stud stocks and pets. Compared with the prior art, the preparation method has the advantages that water is taken as a solvent, so that the environmental pollution caused due to use of organic solvents such as DMF, toluene and dichloromethane is avoided; and a preparation prepared from water-soluble tilmicosin phosphate has good palatability, so that the ingestion of animals is not influenced; and water-soluble tilmicosin phosphate is applied to the prevention and control of animal diseases and has good mass uniformity and stability and very good application prospects.

Description

technical field [0001] The invention belongs to the field of veterinary drug preparations, and relates to a water-soluble tilmicosin phosphate and a preparation method and application thereof. Background technique [0002] Tilmicosin is a semi-synthetic macrocyclic lipid antibiotic for livestock and poultry. It has strong antibacterial activity and a wide antibacterial spectrum. It is effective against all Gram-positive bacteria and some Gram-negative bacteria, mold It has inhibitory effect on form, spirochete, mycoplasma, etc., especially against Actinobacillus pleuropneumoniae, Pasteurella, Staphylococcus aureus, Streptococcus pyogenes, Corynebacterium pyogenes and mycoplasma of livestock and poultry, which is stronger than Tylosin . Its antibacterial mechanism is to reversibly combine with the 50S subunit of bacterial ribosomes, block transpeptidation and mRNA displacement and inhibit bacterial protein synthesis, thereby inhibiting bacterial reproduction. Sensitive Gram...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/08C07H1/02A61P11/00A61P11/06A61P11/14A61P31/04A61P31/00
CPCC07H17/08C07H1/02
Inventor 王庆福戴多亮肖丽萍樊倩吴有林梁世仁
Owner JIANGXI AOXIN BIOTECH CO LTD
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