Abstract: OBJECTIVE To establish a LC-MS/MS analytical method for simultaneous determination of tacrolimus and five compounds of Wuzhi capsule in liver transplant recipients’ whole blood and to study the pharmacokinetic characteristic of the analytes in liver transplant patients. METHODS The zinc sulfate was added to whole blood to lyse the blood cells, and then the sample was deposited by methanol. The upper layer was injected into the LC-MS/MS. Then a LC-MS/MS method was established for the determination of tacrolimus, schisandrin, schisandrol B, schisantherin A, deoxyshisandrin and schisanhenol. RESULTS The calibration curve of six compounds showed a good linear relationship. The intra and inter day precisions and accuracy met the requirements and the extraction recovery was all right. CONCLUSION This method is accurate, precise, sensitive and specific to be suitable for concentration of therapeutic drug monitoring and pharmacokinetic study of tacrolimus, schisandrin, schisandrol B, schisantherin A, deoxyshisandrin and schisanhenol.