The present invention relates to the field of biological medicine, and specifically relates to a composition comprising an M10C1 compound and an active ingredient, and a preparation method thereof. The active ingredient is siRNA, and calculated in parts by weight, the composition comprises 1-5 parts siRNA, 1-24 parts of the M10C1 compound, and 1-10 parts of cholesterol-polyethylene glycol. The composition of the present invention, which comprises an M10C1 compound and siRNA, can improve pharmacokinetic characteristics of siRNA treatment, change biological distribution, intracellular uptake, targeting and delivery efficiency, reduce adverse reactions, etc.
