Although brain malignant tumors are treated by surgical resection, radiotherapy and intravenous chemotherapy, their average survival period still does not exceed 16 months. The efficacy of intravenous systemic chemotherapy is affected by the dose limitation due to the large systemic toxic side effects, while internal carotid artery infusion chemotherapy can infuse the effective concentration of drugs into intracranial tumor tissues, reduce the systemic toxic reactions, prolong the retention time of chemotherapeutic drugs in the tumor, and effectively exert the killing effect of chemotherapeutic drugs on tumor cells. Animal experiments showed that the drug concentration in tumor tissues was measured by applying carbon-14-labeled nintedan, respectively, under two conditions of perfusion via internal carotid artery and intravenous injection, and found that the former was 5 times higher than the latter at 1 min after perfusion; the former was 1.5-2 times higher than the latter at 30 min after perfusion. Pharmacokinetic tests revealed that the drug content in tumor tissues was 3.8 times higher 1 min after perfusion via the internal carotid artery than that via intravenous injection, and increased to 18 times after 15 min. The drug content in the brain tissue of the cerebral hemisphere on the perfusion side was 2.5 times higher when administered via internal carotid artery perfusion than via intravenous infusion. However, in the brain tissue of cerebral hemisphere, the highest value of drug content was 20.16 nmol/g when administered via internal carotid artery perfusion, while the tumor tissue was 271.51 nmol/g. This indicates that the chemotherapeutic drugs can be effectively concentrated in the tumor tissue and exert the maximum chemotherapeutic effect when administered via internal carotid artery perfusion.