Abstract: Objective To evaluate the clinical efficacy of the argatroban in the treatment of acute cerebral infarction (ACI). Methods Total 52 cases of ACI in our hospital from June 2014 to June 2016 were enrolled and randomly divided into two groups with 26 cases in each group. The conventional drugs (bayaspirin, atorvastatin, safflower Injection and deproteinized hemoderivative of calf blood) were administrated in the control group, and additional argatroban (60 mg/day, continuous pump for 48 hours; then 10 mg/time, bid, pump for 5 days). The levels of lactic acid, hs-CRP, TNF-α and IL-6 were tested, and National institutes of health stroke scale(NIHSS) score and BI scale were conducted to evaluated the therapeutic efficacy at different time points. Results In the treatment group, NIHSS score decreased significantly, however, BI score increased significantly on d10 after the treatment, there were statistically difference when compared with the control group (P<0.05). There was no significant difference in the levels of lactic acid, hs-CRP, TNF-α and IL-6 before the treatment between the two groups (P>0.05). On 48 h and 7 d time points, these levels in the treatment group was significantly lower than that of the control group, there was significant difference between the two groups (P<0.05). The serum APTT on each time points were significantly different between the two groups (P<0.01), but there was no significant difference on 10 d after the treatment (P>0.05). Conclusion Argatroban can effectively improve the blood supply of brain tissue, relieve tissue hypoxia, reduce the release of inflammatory mediators, and improve survival. As one good choice for the ACI patients, the curative effect of argatroban is significant.