Identifying, Characterizing, and Understanding Nefiracetam in Its Solid State Forms: A Potential Antidementia Drug

Xavier Buol; Koen Robeyns; Nikolay Tumanov; Johan Wouters; Tom Leyssens

doi:10.1016/j.xphs.2019.07.010

Identifying, Characterizing, and Understanding Nefiracetam in Its Solid State Forms: A Potential Antidementia Drug

J Pharm Sci. 2019 Nov;108(11):3616-3622. doi: 10.1016/j.xphs.2019.07.010. Epub 2019 Jul 24.

Authors

Xavier Buol¹, Koen Robeyns², Nikolay Tumanov³, Johan Wouters³, Tom Leyssens⁴

Affiliations

¹ Institute of Condensed Matter and Nanosciences, UCLouvain, 1 Place Louis Pasteur, B-1348 Louvain-la-Neuve, Belgium. Electronic address: [email protected].
² Institute of Condensed Matter and Nanosciences, UCLouvain, 1 Place Louis Pasteur, B-1348 Louvain-la-Neuve, Belgium.
³ Unité de Chimie Biologique et Structurale, Chemistry Department, UNamur, 61 rue de Bruxelles, B-5000 Namur, Belgium.
⁴ Institute of Condensed Matter and Nanosciences, UCLouvain, 1 Place Louis Pasteur, B-1348 Louvain-la-Neuve, Belgium. Electronic address: [email protected].

PMID: 31348939
DOI: 10.1016/j.xphs.2019.07.010

Abstract

In this work, 3 hitherto unidentified solid state forms of the nootropic drug Nefiracetam are identified: a monohydrate and 2 polymorphic phases of the anhydrate. These new forms were investigated from a structural and thermodynamic point of view to evaluate the possibility of using these forms in alternative formulations. Furthermore, their dissolution rate and solubility were compared.

Keywords: dissolution; formulation; hydrate; nefiracetam; polymorph; solid state.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Chemistry, Pharmaceutical / methods
Nootropic Agents / chemistry*
Polymers / chemistry
Pyrrolidinones / chemistry*
Solubility / drug effects
Thermodynamics

Substances

Nootropic Agents
Polymers
Pyrrolidinones
nefiracetam