A 5±-androstane-3²,5,6²-triol injection and its preparation are disclosed. The injection uses hydroxypropyl-²-cyclodextrin as a solubilizing agent and the active ingredient is present in a part by weight ratio of 1-20:40-500 to the hydroxypropyl-²-cyclodextrin. The injection may also comprise 1ˆ¼100 parts of an isotonic adjusting agent, 0ˆ¼200 parts of a freeze drying filler, and 0ˆ¼2000 parts of a solvent. The preparation method comprises dissolving hydroxypropyl-²-cyclodextrin solution, 5±-androstane-3²,5,6²-triol and soluble excipients in water for injection in sequence to obtain a raw injection solution, and subjecting the raw injection solution to decolorization, depyrogenation, filtration and sterilization to obtain the injection. Drying the filtrate yields a solid for injection.
