Abstract: Pharmacokinetic behavior of orally administrated formulations involves dissolution and absorption in the gastrointestinal tract (GIT), which is required for the systemic effects of a drug. The dissolution and subsequent penetration through the intestinal epithelia is a vital step toward in vivo bioavailability. A lot of effort has been devoted to the study of physiological characteristics of GIT by means of in vitro dissolution methods or in vitro permeation methods. Moreover, drug dissolution/permeation synchronous evaluation technology could be employed to predict the process of drug dissolution and absorption by the combination of dissolution apparatus and permeation apparatus. Better prediction tools are priority in the critical path initiative of US Food and Drug Administration. The studies and applications of the drug dissolution/permeation synchronous evaluation technology are attracting more and more attention each year. However, there is no systematic review on the theoretical basis and the recent development. Therefore, in this review, we will give an overview on the physiological basis and theoretical basis of the drug dissolution/permeation synchronous evaluation technology, as well as their recent advances of this kind of equipments at home and abroad. Moreover, we have also compared their advantages and disadvantages, and the applicable scopes. With hope that the critical path study will promote the development of innovative drug research and development, and improve the druggability.