Ligusticum sinense, also named Fuxiong, is one of the specialty Chinese medicinal herbs in Jiujiang, Jiangxi Province. It is the dried rhizome of L. sinense, a plant belonging to the Umbelliferae family and the Ligusticum genus. It has the effects of moving qi and activating blood, expelling wind and relieving pain. As a traditional Chinese medicine that can be used as both medicine and food, the phthalein in L. sinense has various pharmacological effects, and it’s excellent anti-cerebral ischemic stroke (CIS) effect has received increasing attention in recent years. Modern research has shown that phthalides compounds in L. sinense can alleviate the treatment of CIS by inhibiting neuronal inflammation response, regulation neuronal excitotoxicity, protecting the blood-brain barrier, reducing neuronal oxidative stress, inhibiting neruonal apoptosis and autophagy, and dilating blood vessels, etc. It is a multipathway treatment for CIS. Understanding the mechanism of action and pharmacokinetic characteristics of the active ingredients of L. sinense against cerebral ischemic stroke in vitro and in vivo can better guide its clinical medication safety standards and formulation development. This article systematically summarizes the composition and pharmacological mechanism of the phthalide components in L. sinense and their anti CIS effects, as well as pharmacokinetic studies, by reviewing domestic and foreign literature. The aim is to provide a reference for further research and new drug development of L. sinense in the treatment of CIS.