RTU Research Information System
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 |
