Abstract: The pharmacokinetic parameters of aristolochic acid-I (AA-I) and -II (AA-II) in rat serum after intragastrical administration of the crude drug powders of Radix Aristolochiae (RA) and Muskone containing equal amounts of RA were compared. The pharmacokinetic profiles of AA-I and AA-II could be fitted with a two-compartment model. The elimination half time (T1/2β) of AA-I in Muskone was 1573.2 min and that of AA-I in RA was 475.8 min; T1/2β of AA-II in Muskone was 2344.8 min and that of AA-II in RA was 427.8 min. The area under the concentration-time curve (AUC) of AA-I in Muskone was 13.07 μg/h/mL and that of AA-I in RA was 3.86 μg/h/mL; AUC of AA-II in Muskone was 67.67 μg/h/mL and that of AA-II in RA was 23.93 μg/h/mL. The bioavailabilities of AA-I and AA-II in Muskone were markedly increased compared with that in RA based on the elimination half-time and AUC values.

Key words: Aristolochiae Radix, Aristolochiae Radix, Muskone, Muskone, Aristolochic acid-I, Aristolochic acid-I, Aristolochic acid-II, Aristolochic acid-II, Pharmacokinetics, Pharmacokinetics