The present invention discloses a preparation and application of flavonol as a brain-targeting synergist. After long-term repeated studies, the inventors have found that some flavonol compounds, particularly kaempferide, rutin, troxerutin, myricetin, hesperidin, and hydroxy derivatives thereof, in particular their glycoside, ester, ether derivatives, can promote the drug molecules that have therapeutic or healthcare effect, such as ginsenoside, stilbene glucoside, resveratrol, levodopa, edaravone, vinpocetine, nicergoline, citicoline, oxiracetam, to enter brain tissues, to dramatically enhance drugs concentrations in the brain tissues and effective enhance the efficacy of drugs without increasing the plasma concentration.
