The present invention discloses a glycyrrhetinic acid composition, which is characterized by comprising 18alpha-glycyrrhetinic acid and 18beta-glycyrrhetinic acid according to a molar mass ratio of (2-15):1, wherein the treatment effect of the glycyrrhetinic acid composition is significantly superior to the treatment effect of the single glycyrrhetinic acid component, and the effect is significant under the equivalent medication dose in the effective dose range. The present invention further discloses applications of the glycyrrhetinic acid composition in preparation of cancer treatment drugs. According to the present invention, with the application of the glycyrrhetinic acid composition in cancer treatment, the total dose of the medication is reduced so as to reduce the harmful effect caused by the toxic-side effect, and the composition of the present invention sufficiently applies the characteristics of the components with different configurations so as to provide basis for the wide and effective application of the glycyrrhetinic acid. In addition, the preparation method of the present invention has characteristics of simpleness, low cost, and no environmental pollution.