CSIR-NCL and University of Hyderabad discover new hydrate polymorphs of Entresto

poona:CSIR-National Chemical Laboratory (CSIR-NCL), Pune and University of Hyderabad have discovered new hydrate polymorphs of Entrestois a product used to treat certain types of heart failure
CSIR-NCL as part of a Mission Mode program funded by the Council for Scientific and Industrial Research (CSIR), had begun research on new crystalline hydrate forms and polymorphs of Entresto in 2018. Ashwini Kumar Nangia, then Director of CSIR-NCL, and Dr. Rajesh G. Gonnade, Chief Scientist of the Division Physical and Materials Chemistryled the project.
The comprehensive study was published in the Royal Society of Chemistry CrystEngComm magazine, which deals with crystal technology and drug polymorphs. The research team successfully characterized and identified six different crystalline forms of Entresto, containing varying amounts of water and containing the active pharmaceutical ingredients (APIs) valsartan and sacubitril in their anionic state with bound sodium cations.
The various hydrated forms of Entresto contain 2.0-3.2% water and exhibit additional stability against temperature and moisture, which is vital for their long-term storage, shelf life and drug bioavailability. This paper is a first of its kind in which researchers have demonstrated that large supramolecular drug complexes pose unique challenges in the characterization of polymorphs and hydrate structures using powder X-ray diffraction, thermal measurements and spectroscopic techniques. The next task for the team will be to understand the molecular packing arrangement and hydrogen bonding with water by determining its crystal structures.
Entresto is the world’s best-selling drug launched for the treatment of chronic heart failure in advanced critical patients, approved by the US FDA in 2015.

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