Aim: To establish the metabolic fingerprint and profile of bioactive components in human plasma after sublingual administration of compound Danshen dripping pills. Methods: Human plasma samples were collected at different time intervals. Powerlab tension system was used to measure their ability of expanding blood vessel and column switching system was employed to purify and enrich the components of interest. Results: The plasma sample of 1.5h had the strongest ability for expanding blood vessel, and had five new peaks in the chromatogram. Conclusion: After being identified, the intensity ratio of these 5 peaks was calculated. The diagram called metabolic profile was established to link bioactive compounds with pharmacodynamic action.