The invention discloses a benflumetol fat emulsion injection preparation which contains 0.03 to 35 wt% of benflumetol, 10.0 to 30.0 wt% of oil for injection, 0.6 to 30.0 wt% of an emulsifier, 0 to 10 wt% of a solubilizer, 0 to 5 wt% of a co-emulsifier, 2.25 to 7 wt% of an isotonic agent and 0.002 to 0.075 wt% of an anti-oxidant, with the balance being injection water. The invention also discloses a preparation method and pharmacodynamic and safety evaluation for the benflumetol fat emulsion injection preparation. The benflumetol fat emulsion provided by the invention has the characteristics of good biocompatibility, high physical stability, convenient preparation, good security, high drug loading capacity and the like, has a particle size of less than 200 mu m and is suitable for injection, e.g, intravenous injection and intramuscular injection. According to the invention, the characteristic that a soybean oil fat emulsion inhibits growth of plasmodium falciparum is utilized to enhance anti-malarial effects of drugs, to improve bioavailability of the drugs and to reduce toxic and side effects of the drugs; nutrients needed by the body of a patient with malaria can be provided, the activity of lymphocytes of the patient is improved, which assists the patient in resisting malaria and recovering.