Fuzi, the processed lateral roots of Aconitum carmichaeli (Ranunculaceae family), is a widely used traditional Chinese medicinal herb due to their excellent pharmacological activities including anti-inflammation, analgesics, local anesthesia, and anti-tumor effect. Since there have been reports of adverse events, even toxic events of Fuzi, many pharmacokinetic studies were conducted to research Fuzi extract and its active ingredients. Present paper summarized progress of the researches.