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Publikācija: Structural Characterization of Cevimeline and Its Trans-Impurity by Single Crystal XRD

Publication Type Scientific article indexed in SCOPUS or WOS database
Funding for basic activity Unknown
Defending: ,
Publication language English (en)
Title in original language Structural Characterization of Cevimeline and Its Trans-Impurity by Single Crystal XRD
Field of research 2. Engineering and technology
Sub-field of research 2.5 Materials engineering
Authors Dmitrijs Stepanovs
Zenta Tetere
Irisa Rāviņa
Viktors Kumpiņš
Daina Zicāne
Ērika Bizdēna
Janis Bogans
Irina Novosjolova
Agnese Ābele
Remo Merijs-Meri
Juris Fotins
Maksims Čerkasovs
Anatolijs Mišņovs
Māris Turks
Keywords Cevimeline, trans-Cevimeline, Impurity standard, Single crystal, X-ray analysis, Thermal analysis, Solubility
Abstract Cevimeline is muscarinic receptor agonist which increases secretion of exocrine glands. Cevimeline base is a liquid (m.p. 20–25◦C) at ambient conditions, therefore its pharmaceutical formulation as asolid hydrochloride hemihydrate has been developed. The synthesis of cevimeline yields its cis- and trans-isomers and only the cis-isomer is recognized as the API and used in the finished formulation.In this study structural and physicochemical investigations of hydrochloride hemihydrates of cis- and trans-cevimelines have been performed. Single crystal X-ray analyses of both cis- and trans-isomers of cevimeline are reported here for the first time. It was found that the cis-isomer, the API, has less dense crystal packing, lower melting point and higher solubility in comparison to the trans-isomer.
DOI: 10.1016/j.jpba.2015.11.006
Hyperlink: http://www.sciencedirect.com/science/article/pii/S0731708515302260 
Reference Stepanovs, D., Tetere, Z., Rāviņa, I., Kumpiņš, V., Zicāne, D., Bizdēna, Ē., Bogans, J., Novosjolova, I., Grigaloviča, A., Merijs-Meri, R., Fotins, J., Čerkasovs, M., Mišņovs, A., Turks, M. Structural Characterization of Cevimeline and Its Trans-Impurity by Single Crystal XRD. Journal of Pharmaceutical and Biomedical Analysis, 2016, Vol.118, pp.404-409. ISSN 0731-7085. Available from: doi:10.1016/j.jpba.2015.11.006
Additional information Citation count:
ID 21095