The invention relates to a triptolide compound composition as well as a preparation method and application thereof, and belongs to the technical field of medicines. The triptolide compound compositionhas an obvious effect-enhancing and toxicity-reducing effect. The triptolide compound composition is prepared from triptolide, an ammonium glycyrrhizinate phospholipid compound, an emulsifier, oil, awater-soluble stabilizer, a fat-soluble stabilizer, glycerol, a co-emulsifier and water according to the following ratio, by weight percentage, 0.01%-0.02% of triptolide, 0.1%-0.9% of the ammonium glycyrrhizinate phospholipid complex, 5%-15% of oil, 0.9%-2.7% of the emulsifier, 0.3%-0.9% of the fat-soluble stabilizer, 2.5% of glycerol, 0.05%-0.1% of the co-emulsifier, 0%-0.2% of the water-solublestabilizer and the balance of water. The triptolide and the ammonium glycyrrhizinate are matched for use, the ammonium glycyrrhizinate is used for protecting cells such as livers and kidneys of organisms from being damaged by the triptolide, and the phospholipid complex prepared from the special structure of the ammonium glycyrrhizinate is high in lipophilicity, high in bioavailability and high in preparation stability, so that the treatment effect is improved.