OBJECTIVE： To discuss clinical efficacy and safety of alteplase combined with butylphthalide to the patients with acute ischemic stroke. METHODS：  98 patients with acute ischemic stroke in our hospital were selected and divided into observation group and control group according to random number table， with 49 patients in each group. Control group was additionally given Butylphthalide and sodium chloride injection 100 ml， ivgtt，bid， on the basis of routine treatment as controlling blood glucose， blood pressure， etc.； observation group additionally received Alteplase for injection 5 mg added into NS 10 ml， iv+ Alteplase for injection 45 mg added into NS 100 ml， ivgtt， qd， on the basis of control group. Both groups were treated for 2 weeks. Clinical efficacies of 2 groups were compared as well as cerebral infarction area， NIHSS score， ability score of daily living， the levels of IL-6， IL-8， IL-10， CRP， 24 h urine protein， Scr and creatinine clearance rate before and after treatment. The occurrence of ADR was also recorded. RESULTS： 1 patient of observation group and 2 patients of control group withdrew from the study due to severe hemorrhage.  Total effective rate of observation group （95.83％） was significantly higher than that of control group （80.85％）， with statistical significance （P＜0.05）. Before treatment， there was no statistical significance in above indexes between 2 groups （P＞0.05）. The cerebral infarction area and NIHSS score were reduced significantly in observation group after treatment， ability score of daily living were increased significantly in observation group after treatment， and the improvement of  observation group was significantly better than control group， with statistical significance （P＜0.05）. 24 h urine protein and Scr of observation group was significantly lower than those of control group， with statistical significance （P＜0.05）. the level of IL-6 in observation group 1 week after treatment and the levels of IL-6， IL-8， IL-10 and CRP 2 weeks after treatment were significantly lower than in control group， with statistical significance （P＜0.05）. There was no statistical significance in the incidence of ADR between 2 groups （P＞0.05）. CONCLUSIONS： Alteplase combined with butylphthalide show significant therapeutic efficacy， can effectively reduce the level of serum inflammatory factors， control brain tissue ischemia and cerebral infarction area， and improve neurologic function and protect renal function in patients with acute ischemic stroke.