Pharmacokinetic characters of rhynchophylline (RIN), gastrodin (GAS), and gastrodigenin (p-hydroxybenzyl alcohol, HBA) were investigated after oral administration of different prescriptions ofYizhi:Yizhitablets or effective parts oftianma(total saponins from Gastrodiae, EPT) andgouteng(rhynchophylla alkaloids, EPG). At different predetermined time points after administration, the concentrations of GAS, HBA, and RIN in rat plasma were determined by an HPLC-ESI/MS method, and the main pharmacokinetic parameters were investigated. The results showed that the pharmacokinetic parametersCmaxandCmaxandAUC0–∞(P<0.05) were dramatically different after oral administration of different prescriptions ofYizhi. The data indicated that the pharmacokinetic processes of GAS, HBA, and RIN in rats would interact with each other or be affected by other components inYizhi. The rationality of the compatibility ofUncariaandGastrodia elataas a classic “herb pair” has been verified from the pharmacokinetic viewpoint.