Azacitidine freeze-drying powder needle for injection and method for preparing azacitidine freeze-drying powder needle

Abstract

The invention discloses an azacitidine freeze-drying powder needle for injection, the azacitidine freeze-drying powder needle comprises the raw materials, by weight, of 2-8 parts of azacitidine, 2-8 parts of mannitol and 150-400 parts of organic solvent. The invention further provides a method for preparing the azacitidine freeze-drying powder needle for injection. According to the azacitidine freeze-drying powder needle for injection and the method for preparing the azacitidine freeze-drying powder needle, by changing the technical key points of the product solvent formula, the solution preparation temperature, the charging sequence, the freeze-drying process and the like, the impurity level of the product can be effectively controlled, and the freeze-drying preparation with the stabilitysuperior to that of the foreign original research products can be produced.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to azacitidine freeze-dried powder for injection and a preparation method thereof. Background technique [0002] Azacitidine is a cytidine analog that is mainly used in the treatment of myelodysplastic syndromes. U.S. FDA approved this medicine to go on the market in 2004, because the active ingredient azacitidine of this medicine is relatively poor in stability, hydrolyzes rapidly in water, so the preparation on the market is a powder injection preparation. At present, only original research products are on the market in my country. [0003] Publication No. CN101632643A, an invention patent titled "Azacitidine Freeze-Dried Powder Injection Preparation and Its Preparation Method", provides a freeze-dried powder injection preparation of azacitidine drug for the treatment of myelodysplastic syndrome and its preparation method , Azacitidine freeze-dried powder preparation prescripti...

AI Technical Summary

Problems solved by technology

This patent uses ethanol, isopropanol, methanol or other alcohols containing hydroxy as solvents to accelerate the dissolution of pharmaceutical active agents, but research has found that when ethanol, isopropanol, methanol or other alcohols containing hydroxy are used as solvents, due to mannitol and There are several hydroxyl groups in the ribose ring of azacitidine, which interact with the solvent hydroxyl groups, and the particle size of the crystals formed during the freeze-drying stage will be significantly reduced, so the bioequivalence of its reconstituted suspension cannot meet FDA requirements. Requirements for the bioequivalence of the product

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