Objective To assess the effects and safety of Tongxinluo (TXL) Capsule for patients with acute ischemic stroke. Methods PubMed (1966 to 2011.12.23), EMbase (1966 to 2011.12.23), Ovid CENTRAL (2011.10), CBM (1978 to 2011.12.23), VIP (1989 to 2011.12.23), CNKI (1980 to 2011.12.23), CDFD (1999 to 2011.12.23), and CDFD (1999 to 2011.12.23) were electronically searched for randomized controlled trials (RCTs) on TXL Capsule for patients with acute ischemic stroke. Meanwhile, relevant data were retrieved by hand search and data from pharmaceutical factories were collected. Two reviewers independently screened literature, extracted data, and assessed the methodological quality. Then, meta-analysis was performed using RevMan 5.1 software. Results Thirty nine RCTs (non-placebo-controlled trials) involving 3 906 patients were included. The quality of the included studies was generally low. The follow-up time started from the end of treatment (minimum: 7 days) to 6 months. The result of meta-analysis (16 trials, 1 445 patients) showed that the TXL group was better than the control group in improving neurological function (SMD= −1.09, 95%CI −1.68 to −0.49). The result of meta-analysis (21 trials, 2 500 patients) showed that, the effectiveness rate (91.3%) of the TXL group was significantly higher than that of the control group (RR=1.22, 95%CI 1.14 to 1.30). Eight trials reported adverse reactions such as nausea and gastric discomfort. Four trials reported that 5 patients in the control group died during the treatment. No studies reported the data of mortality, dependency rate during 3-month follow up, or quality of life. Conclusion Current studies show that, TXL Capsule improves neurological impairment of patients with acute ischemic stroke which has less adverse reactions. Further studies are still needed to verify the effects of TXL on long-term mortality and disability. It is necessary to conduct more high quality RCTs especially with placebo-controlled trials to confirm the efficacy of Tongxinluo for acute ischemic stroke.