Abstract: To optimize the alcohol extraction process of Platycodon grandiflorum by response surface methodology, then investigate its whitening activity. With extracting time, extracting times and solvent volumn as factors, the ethanol extraction process of Platycodon grandiflorum was optimized by single factor investigation and Box-Behnken response surface design. The optimal ethanol extracting technology was 8 times of solvent, extraction for 3 times, 1 h each time. The extraction rates of platycodon D, arbutin, and total saponins in the ethanol extract were 0.122%±0.003%, 0.128%±0.005%, and 0.582%±0.007%, respectively, and the extract had good tyrosinase inhibition activity (92.39%), hyaluronidase inhibition activity (88.26%), cell melanin inhibition effect, and DPPH· (90.19%), ABTS⁺ (80.57%) free radical scavenging activity. The optimal ethanol extraction process of Platycodon grandiflorum was stable, reliable and operable. The ethanol extract had good whitening and antioxidant activity, which would provide scientific basis for further research on biological activity and whitening mechanism of Platycodon grandiflorum.