Valproic acid is a first-line broad-spectrum antiepileptic drug, however, the pharmacokinetics of valproic acid are affected by many factors, such as heredity, drug combination and so on. So, how to realize the individualized dosing regimen of valproic acid has received much attention. Population pharmacokinetics combines classical pharmacokinetic principles and population statistical models to quantitatively evaluate the influence factor of drug concentration in the patient population. Thus, it can optimize characterization of the differences among individuals. This article reviews the researches about valproic acid in recent years, and summarizes the effect of the factors on the metabolism of valproic acid, such as drug combination and gene polymorphism. Additionally, focus on the latest research progress of individual administration of valproic acid under the guidance of population pharmacokinetics.