Nelarabine injection

Abstract

The invention relates to a nelarabine injection, which is characterized by consisting of nelarabine, EDTA or EDTA salt, sodium chloride, and water for injection, wherein the nelarabine accounts for 0.25 to 0.625 percent of the total weight of the injection, the EDTA or the EDTA salt accounts for 0.001 to 0.01 percent of the total weight of the injection, the content of the sodium chloride is 0 or the dose is used for regulating the osmotic pressure, and the balance is the water for injection. The preparing process comprises the following steps: taking 80 percent of the water for injection, adding raw supplementary materials into the water for injection, stirring the mixture to fully dissolve the raw supplementary materials and mixing the mixture evenly, adjusting the pH value, adding 0.02 percent of needle activated carbon into the mixture, keeping the water temperature at 70 DEG C, stirring the mixture for 30 minutes, filtering the mixture to remove the activated carbon when the mixture is hot, cooling the mixture to room temperature, measuring the contents and the pH value of the solution, adding the water for injection with full dose into the solution, mixing the mixture evenly, filtering the mixture through 0.22 mu m of microfiltration membrane until the mixture is clear, packaging the filtrate into infusion bottles after intermediates are measured to be qualified, plugging the bottles, and rolling the mouths of the bottoms to obtain the nelarabine injection after hot pressing sterilization.

Description

technical field [0001] What the present invention relates to is a kind of nelarabine injection, can be used as T-cell acute lymphoblastic leukemia (T-ALL) and T-cell lymphoblastic lymphoma (T-ALL) that relapse after at least two treatment schemes are ineffective or treated. LBL) therapeutic drugs. Background technique [0002] Leukemia, especially acute lymphoblastic leukemia (ALL) has become one of the most common malignant tumors in children and adolescents. Approximately 2,400 children and 1,200 adults are diagnosed with ALL each year in the United States, of whom approximately 720 develop T-cell acute lymphoblastic leukemia (T-ALL). Although the cure rate of children suffering from ALL in developed countries has reached about 80% in the past 10 years, there are still about 250 cases of patients who do not respond to drugs or relapse every year and are difficult to cure. Adults with T-ALL are more likely to develop drug resistance than children, and their 5-year event-f...

AI Technical Summary

Problems solved by technology

In the 1960s, the deoxyguanylic acid analogue 9-β-D-arabinofurano-syl-guanine (ara-G) was discovered, which was not used clinically due to poor solubility

[0006] It has been found through research that nelarabine is basically stable under conditions of light (4500Lx±500Lx), high temperature (40°C, 60°C) and high humidity (25°C RH75%, 25°C RH92.5%), and is stable under oxidation (10% over Hydrogen oxide, heated in a water bath for 1 hour), acid (1.0 mol / L hydrochloric acid, heated in a boiling water bath for 1 hour) and alkali (1.0 mol / L sodium hydroxide solution, heated in a boiling water bath for 1 hour) have a certain degree of damage. The aqueous solution cannot withstand high temperature sterilization, and the use of higher sterilization temperature will lead to the degradation of nelarabine, resulting in degradation products (impurities) that may cause toxic and side effects

Therefore, ordinary preparations generally adopt the sterilization scheme of adding antioxidants and F0 value control, but nelarabine still has a certain degree of degradation, and its sterility assurance level is not as good as the high sterilization temperature sufficient sterilization scheme, which is of great concern to clinical practice. Safe drug use poses hidden dangers

Existing known technology also does not improve the suggestion of above defective

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