Icatibant composition for injection and preparation method and preparation thereof

Abstract

The invention relates to the technical field of medicine, and in particular relates to an Icatibant composition for injection and a preparation method and a preparation thereof. Icatibant composition for injection includes Icatibant, a freeze-drying protective agent, a cosolvent and stabilizer, and a pH regulator, wherein the mass ratio of Icatibant, the freeze-drying protective agent and the cosolvent and stabilizer is 1:(1-100):(1-100). The freeze-drying protective agent ensures that Icatibant does not degrade in the preparation and preservation processes; the cosolvent and stabilizer not only solves the problem of easy precipitation of Icatibant in solution state, but also plays the role of accelerating the re-dissolution of the freeze-dried injection powder preparation; the pH regulator can regulate the pH value of the Icatibant composition for injection after re-dissolution, and further maintains the stability of Icatibant. The Icatibant composition for injection provided by the invention has good stability, simple and reasonable formula and good re-dissolution performance, and can be prepared into the freeze-dried injection powder without being prepared into a pre-filled syringe; and the production process is simple.

Description

Technical field [0001] The invention belongs to the technical field of medicine, and particularly relates to an icatibant injection composition and a preparation method and preparation thereof. Background technique [0002] Icatibant, the English name: Icatibant, is a decapeptide containing 5 non-protein-derived amino acids. The structural formula is as follows: [0003] [0004] The peptide sequence is: H-D-Arg-Arg-Pro-Hyp-Gly-Thi-Ser-D-Tic-Oic-Arg-OH. [0005] Hereditary angioedema (HAE), also known as C1 inhibitor deficiency, is a rare autosomal dominant genetic disease caused by genetic defects, with an incidence of 1 / 50000~1 / 10000. HAE is characterized by unpredictable episodic edema and swelling of the hands, feet, face, throat, and abdomen, leading to disfigurement, disability or death. Patients usually have a family history of the disease. HAE patients may develop rapid edema of the hands, feet, limbs, face, intestines, larynx, or trachea, which may cause respiratory tract ...

AI Technical Summary

Problems solved by technology

During the preparation of the existing icatibant injection for long-term storage, particle precipitation and discoloration will occur, which is more likely to cause the degradation of icatibant, resulting in an excessively high impurity content; in addition, the commercially available injection products use prepackaged Syringe, this kind of filling production line is relatively complicated, the production cost is high, and the product price is expensive

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