The invention discloses the preparation and application of flavonol as a brain targeting synergist. The inventors have found in long-term experimental research that some flavonol compounds, especially kaempferol, rutin, troxerutin, myricetin, hesperidin, and their hydroxy derivatives, especially their glycosides, esters, ethers Derivatives, can be very good to promote the therapeutic drug molecules ginsenoside, stilbene glycoside, resveratrol, levodopa, edaravone, vinpocetine, nicergoline, cytosine When choline, oxiracetam, etc. enter the brain tissue, the concentration of the drug in the brain tissue is greatly increased without increasing its blood concentration, and the curative effect of the drug is effectively improved.