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Ai pian, derived from Blumea balsamifera (L.) DC. has various medicinal effects and a complex composition. The goal of this study was to analyze the chemical composition of Ai pian by using samples from different regions to explore differences between the chemical composition and its blood composition from treated mice to clarify whether its efficacy is related to synergism of multiple components to provide references for rational quality control. Gas chromatography – mass spectrometry (GC-MS) was used to determine and compare chemical compositions of blank and Ai pian containing serum of mice after 30 min of oral administration of Ai pian of seven batches from Zhenfeng, Wangmo and Luodian Counties; Guizhou Province; and Tian'e County; and Guangxi Province. Sixteen to twenty-two compounds of Ai pian were identified, with fourteen common compounds including L-borneol, L-camphor, borneol acetate, L-linalool, α-gurjunene, and 3-t-butyl-1, 2-dimethoxybenzene. Four to seven compounds were identified as blood components of Ai pian, and L-borneol, L-camphor, and borneol acetate were common prototypes with relative compositions from 13.720 to 36.509%, 2.336 to 5.219%, and 0.401 to 1.188%, respectively. Methyl oleate was a common metabolic component with a relative concentration of 0.021 to 0.446%. The chemical composition and blood components of Ai pian were complex, and its efficacy was related to synergism between several components including L-borneol, L-camphor, and borneol acetate. Therefore, detecting multiple index components of Ai pian is essential for quality control. [ABSTRACT FROM AUTHOR]