OBJECTIVE: To compare therapecttic efficacy and safety of rosuvastation for patients with acute cerebral infarction (ACI) before and after the application of intravenous thrombolysis. METHODS: A total of 90 ACI patients receiving intravenous thrombolysis selected from Hainan Provincial People’s Hospital during Jan. 2014-Oct. 2016 were divided into pre-thrombolytic group (45 cases) and post-thrombolytic group (45 cases) according to random number table. Both were given rosuvastation (10 mg,qd) orally within 24 h before and after intravenous thrombolysis for 8 weeks. The rate of excellent prognosis were compared between 2 groups, and NIHSS score, ADL-Barthel index score, the levels of laboratory indexes (HMGB1, MMP-9, IL-17), the incidence of intracranial hemorrhage and the occurrence of ADR were compared before and after treatment. RESULTS: The rate of excellent prognosis in pre-thrombolytic group one and eight weeks after thrombolysis was significantly higher than post-thrombolytic group. NIHSS score, ADL-Barthel index score, the levels of HMGB1, MMP-9 and IL-17 in 2 groups after treatment were significantly better than before treatment; the pre-thrombolytic group were significantly better than the post-thrombolytic group, with statistical significance (P<0.05). There was no significant difference in the incidence of intracranial hemorrhage between 2 groups(P>0.05), and no obvious ADR was found. CONCLUSIONS: Compared with post-thrombolytic medication, rosuvastation used before intravenous thrombolysis can significantly improve long-term prognosis, promote the recovery of neurological function and quality of daily life and reduce the levels of HMGB1, MMP-9 and IL-17, but does not increase the risk of intracranial hemorrhage with good safety.