Neratinib sustained-release implant for treating solid tumor

Abstract

A sustained release implant includes 0.1%-50% (w / w) nilotinib, 50-99% sustained release excipients and 0-15% sustained release moderator. Sustained release excipients are mainly one or combination of poly (L-lactide-co-ethyl phosphate), poly (L-lactide-co- phosphoric acid propyl), polylactic acid, the copolymer of polylactic acid and hydroxyacetic acid and polifeprosan; sustained release moderator is one or combination of mannitol, sorbic alcohol and chondroitin; sustained release implant applied in local tumor can slowly release nilotinib onto local tumor, thus maintaining effective drug concentration of local tumor as well as significantly reducing overall toxic reaction; the invention not only reduces overall toxic reaction of nilotinib, but also selectively improves drug concentration in local tumor, enhancing the therapeutic effects of non-operative therapy such as chemotherapy drugs and radiotherapy. The implant can be used for treating solid tumors including lung cancer, esophageal carcinoma, gastric cancer, liver cancer, breast cancer, ovarian cancer, prostatic carcinoma, pancreatic cancer, bladder carcinoma, cerebroma, and colorectal cancer.

Description

(1) Technical field [0001] The invention relates to a niratinib slow-release implant for treating solid tumors, belonging to the technical field of medicines. (2) Background technology [0002] The latest data show that in 2006, 3 million people died of cancer in China. The incidence of cancer is increasing year by year and tends to be younger. Statistics show that in less than 20 years, the incidence of cancer in my country has increased by 69%, and the mortality rate has increased by 29.4%. According to the latest statistics from the World Health Organization, the global cancer incidence rate will increase by 50% by 2020, and the number of patients will increase to 15 million. It is estimated that 4 million people will die of cancer every year in my country in 2020. Therefore, exploring an effective method or drug for treating cancer has become a hot research topic at present. [0003] At present, there are many drugs for the treatment of tumors. However, many drugs have...

AI Technical Summary

Problems solved by technology

Systemic administration is difficult to obtain effective drug concentration at the tumor site, and simply increasing the administration concentration is limited by systemic reactions

[0004] The latest research shows that tyrosine kinases play an increasingly important role in the development of tumors, and Niratinib (Neratinib: (2E)-N-[4-({3-chloro-4-[( pyridin-2-yl)methoxy]phenyl}amino)-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)but-2-enamide, (2E)-N-[4-[[3- Chloro-4-[(pyridin-2-yl)methoxy]phenyl]amino]-3-cyano-7-ethoxyquinolin-6-yl]-4-(dimethylamino)butyl- 2-enamide) is the most potential tyrosine kinase inhibitor to show inhibition of tumor blood vessels, but the effect of this drug alone in the treatment of other solid tumors is unclear

Although the combination with other anticancer drugs such as paclitaxel may have a certain effect on lung cancer and other tumors, the systemic side effects caused by conventional administration limit its clinical application