Production process of icariside II

A technology of icariin and production process, which is applied in the field of production process of icariin II, can solve the problems of lack of understanding of glycosyl hydrolase, low hydrolysis efficiency, etc., and achieves low equipment requirements, improved purity, and simplified Effects of purification steps

Inactive Publication Date: 2016-09-07
宁波旋光医药科技有限公司 +1
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  • Claims
  • Application Information

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Problems solved by technology

As a result, fungi and bacteria with the ability to hydrolyze glycosyl groups have been developed one after another. However, due to the lack of understanding of glycosyl hydrolases at the molecular level, there are problems such as low hydrolysis efficiency, and it is impossible to greatly improve the hydrolytic enzymes in bacteria or bacteria through genetic engineering. Expression and activity in fungi

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  • Production process of icariside II
  • Production process of icariside II

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Embodiment approach

[0032] A kind of production technology of icariside II:

[0033] (1) First extract icariin monomer from Epimedium: the process steps of extracting icariin monomer from Epimedium are as follows: crush Epimedium to 20-80 mesh, 100g Epimedium pulverized Add 300-800mL ethanol with a mass concentration of 45-85%, heat and reflux for 1-4h to obtain Epimedium crude extract; Epimedium crude extract is dissolved in water and ethyl acetate and separated, and the aqueous phase is extracted with ethyl acetate for 3- 5 times, combined the ethyl acetate phase, washed with saturated brine, dried over anhydrous sodium sulfate, and spin-dried to obtain a dried product; the dried product was heated to reflux with a mixed solvent for 1-4 hours, filtered, and the filter residue was heated to reflux with a mixed solvent for 1-4 hours. 4h, filter, combine the filtrates, and dry to obtain icariin monomer. The mixed solvent is a mixture of water and methanol at a volume ratio of 1:2-3.

[0034] (2)...

Embodiment 1

[0040] Epimedium (40-60 mesh) 100g, 400ml of 75% ethanol was heated to reflux for 1h to obtain 15.5g Epimedium crude extract (HPLC icariin content 10%), dissolved in 150ml water and 150ml ethyl acetate and The layers were separated, and the aqueous phase was extracted three times with 150 ml of ethyl acetate each time. The ethyl acetate phases were combined, washed with saturated brine, dried over anhydrous sodium sulfate, and spin-dried to obtain 8.5 g of a tan solid. Water: 100ml of mixed solvent of methanol = 1:2 was heated to reflux for 1h, filtered, and the filter residue was refluxed with 100ml of mixed solvent for 1h, the mother liquor was combined twice, spin-dried, and dried to obtain 1.49g light yellow solid (HPLC icariin content 98.5%), yield 96.1%.

Embodiment 2

[0042] Epimedium (20-40 mesh) 100g, 75% ethanol 500ml heating reflux 1h, get 14.5g Epimedium crude extract (HPLC icariin content 10%), dissolve with 150ml water and 150ml ethyl acetate and The layers were separated, and the aqueous phase was extracted three times with 150 ml of ethyl acetate each time. The ethyl acetate phases were combined, washed with saturated brine, dried over anhydrous sodium sulfate, and spin-dried to obtain 8.2 g of a tan solid. Water: 100ml of mixed solvent of methanol = 1:2 was heated to reflux for 1h, filtered, and the filter residue was refluxed with 100ml of mixed solvent for 1h, the mother liquors were combined twice, spin-dried, and dried to obtain 1.35g light yellow solid (HPLC icariin content 98.3%), yield 93.1%.

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Abstract

The invention discloses a production process of icariside II, wherein the production process comprises the following steps: firstly, extracting an icariin monomer from herba epimedii; and then, enzymatically hydrolyzing the icariin monomer by virtue of glycosyl hydrolase which is high in catalytic activity, so that the icariside II is obtained. The production process disclosed by the invention has the advantages of being efficient and gentle in reaction, low in cost, high in product purity and applicable to industrial production.

Description

technical field [0001] The invention relates to a production process of medicine, in particular to a production process of icariside II. Background technique [0002] Erectile dysfunction (ED) is a common disease in men. According to the statistics of WHO, men with ED account for about 10% of the world, and the proportion of ED patients in adult men reaches more than 1 / 4. Among the 300 million adult males in my country, there are more than 100 million ED patients, mostly caused by psychological or organic reasons, and they are getting younger and younger, seriously affecting the physical and mental health of couples. [0003] Anti-ED drugs can significantly improve erectile dysfunction in ED patients. According to statistics, the global market size of first-line anti-ED drugs reached US$4.5 billion in 2012. The number of adult male ED patients in my country is huge, and the market potential capacity is tens of billions of dollars. The development and application of these ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C12P17/16
CPCC12P17/162
Inventor 吴涛吴志革高坤陈佳高章华
Owner 宁波旋光医药科技有限公司
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