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 a solid 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.
journal_name
J Pharm Biomed Analjournal_title
Journal of pharmaceutical and biomedical analysisauthors
Stepanovs D,Tetere Z,Rāviņa I,Kumpiņš V,Zicāne D,Bizdēna Ē,Bogans J,Novosjolova I,Grigaloviča A,Meri RM,Fotins J,Čerkasovs M,Mishnev A,Turks Mdoi
10.1016/j.jpba.2015.11.006subject
Has Abstractpub_date
2016-01-25 00:00:00pages
404-409eissn
0731-7085issn
1873-264Xpii
S0731-7085(15)30226-0journal_volume
118pub_type
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