Abstract: AimTo investigate the chemical constituents of the Tibetan herbal medicine Halenia elliptica by guidance of in vivo absorption and distribution of the constituents. MethodsHPLC with a diode array detector (DAD) and HPLC-MS were used for detecting the constituents of extracts of Halenia elliptica and animal samples. Several kinds of column chromatography were used for the isolation and purification of the main in vivo absorbed and distributed compounds from the extract of Halenia elliptica. ResultsSix main components detected in the extracts of the animal samples were isolated from the ethanolic extract of Halenia elliptica. ConclusionAfter rats were treated with different extracts of Halenia elliptica, low polar components xanthone aglycon of Halenia elliptica were clearly observed in the extracts of liver, lipid, blood, hidney, heart and brain tissue of rats, while the polar components xanthone glycosides were detected in very small amounts in the animal samples. The xanthone glycosides can be decomposed into xanthone aglycons during the digestion, absorption and metabolism procedure. Therefore, the in vivo activity of the xanthone glycosides might be exhibited by their decomposed products. It is an accessibly valuable method to investigate chemical components of herbal medicines under the guidance by detecting in vivo absorption and distribution of chemical components of the herbal medicine extract.