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To clarify the active components of Wuzhuyu-tang, this study analyzed dynamic changes of 10 ingredients of Wuzhuyu-tang in plasma using combination high performance liquid chromatography-mass spectrometry after oral administration in rats. The results showed that seven ingredients were detected in portal vein plasma after oral administration of 16.3 or 8.15 g/kg equivalent of raw material of Wuzhuyu-tang extract. The absorption rate of limonin, evodiamine, gingerol (6-Gi), and ginsenoside-Rg1 was greater than that of isorhamnetin-3-O-β-D-glucosyl (6″→1″′)-α-L-rhamnoside, ginsenoside-Rb1 (Rb1), and ginsenoside-Re (Re). The time most elements were absorbed into the blood was 30 to 60 minutes after administration. Re, 6-Gi and Rb1 were metabolized faster. The results suggest that the seven ingredients described above are the active components for treating migraines.