Abstract: Herb and drug combination has become a common phenomenon on the clinical treatment, but its judgement criteria lacks a complete scientific basis. Traditional pharmacokinetic studies, restricted to plasma drug concentration, cannot clarify drug metabolism and disposition process in the target site, creating limitations such as irrelevant relationship between plasma PK and PD. In recent years, more and more studies focus on quantitative analysis of the process of drugs into the target area and cells through blood, which promotes pharmacokinetic researches from "macro" plasma into "micro" cells. Therefore, this paper mainly summarizes new technologies, new methods of herb-drug interaction researches based on the thought of cellular pharmacokinetics, as well as studies and clinical applications of herb-drug combination to improve effect and decrease toxicity.