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

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Nosaukums oriģinālvalodā Structural Characterization of Cevimeline and Its Trans-Impurity by Single Crystal XRD
Pētniecības nozare 2. Inženierzinātnes un tehnoloģijas
Pētniecības apakšnozare 2.5. Materiālzinātne
Autori 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
Atslēgas vārdi Cevimeline, trans-Cevimeline, Impurity standard, Single crystal, X-ray analysis, Thermal analysis, Solubility
Anotācija 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
Hipersaite: http://www.sciencedirect.com/science/article/pii/S0731708515302260 
Atsauce 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, 404.-409.lpp. ISSN 0731-7085. Pieejams: doi:10.1016/j.jpba.2015.11.006
Papildinformācija Citējamību skaits:
ID 21095