Fosaprepitant composition and preparation method thereof

Abstract

The present application and its embodiments teach stable compositions of fosaprepitant or a pharmaceutically acceptable salt thereof with such compositions lacking polysorbate 80 and containing dual functional excipients of hydrolysis inhibition and solubility enhancement. Further described are methods of preparation of such compositions. Among other advantages of contemplated compositions, fosaprepitant hydrolysis degradation is kept low and the compositions maintain physically and chemically stable for prolonged period.

Description

[0001] priority claim [0002] This application claims priority to U.S. Application No. 16 / 245,992, filed January 11, 2019, which claims priority to U.S. Provisional Application No. 62 / 673,522, filed May 18, 2018 Right, the entire content of said application is incorporated herein by reference in its entirety. technical field [0003] The field of the invention and its embodiments relates to stable compositions of fosaprepitant or a pharmaceutically acceptable salt thereof. In particular, the present application relates to compositions of fosaprepitant dimeglumine that do not contain polysorbate 80 or similar surfactants. Methods of preparing such compositions are further described herein. Background technique [0004] Fosaprepitant dimeglumine is an injectable drug sold by Merck Sharp & Dohme Corp. active pharmaceutical ingredients. Fosaprepitant is a water-soluble phosphorylated prodrug of aprepitant that is rapidly converted to aprepitant in vivo after intravenous (I...

AI Technical Summary

Problems solved by technology

However, polysorbate 80, a common solubilizer for low solubility drug formulations, is known to cause a variety of adverse reactions, including severe infusion site reactions and potentially life-threatening anaphylaxis

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