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Separation and purification method of high-purity moxidectin

A technology for the separation and purification of moxidectin, which is applied in the field of antibiotic separation and purification, can solve the problems of complex separation process, large amount of solvent, and high cost of moxidectin separation, and achieve good extraction ability, improved purification effect, and short phase separation time Effect

Active Publication Date: 2018-02-13
JIANGSU WEI LING BIOCHEM TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The present invention provides a method for the separation and purification of high-purity moxidectin, which solves the problems in the background technology that the separation process of moxidectin is complex, requires multiple chromatographic operations, requires a large amount of solvent, low yield, and high cost.

Method used

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  • Separation and purification method of high-purity moxidectin
  • Separation and purification method of high-purity moxidectin
  • Separation and purification method of high-purity moxidectin

Examples

Experimental program
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Effect test

Embodiment 1

[0035] The fermentation broth produced by the streptomycin fermentation is separated from the solid and liquid, and the nimoxine concentrate is obtained after leaching, and the methanol solution of moximectin (MX-4) is obtained by the protection, oxidation, deprotection and amination reaction. 34.5kg, content 12.3%, purity 80.6%, pump the above solution into a stainless steel reactor, add MX-4 methanol solution equivalent to 40±1 times the volume of 68-72% methanol / acetonitrile / ethanol aqueous mobile phase to match The column liquid was prepared, and the titer was 21527μg / mL.

[0036] Take the mobile phase to equilibrate the preparative column (model: DAC-100 chromatography packing: ODS-C18) for 20-25 minutes at a flow rate of 2L / min.

[0037] Add 20 kg of methyl methacrylate to the methanol solution of moximectin and heat for 1 h.

[0038] Sampling: open the system equipment monitor, select the appropriate online filter, set the sampling mode to automatic, set the feed flow rate to...

Embodiment 2

[0045] The fermentation broth produced by the streptomycin fermentation is separated from the solid and liquid, and the nimoxetine concentrate is obtained after leaching, and the methanol solution of moximectin is obtained by the protection, oxidation, deprotection and amination reaction (conventional reaction). MX-4) 31.3kg, the content is 15.7%, the purity is 84.7%, the above solution is pumped into a stainless steel reactor, and the volume of the MX-4 methanol solution is 40±1 times the volume of 68-72% methanol / acetonitrile / The mobile phase of the ethanol aqueous solution was mixed into the upper column liquid, and the titer was 18828μg / mL.

[0046] Take the mobile phase to equilibrate the preparative column (model: DAC-100 chromatography packing: ODS-C18) for 20-25 minutes at a flow rate of 2L / min.

[0047] 21kg methyl methacrylate was added to the methanol solution of moximectin and heated for 1.5h.

[0048] Sampling: open the system equipment monitor, select the appropriate ...

Embodiment 3

[0055] The fermentation broth produced by the streptomycin fermentation is separated from the solid and liquid, and the nimoxetine concentrate is obtained after leaching, and the methanol solution of moximectin is obtained by the protection, oxidation, deprotection and amination reaction (conventional reaction). MX-4) 28.5kg, content 15.8%, purity 80.8%, pump the above solution into a stainless steel reactor, add MX-4 methanol solution equivalent to 40±1 times the volume of 68-72% methanol / acetonitrile / The mobile phase of the ethanol aqueous solution was mixed into the upper column liquid, and the titer was 22214μg / mL by sampling.

[0056] Take the mobile phase to equilibrate the preparative column (model: DAC-100 chromatography packing: ODS-C18) for 20-25 minutes at a flow rate of 2L / min.

[0057] 22kg of methyl methacrylate was added to the methanol solution of moximectin and heated for 2h.

[0058] Sampling: open the system equipment monitor, select the appropriate online filter...

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Abstract

The invention provides a separation and purification method of high-purity moxidectin. The method includes the steps: performing solid-liquid separation on fermented liquid generated by streptomycin in a fermented manner; performing leaching to obtain nemadectin concentrated solution; performing upper protection, oxidation, deprotection and amination reaction on the nemadectin concentrated solution to obtain moxidectin methanol solution (MX-4); performing preparative HPLC (high-performance liquid chromatography) on the moxidectin methanol solution, performing concentration, extracting and layering, crystal, suction filtration and drying to obtain moxidectin finished products with the purity of 98%. The method is high in separation purity and product yield, low in solvent consumption, lessin operation step and suitable for commercial mass production.

Description

Technical field [0001] The invention belongs to the technical field of separation and purification of antibiotics, in particular to a method for separation and purification of high-purity moxicillin. Background technique [0002] Moxidectin (Moxidectin) is a new type of antiparasitic drug. It is a single-component macrolide antibiotic fermented by Streptomyces. Moxidectin can increase the level of Cl- in the postsynaptic membrane of the worm. Permeability, thereby blocking the transmission of nerve signals, and ultimately paralyzing the nerves and causing the death of the worm. Moximectin enhances the permeability of the nerve membrane to Cl- through two different ways. One is to enhance the release of the inhibitory transmitter r-aminobutyric acid (GABA) in the peripheral nerves of the insects; the other is Cause the Cl-channel controlled by glutamate to open. The difference from other macrolide antiparasitic drugs is that its composition is single. Its drug concentration in a...

Claims

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Application Information

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IPC IPC(8): C07D493/22
CPCC07D493/22
Inventor 凌青云卢创刘言华苗玉武
Owner JIANGSU WEI LING BIOCHEM TECH CO LTD
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