Szymon Kamil Araj , Łukasz Szeleszczuk , Tomasz Gubica , Monika Zielińska-Pisklak , Kostas Bethanis , Elias Christoforides , Marta Katarzyna Dudek , Dariusz Maciej Pisklak
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Despite the significant amount of works devoted to the pharmacodynamics of Noopept, very little is known about its structural and physicochemical properties. Therefore, the aim of current study was to investigate this API in a very thorough way. In this work, the detailed physicochemical analysis of Noopept has been done using TGA/DSC, <sup>1</sup>H and <sup>13</sup>C liquid state NMR, <sup>13</sup>C CP/MAS NMR, SEM, SCXRD, and PXRD. Additionally, quantum chemical DFT computations under periodic boundary conditions, using CASTEP, were conducted to facilitate the analysis of experimental results. Besides, we’ve performed a polymorphism screening of this molecule.</p></div>","PeriodicalId":16685,"journal":{"name":"Journal of pharmaceutical and biomedical analysis","volume":"252 ","pages":"Article 116474"},"PeriodicalIF":3.1000,"publicationDate":"2024-09-16","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://www.sciencedirect.com/science/article/pii/S0731708524005144/pdfft?md5=e6277c2787efee3428c14fce11dd379c&pid=1-s2.0-S0731708524005144-main.pdf","citationCount":"0","resultStr":"{\"title\":\"Physicochemical and structural analysis of N-phenylacetyl-L-prolylglycine ethyl ester (Noopept) – An active pharmaceutical ingredient with nootropic activity\",\"authors\":\"Szymon Kamil Araj , Łukasz Szeleszczuk , Tomasz Gubica , Monika Zielińska-Pisklak , Kostas Bethanis , Elias Christoforides , Marta Katarzyna Dudek , Dariusz Maciej Pisklak\",\"doi\":\"10.1016/j.jpba.2024.116474\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p><em>N</em>-Phenylacetyl-L-prolylglycine ethyl ester (Noopept, GVS-111, omberacetam) is an orally available active pharmaceutical ingredient (API), with neuroprotective properties and ability to enhance cognitive function. It belongs to nootropic family of drugs and is included in the group of racetams, although its chemical structure is quite different than the other compounds from this group, including the most popular one – piracetam. The mechanism of action of this API is multifaced and is considered to be involving modulation of various neurotransmitter systems within the brain. Despite the significant amount of works devoted to the pharmacodynamics of Noopept, very little is known about its structural and physicochemical properties. Therefore, the aim of current study was to investigate this API in a very thorough way. In this work, the detailed physicochemical analysis of Noopept has been done using TGA/DSC, <sup>1</sup>H and <sup>13</sup>C liquid state NMR, <sup>13</sup>C CP/MAS NMR, SEM, SCXRD, and PXRD. Additionally, quantum chemical DFT computations under periodic boundary conditions, using CASTEP, were conducted to facilitate the analysis of experimental results. 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Physicochemical and structural analysis of N-phenylacetyl-L-prolylglycine ethyl ester (Noopept) – An active pharmaceutical ingredient with nootropic activity
N-Phenylacetyl-L-prolylglycine ethyl ester (Noopept, GVS-111, omberacetam) is an orally available active pharmaceutical ingredient (API), with neuroprotective properties and ability to enhance cognitive function. It belongs to nootropic family of drugs and is included in the group of racetams, although its chemical structure is quite different than the other compounds from this group, including the most popular one – piracetam. The mechanism of action of this API is multifaced and is considered to be involving modulation of various neurotransmitter systems within the brain. Despite the significant amount of works devoted to the pharmacodynamics of Noopept, very little is known about its structural and physicochemical properties. Therefore, the aim of current study was to investigate this API in a very thorough way. In this work, the detailed physicochemical analysis of Noopept has been done using TGA/DSC, 1H and 13C liquid state NMR, 13C CP/MAS NMR, SEM, SCXRD, and PXRD. Additionally, quantum chemical DFT computations under periodic boundary conditions, using CASTEP, were conducted to facilitate the analysis of experimental results. Besides, we’ve performed a polymorphism screening of this molecule.
期刊介绍：
This journal is an international medium directed towards the needs of academic, clinical, government and industrial analysis by publishing original research reports and critical reviews on pharmaceutical and biomedical analysis. It covers the interdisciplinary aspects of analysis in the pharmaceutical, biomedical and clinical sciences, including developments in analytical methodology, instrumentation, computation and interpretation. Submissions on novel applications focusing on drug purity and stability studies, pharmacokinetics, therapeutic monitoring, metabolic profiling; drug-related aspects of analytical biochemistry and forensic toxicology; quality assurance in the pharmaceutical industry are also welcome.
Studies from areas of well established and poorly selective methods, such as UV-VIS spectrophotometry (including derivative and multi-wavelength measurements), basic electroanalytical (potentiometric, polarographic and voltammetric) methods, fluorimetry, flow-injection analysis, etc. are accepted for publication in exceptional cases only, if a unique and substantial advantage over presently known systems is demonstrated. The same applies to the assay of simple drug formulations by any kind of methods and the determination of drugs in biological samples based merely on spiked samples. Drug purity/stability studies should contain information on the structure elucidation of the impurities/degradants.
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