Clofarabine injection and preparation method thereof

Abstract

The invention relates to a clofarabine injection, which is composed of: clofarabine 0.005-0.025g / mL, sodium chloride 0.045-0.12g / mL, and the rest are pH regulator and water for injection; the pH regulator regulates The pH of the injection is 6.0-6.5. The invention also relates to a preparation method of clofarabine injection. Compared with the prior art, the clofarabine injection involved in the present invention has the following advantages: (1) Compared with the existing clofarabine injection, the present invention increases the concentration of clofarabine by more than 5 times, greatly The volume of transfusion in clinical application is greatly reduced, the cost of medication is reduced, and the compliance of patients with medication is increased. (2) The quality of the clofarabine injection of the present invention is stable, and there is no precipitation of particles after long-term storage. (3) In clinical use, it can be easily compatible with a variety of drugs, and can also be added to sodium chloride or glucose infusion for intravenous infusion to patients, increasing the number of patients suitable for use.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a clofarabine injection and a preparation method thereof. Background technique [0002] Clofarabine, also known as lufarabine and clorabine, is a nucleoside purine antimetabolite developed by American Bioenvision Company and produced by Genzyme Company. It is used for the treatment of refractory or recurrent acute patients with lymphocytic leukemia. Clofarabine is converted into a 5'-monophosphate metabolite by deoxycytidine kinase in the cell, and then converted into an active 5'-triphosphate form by monophosphate and bisphosphate kinases. Clofarabine triphosphate inhibits ribose Nucleic acid reductase and DNA polymerase inhibit DNA synthesis, and have cytotoxic effects on both rapidly growing and quiescent cancer cells in vitro. [0003] Clofarabine is a white crystalline powder, chemical name: 2-chloro-9-(2-deoxy-2-fluoro-β-D-arabinofuran)-9H-...

AI Technical Summary

Problems solved by technology

[0005] In summary, in the prior art, the solubility of clofarabine is usually improved by adding a large dose of solubilizing agent to the prescription. Solvents have certain hemolytic properties, and some compatibilizers such as polyoxyethylene castor oil can also cause severe allergic reactions, and the pain caused often requires the addition of benzyl alcohol

Simultaneously, the freeze-dried powder injection of clofarabine provided by prior art, because its solubility in water is low, the stability of resulting freeze-dried product is not high, is not suitable for storage

[0006] It can be seen that the existing clofarabine injections have certain limitations in enhancing the water solubility of clofarabine and solving the problem of particle precipitation in aqueous solution.

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