The Effect of pH on Polymorph Formation of the Pharmaceutically Active Compound Tianeptine

International Journal of Pharmaceutics 2012
Liāna Orola, M.V. Veidis, I. Sarcevica, A. Actiņš, Sergejs Beļakovs, A. Platonenko

The anti-depressant pharmaceutical tianeptine has been investigated to determine the dynamics of polymorph formation under various pH conditions. By varying the pH two crystalline polymorphs were isolated. The molecular and crystal structures have been determined to identify the two polymorphs. One polymorph is an amino carboxylic acid and the other polymorph is a zwitterion. In the solid state the tianeptine moieties are bonded through hydrogen bonds. The zwitterion was found to be less stable and transformed to the acid form. During this investigation an amorphous form was identified.

Keywords
Tianeptine; Polymorph; Crystallization; pH; Crystal structure; X-ray diffractometry
DOI
10.1016/j.ijpharm.2012.04.061
Hyperlink
http://www.sciencedirect.com/science/article/pii/S0378517312004073

Orola, L., Veidis, M., Sarcevica, I., Actiņš, A., Beļakovs, S., Platonenko, A. The Effect of pH on Polymorph Formation of the Pharmaceutically Active Compound Tianeptine. International Journal of Pharmaceutics, 2012, Vol.432, Iss.1–2, pp.50-56. ISSN 0378-5173. Available from: doi:10.1016/j.ijpharm.2012.04.061

Publication language
English (en)