Abstract: A 5?-androstane-3?,5,6?-triol injection and its preparation are disclosed. The injection uses hydroxypropyl-?-cyclodextrin as a solubilizing agent and the active ingredient is present at a weight ratio of 1-20:40-500 to the hydroxypropyl-?-cyclodextrin. The injection may also comprise, by weight, 1-100 parts of at least one isotonic adjusting agent, 0-200 parts of at least one freeze drying filler, and 0-2000 parts of at least one solvent. The preparation method comprises dissolving hydroxypropyl-?-cyclodextrin solution, 5?-androstane-3?,5,6?-triol and at least one additional soluble excipient 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.

Abstract: Disclosed is the use of 5?-androstane(alkyl)-3?,5,6?-triol in preparing neuroprotective drugs. The compound has significant protective effect against neuron injuries caused by cerebral ischemia, spinal cord isehemia or hypoxia and has no obvious toxic reaction within effective dose thereof.