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Crystal structure and solid-state studies of aged samples of tienoxolol, an API designed against hypertension

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10.1016/j-ijpharm.2011.10.025
 
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hdl:2117/14578

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Teulon, Jean-Marie
Mahé, Nathalie
Do, Bernard
Nicolaï, Béatrice
Rietveld, Ivo B.
Barrio Casado, María delMés informacióMés informacióMés informació
Tamarit Mur, José LuisMés informacióMés informacióMés informació
Céolin, René
Ghéchot, Christophe
Document typeArticle
Defense date2012
Rights accessRestricted access - publisher's policy
Attribution-NonCommercial-NoDerivs 3.0 Spain
Except where otherwise noted, content on this work is licensed under a Creative Commons license : Attribution-NonCommercial-NoDerivs 3.0 Spain
Abstract
Aging of drug molecules is generally studied following regulatory procedures, i.e. under forced conditions and for relatively limited storage time; therefore naturally aged samples are rare and provide scientific reference data beyond regulatory considerations. Tienoxolol was studied after 25 years of storage in the dark under ambient conditions. About 86% of the samples still consisted of tienoxolol and the main impurity (13%) was caused by the hydrolysis of the ester moiety. Protection from humidity is therefore important. Other sensitive groups containing nitrogen and sulfur appear to be quite stable with less than 0.8% conversion over 25 years. In addition, the crystal structure has been solved. Tienoxolol orange needles were found to crystallize in the orthorhombic non-centrosymmetric space group Iba2, indicating that the crystal is a racemic compound. The unit cell parameters at room temperature are a = 10.069(5)A˚ , b = 45.831(10)A˚ , and c = 9.822(5) ˚A and the unit cell volume is 4533(3) ˚A3 with Z = 8. © 2011 Elsevier B.V.
CitationMahé, N. [et al.]. Crystal structure and solid-state studies of aged samples of tienoxolol, an API designed against hypertension. "International journal of pharmaceutics", 2012, vol. 422, núm. 1-2, p. 47-51. 
URIhttp://hdl.handle.net/2117/14578
DOI10.1016/j-ijpharm.2011.10.025
ISSN0378-5173
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  • Departament de Física i Enginyeria Nuclear (fins octubre 2015) - Articles de revista [603]
  • GCM - Grup de Caracterització de Materials - Articles de revista [332]
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