Abstract: AIM　To study the metabolism of perlolyrine, an active ingredient from the traditional Chinese herb, Chuanxiong, Ligusticum wallichii Franch in rats. METHODS　After oral administration of perlolyrine and ［2-¹⁵N］ perlolyrine, the rat urine samples were hydrolyzed with glucuronidase, alkalinized with NaHCO₃-Na₂CO₃ and extracted with ethyl ether-isopropyl alcohol. The organic phases (neutral and basic fraction) were concentrated for TMS derivatization. The aqueous phase was acidified with sulfuric acid, taken to dryness and extracted with methanol (water soluble acidic fractions) and concentrated for TMS derivatization. The TMS derivatives were determined by GC-MS. RESULTS　Perlolyrine and one metabolite were found from the neutral and basic fraction, and two different metabolites were found from the water soluble acid fraction. CONCLUSION　It was proposed that the major metabolic pathways of perlolyrine were the hydroxylation of perlolyrine and the oxidation of its hydroxylmethyl group.