Deoxyuridine powder injection and its preparing method

Abstract

A process for an injection from frozen powder of doxifluridine applying to mainline and its preparation method, said injection comprise 5 parts of doxifluridine, 0.1-100 parts of excipient or 0.1-100 parts of cyclodextrin.; said product can be dissolved quickly when meeting water and convenient for clinical use.

Description

technical field

[0001] The invention relates to doxifluridine powder injection and a preparation method thereof, in particular to doxifluridine freeze-dried powder injection suitable for infusion and a preparation method thereof. technical background

[0002] Doxifluridine (5'-DFUR) is a nontoxic prodrug of 5-fluorouracil (5-FU). It is an anti-tumor drug developed by the American branch of Roche in the 1970s, and its trade name is Furtulon. It was first put into the market in Japan in the 1990s. In the past, the fluorinated pyrimidine series drugs were mainly enzymatically or naturally hydrolyzed into 5-FU by liver drug enzymes after oral administration. In contrast, Fluferolone can be converted into 5-FU by pyrimidine nucleoside phosphorylase (PyNPase), which shows high activity in tumor tissue. Because the enzyme is high in breast cancer, gastric cancer, colon cancer and other solid tumors, 5'-DFUR is preferentially activated in the tumor site, and the drug concentratio...