The invention discloses a brain-targeting prodrug with vitamin C as a carrier, which is a structure shown in the general formula (I) or a pharmaceutically acceptable salt or hydrate thereof, wherein X is -(CH2)n-, -C(O)-(CH2)n-C(O)- or -O-(CH2)m-, -NH-(CH2)m-, -C(O)-(CH2)m- or -NH-(CH2)m-C(O)-, n is 0- 6, and m is 1-4; Y is -(CH2)a-, -C(O)-(CH2)a-C(O)- or -O-(CH2)b-, -NH-(CH2)b-, -C(O)-(CH2)b-, -NH-(CH2)b-C(O)-, a is 0-6, and b is 1-4; and drug1 and Drug2 represent independent different or same drugs acting on the central nervous system. The invention provides a series of drugs, which can improve the brain targeting property of drugs and the central concentration of the drugs, thereby enhancing the curative effects of the drugs; and meanwhile, the distribution of drugs on peripheral organs is reduced, and the toxic or side effect of the drugs is reduced.