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Preparation method of medicinal salt of 3-acetyl desmycosin and application thereof

A technology of tylosin and mycose, which is applied in the field of biomedicine to achieve the effects of easy industrialization, simple and efficient preparation process

Active Publication Date: 2020-01-14
CHINA ANIMAL HUSBANDRY IND
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Although tyvanectin has obvious advantages in the treatment of some animal diseases compared with tylosin, it is necessary to modify tyvanectin by biological or chemical methods to further improve the efficacy of this macrolide antibiotic Research work has not stopped

Method used

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  • Preparation method of medicinal salt of 3-acetyl desmycosin and application thereof
  • Preparation method of medicinal salt of 3-acetyl desmycosin and application thereof
  • Preparation method of medicinal salt of 3-acetyl desmycosin and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1 Laboratory preparation process of 3-acetyl decarbamucose tylosin tartrate

[0035] Weigh 200 g of tyvalectin tartrate with a purity of 85.1%, add 4000 mL of water, adjust the pH value of the solution to 1.5 with 5% sulfuric acid solution, heat the solution system to 50° C. and maintain the temperature for 2 hours. Add about 4000 mL of butyl acetate to the solution, adjust the pH value of the solution to 12 with 30% sodium hydroxide solution, and stir at a constant speed with a mechanical stirrer at a speed of 100 rpm for 1 hour. Let the solution stand for at least 2 hours, until the organic solvent phase and the water phase are completely separated into two phases, remove the water phase, and obtain the butyl acetate phase; add 1000 mL of water to the butyl acetate phase, and adjust the pH value of the solution with solid tartaric acid to 5.0, use a mechanical stirrer with a speed of 100 rpm for uniform stirring, and the stirring time is 1 hour. Let the solut...

Embodiment 2

[0036] Example 2 The industrial production process of 3-acetyl decarbaminosyl tylosin tartrate

[0037] Weigh 200kg of tyvalactin tartrate with a purity of 85.1%, add 4000L of water, adjust the pH value of the solution to 1.6 with 5% sulfuric acid solution, heat the solution system to 50-70°C and maintain the temperature for 2 hours. Add about 4000 L of butyl acetate to the solution, adjust the pH value of the solution to 12.8 with 30% sodium hydroxide solution, and stir at a constant speed with a mechanical stirrer at a speed of 100 rpm for 1 hour. Let the solution stand for 5 hours, until the organic solvent phase and the water phase are completely separated into two phases, remove the water phase to obtain the butyl acetate phase; add 1000L of water to the butyl acetate phase, and adjust the pH value of the solution to 4.8 with solid tartaric acid , using a mechanical stirrer with a speed of 100 rev / min for uniform stirring, and the stirring time is 1 hour. Let the solutio...

Embodiment 3

[0038] Antibacterial effect test of embodiment 3 medicinal compounds

[0039] 1, test drug: the tartrate of the compound shown in formula (I). Control drugs: tyvanectin tartrate, tylosin tartrate, tiamulin fumarate, tilmicosin phosphate, doxycycline hydrochloride, oxytetracycline, florfenicol.

[0040] 2. Test strains: Mycoplasma Synoviae (MS), standard strain (WVU1853, China Veterinary Drug Control Institute).

[0041] 3. Test method

[0042] 3. The 1MS standard strain was revived and cultured, and when the color of the medium turned orange, it was subcultured twice as the seed bacterial liquid. For quantitative counting of MS, the color change unit method (colour change unit, CCU) was used to calculate CCU50. For the dilution of MS bacteria solution, take appropriate amount of seed bacteria solution and dilute to 10 -4 , with a titer of about 10 4CCU / mL. The CCU of the standard strain of Mycoplasma gallinarum (WVU1853) was 8787.

[0043] 3.2 MIC determination: Add dru...

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Abstract

The invention provides a preparation method of a medicinal salt of 3-acetyl desmycosin and an application thereof. The medicinal salt of 3-acetyl desmycosin is selected from hydrochloride, hydrobromide, sulfate, nitrate, phosphate, mesylate, maleate, tartrate, succinate, acetate, trifluoroacetate, fumarate, citrate, citrate, benzene sulfonate, benzoate, benzene sulfonate, lactate or malate. The medicinal salt of the 3-acetyl desmycosin prepared by the method disclosed by the invention can be used as an antimycoplasma active compound. The bacteriostatic tests show that the antibacterial activity of the compound is obviously higher than that of existing tylosin derivatives such as tilmicosin, tylosin and acetylisovaleryltylosin tartrate, and a new choice is provided for treating related diseases in the animal breeding industry. The active compound is simple and efficient in preparation process, stable in quality and easy to industrialize.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a preparation method and application of 3-acetyl descarbamicose tylosin medicinal salt. Background technique [0002] Tyvanectin, also known as super tylosin, chemically named 3-O-acetyl-4”-O-isovaleryl tylosin, is a sixteen-ring macrolide antibiotic for livestock and poultry Tyvanectin is a new type of macrolide antibiotic obtained by biotransformation of tylosin by Streptomycesthermotolerans, acetylation at the 3-position and isovalerylation at the 4” position, because of the change in its chemical structure Compared with tylosin, it has obvious advantages in antibacterial spectrum, antibacterial activity, drug resistance, chemical stability, oral absorption and blood drug concentration. [0003] Although tyvanectin has obvious advantages in the treatment of some animal diseases compared with tylosin, it is necessary to modify tyvanectin by biological or chemical methods to further ...

Claims

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Application Information

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IPC IPC(8): C07H17/08C07H1/00A61P31/04A61P31/10A61P31/00A61K31/7048
CPCA61P31/00A61P31/04A61P31/10C07H1/00C07H17/08Y02A50/30
Inventor 梁景乐牛志强李新国颜晓冬赵学朋闵江张正海
Owner CHINA ANIMAL HUSBANDRY IND