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
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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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