The invention relates to a preparation method and applications of an active matter capable of efficiently removing chloasma. The preparation method and applications are characterized in that the preparation method includes the following steps: A, drying fresh folium artemisiae argyi to add into a round-bottom flask with deionized water, adjusting pH to 2.0-3.0 with concentrated hydrochloric acid,performing heating extraction through a water bath, receiving folium artemisiae argyi essential oil with a taper flask at the liquid outlet of a condensing tube, performing water bath extraction on the first filtered residue under the environment where the pH is 6.5-7.0, and performing water bath extraction on the second filtered residue under the environment where the pH is 8.2-8.6; B, pooling the first filtrate, the second filtrate and the third filtrate after filtration so as to obtain a folium artemisiae argyi extracting solution; C, performing reduced pressure distillation and concentration on the folium artemisiae argyi extracting solution to obtain folium artemisiae argyi extract, taking a proper amount of the extract to add into an ethanol/ammonium sulfate aqueous two-phase system,adjusting the pH to 3-4 with the concentrated hydrochloric acid, performing full shaking, then allowing the solution to stand, collecting an ethanol phase at the upper layer, and obtaining folium artemisiae argyi flavonoids through vacuum concentration; and D, mixing the folium artemisiae argyi essential oil and the folium artemisiae argyi flavonoids so as to obtain the active matter capable of efficiently removing chloasma. The obtained active matter has good effects on improving the chloasma.