The tissue distribution profile of danshensu, one of the bioactive components in Radix salviae miltiorrhiae, was investigated after oral administration of Radix salviae miltiorrhiae coupled with Radix curcumae in rabbits. Eighteen rabbits were evenly divided into 3 groups. Rabbits of the groups were orally administrated with carboxymethyl cellulose, Radix salviae miltiorrhiae (10.0 g/kg) and Radix salviae miltiorrhiae (10.0 g/kg) coupled with Radix curcumae (5.0 g/kg), respectively. High performance liquid chromatography-electrospray ionic trap mass spectrometry (HPLC-ESI-MS(n)) was used for the determination of danshensu in the tissues including heart, liver, kidney and brain. The statistical results demonstrated that the characteristic profiles of danshensu were c(kidney) > c(heart) > c(liver) > c(brain) and c(kidney) > c(brain) > c(liver) > c(heart) after administration of Radix salviae miltiorrhiae and Radix salviae miltiorrhiae coupled with Radix curcumae, respectively, indicating that Radix curcumae could obviously increase the concentration of danshensu in brain. This result would provide substantial foundation for the harmonizing effect of shi herb in a Chinese compound prescription.