Pharmaceutical composition containing arctigenin and preparation method

A technique for arctigenin and composition is applied in the field of medicinal composition containing arctigenin and its preparation field, and can solve the problems of increasing the water solubility of arctigenin, increasing the bioavailability, and poor solubility of arctigenin And other issues

Inactive Publication Date: 2007-09-19
海南盛科天然药物研究院有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The object of the present invention is to provide a medicinal composition containing arctigenin and its preparation method, increase the water solubility of arctigenin without changing the structure of arctigenin, and overcome the poor solubility of arctigenin deficiencies and increase its bioavailability

Method used

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  • Pharmaceutical composition containing arctigenin and preparation method

Examples

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Effect test

preparation example 1

[0016] Preparation Example 1: Preparation of Arctiin

[0017] The burdock fruit is ground into a coarse powder, extracted with petroleum ether, ethyl acetate and 80% ethanol in sequence, and the solvent is recovered separately, and the ethanol extract is taken. Adjust this extract to a certain volume with water, extract with n-butanol, reclaim n-butanol to obtain n-butanol extract, take the above-mentioned n-butanol extract dry paste, and carry out macroporous adsorption resin column chromatography (dry paste and The resin ratio is 1:30). First wash with water until the eluent is colorless, then use 30% ethanol to elute until the solution is colorless, recover the ethanol, concentrate and stand still, and then gray-white powder particles appear. The off-white powder was passed through a silica gel H decompression column (dry packing), eluted with chloroform-methanol (9:1), and after the solvent was recovered, pure white crystals were obtained which were arctiin, and the purit...

preparation example 2

[0018] Preparation Example 2: Preparation of Arctigenin

[0019] Add arctiin from Preparation Example 1 into sterile water, heat to dissolve, let cool, add an appropriate amount of helicase, incubate on a constant temperature shaker at 37°C for 36 hours, add ethanol to stop the enzymatic hydrolysis reaction, evaporate the enzymolysis solution to dryness under reduced pressure, and the residue Add chloroform to dissolve, take the chloroform solution, recover the solvent to obtain the degraded product, pass the obtained degraded product through a silica gel H decompression column (dry packing), and elute with a gradient of chloroform-methanol, and after recovering the solvent, a pure white crystal is obtained, which is burdock Aglycone, the purity measured by HPLC method is 98.2%.

Embodiment 1

[0021] Take 100 mg of arctigenin, heat it with about 15 mL of 60% ethanol to dissolve it; weigh 3.0 g of hydroxypropyl-β-cyclodextrin, add 5 mL of water and stir to dissolve at room temperature. Arctigenin solution was added dropwise. After adding the solution, continue to stir until the solution is viscous, and dry under reduced pressure to obtain.

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Abstract

A composition for medicine having arctigenin and a method for preparing the same, in particular the arctigenin is involved in a cyclodextrin derivative, which mixture ratio is in a range of 1g:3g-30g, and the composition can effectively increase solubility and bioavailability of the arctigenin.

Description

technical field [0001] The invention relates to a medicinal composition containing arctigenin and a preparation method thereof, in particular to an inclusion compound of arctigenin and cyclodextrin. Background technique [0002] Arctium lappa L. is a plant of the genus Arctium of Compositae, and its seeds, roots and leaves can be used as medicine. The commonly used medicinal part of burdock is its fruit, which is called burdock seed. Its taste is hard and cold. It has the effects of evacuating wind-heat, clearing the lungs and clearing the rash, reducing swelling and detoxification, and is used for wind-heat and cold, cough with excessive phlegm, sore throat, opaque rash, itchy rubella, carbuncle and sore. Burdock mainly contains lignans and their glycosides. There are many types of lignans found in nature. Recent studies have shown that the physiological and pharmacological activities of lignans with different structural types are not the same. The lignans in Arctium ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/365A61K47/40A61P3/10A61P29/00A61P31/12A61P35/00A61P37/02
Inventor 滕厚雷于翠翠韩飞翟大伟刘军锋邵萌
Owner 海南盛科天然药物研究院有限公司
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