Objectives : I analysed daehwangmokdan-tang's compatibility principle by the system of chief, deputy, assistant, and envoy and investigated pharmacological activities by categorizing with chemical components, molecular level, cellular level, animal level and human level based on Korean and Chinese studies for this formula. Methods : Daehwangmokdan-tang's compatibiltity principle was examined by the system of chief, deputy, assistant, and envoy. I looked into studies that presented in Korea from 1956 to 2016 about daehwangmokdan-tang through KOREA INSTITUTE OF ORIENTAL MEDICINE, Korean medicine information system (OASIS) and in Chinese for 20 years about daehwangmokdan-tang through China National Knowledge Infrastructure, CNKI. Then classify into chemical components, molecular level, cellular level, animal level and human level to analyse. Results : According to the system of chief, deputy, assistant, and envoy, chief herb is Rhei Radix et Rhizoma and Moutan Cortex, deputy herb is Natrii Sulfas and Persicae Semen, assistant and envoy herbs are Trichosanthis Semen. The amount of extraction of paeonol, total anthraquinone, and conjugated anthraquinone from daehwangmokdan-tang with the formulation of the system of chief, deputy, assistant, and envoy was the highest, and in the formulation of chief herb and deputy herb, the extraction amount of paeonol and conjugated anthraquinone was the lowest. With other formulations, the amount of extraction of total anthraquinone and conjugated anthraquinone was improved, although the degree was different. In particular, when it is blended with Persicae Semen as a deputy herb, the extraction amount of total anthraquinone and conjugated anthraquinone of Rhei Radix et Rhizoma as a chief herb is greatly increased, and the extraction amount of paeonol is rather different, but it is lowered. It was found that the amount of Mg Ca K Na in daehwangmokdan-tang was the highest. Pharmacological activities can be detected in inflammatory mediators and enzymes for molecular level. For cellular level, it can be determined in lipopolysaccharide (LPS)-stimulated RAW 264.7 cell line. In mouse and rats for animal level and human level, in inflammatory diseases (acute appendicitis, acute pancreatitis, acute cholecystitis, acute abdominal disease, ect.), pharmacological activities was caught. Conclusions : From the above results, daehwangmokdan-tang is composed in line with the system of chief, deputy, assistant, and envoy, suggesting that there is certain rationality and scientific. Pharmacological activities of daehwangmokdan-tang are effective to anti-inflammation, improvement of sepsis, analgesic, muscle relaxation, and improvement of intestinal flora and its metabolites. Daehwangmokdan-tang is consistent with the action of diuresis and anti-inflammation in terms of the content of elements, suggesting that there is action of purging fire and removing blood stasis, defecation detoxification, cooling blood and clearing heat and activating blood and dispersing stasis.