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Preparation method of amygdalin

The technology of amygdalin and amygdalin is applied in the field of preparation of amygdalin, which can solve the problems of restricting the in-depth research of amygdalin medicines, not preparing D-amygdalin or L-amygdalin epimers separately, and the like. , to achieve the effect of low cost, environmental friendliness and high efficiency

Active Publication Date: 2016-04-06
JIANGSU KANION PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, there is no method for preparing D-amygdalin or L-amygdalin epimer alone, which greatly limits the in-depth research of bitter almond medicine in the later stage

Method used

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  • Preparation method of amygdalin
  • Preparation method of amygdalin
  • Preparation method of amygdalin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] 1. Extraction: add 20 grams of bitter almonds (commercially available) to 5 times the amount of water, boil for 1 hour, repeat 2 times, combine the extracts, and concentrate under reduced pressure to obtain the crude extract of amygdalin.

[0035] 2. Extraction, extract the crude extract obtained in step 1 with ethyl acetate at a ratio of 1:1 by volume, repeat twice, and then extract three times with n-butanol at a ratio of 1:1 by volume. The n-butanol extract was collected and concentrated under reduced pressure to obtain the amygdalin extract.

[0036] 3. Dynamic axial compression reverse chromatographic separation (DAC-HB80 Jiangsu Hanbang Technology Co., Ltd.). The above extract was separated by compression chromatography, using C 18 Chromatographic column (250mmx50mm, 10μm), eluting with 15% acetonitrile-0.5% formic acid water as the mobile phase by mass percentage, flow rate: 30ml / min, column temperature: room temperature, pH value: 2.0, detection wavelength: 210...

Embodiment 2

[0049] 1. Extraction. Add 2 kg of peach kernels (commercially available) to 8 times the amount of water, boil for 2 hours, repeat 3 times, combine the extracts, and concentrate under reduced pressure to obtain the crude extract of amygdalin.

[0050] 2. Extraction, the crude extract obtained in step 1 was extracted with ethyl acetate at a volume ratio of 1:1, repeated 3 times, and then extracted with n-butanol at a volume ratio of 1:1 for 3 times. Take n-butanol extract, concentrate under reduced pressure to obtain amygdalin extract.

[0051] 3. Dynamic axial compression reverse chromatographic separation (DAC-HB80 Jiangsu Hanbang Technology Co., Ltd.). The above extract was separated by compression chromatography, using C 18 Chromatographic column (250mmx50mm, 10μm), eluted with 11% acetonitrile-0.2% formic acid water as mobile phase, flow rate: 100ml / min, column temperature: room temperature, pH value: 5.0, detection wavelength: 210nm, injection volume: 5000μL . Observe t...

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Abstract

The invention discloses a preparation method of D-amygdalin and / or neoamygdalin; the amygdalin is extracted from peach kernels or bitter apricot kernels, an organic solvent is used for extraction, chromatography is used for separating D-amygdalin and neoamygdalin isomers and for detecting the purity of the two isomers, and nuclear magnetic resonance is used for detecting the structures of the two isomers. By adoption of the reverse chromatography technique and combination of the NMR technology, high-precision separation preparation of arbitrary one epimer of D-amygdalin and / or neoamygdalin of the amygdalin is realized. The separation operation process is simple, easy to operate and easy to repeat, the separation cycle is short, and the efficiency is high; moreover, the method is low in cost, friendly to the environment, and suitable for large-scale industrialized production; and in addition, the purity and the yield of the prepared D-amygdalin and neoamygdalin are higher.

Description

technical field [0001] The invention relates to a preparation method of amygdalin, in particular to a preparation method of D-amygdalin or L-amygdalin. Background technique [0002] Amygdalin is a main component of bitter almonds. It has the effects of antitussive and asthmatic, anti-tumor, blood pressure-lowering and anti-coagulant effects. It has been widely used in the field of medicine as an anti-phlegm and anti-cancer drug; Qi stagnation, intestinal dryness, constipation, edema and fullness have good clinical therapeutic effects. [0003] The methods currently used to prepare amygdalin mainly use water extraction, ethanol reflux, ultrasonic extraction, and resin separation and purification. Although it has been reported that the above-mentioned process has been improved and its optimal conditions have been studied to obtain amygdalin with higher purity or yield. To prevent the amygdalinase in bitter almonds from hydrolyzing amygdalin; using different solvents and diff...

Claims

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Application Information

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IPC IPC(8): C07H15/18C07H1/08
CPCC07H1/08C07H15/18
Inventor 萧伟谢雪宋亚玲温建辉赵祎武王雪晶罗鑫倪付勇黄文哲王振中
Owner JIANGSU KANION PHARMA CO LTD
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