OBJECTIVE To study the analysis method of mycophenolic acid in human plasma and to establish the standard procedure of therapeutic drug monitoring (TDM).METHODS The concentration of mycophenolic acid in the human plasma was determined by the high-performance liquid chromatography (HPLC).The internal standardization with correction factor and the standard curve method were compared.The date of drug concentration in patients were analyzed and the distribution in patients of steady state was observed.RESULTS High-performance liquid chromatography analysis technique was accurate and reliable.The internal standardization with correction factor showed no difference from the standard curve method,the concentration of mycophenolic acid in human was influenced by the combination therapy and significant variability was obtained among patients.CONCLUSION This standard procedure includs the fast and accurate analysis method and quality control method.The effective concentration of therapeutic drug monitoring (TDM) is still discussed.