The invention relates to a formula of injection and powder prepared from catalpol and puerarin and a preparation method thereof. The formula is characterized by containing 0.05 to 30 grams of catalpol, 0.05 to 30 grams of puerarin, 1 to 100 grams of sulfobutyl ether-beta-cyclodextrin and / or hydroxypropyl-beta-cyclodextrin and 0 to 30 grams of isoosmotic adjusting agent. One or mixture of sodium chloride, glucose, cane sugar, sorbitol, mannitol, dextran and xylitol can be used as the isoosmotic adjusting agent. The invention aims to provide a Chinese medicinal effective ingredient compound injection preparation for treating cerebral ischemic diseases. The preparation can permeate the blood brain barrier, relieve the cerebral ischemic injury, improve ischemic and hypoxic tolerance of brain tissues, promote neogenesis and maturity of cerebral capillaries, protect neurovascular units, promote neuron axon and dendrite growth, enhance synaptic reconstruction, improve cerebral ischemic posterior nerve behaviors, improve the neural function score and promote affected limb motion function recovery.