Crystal structure and solid-state studies of aged samples of tienoxolol, an API designed against hypertension - Archive ouverte HAL Accéder directement au contenu
Article Dans Une Revue International Journal of Pharmaceutics Année : 2012

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

Résumé

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) angstrom, b = 45.831(10) angstrom, and c = 9.822(5) angstrom and the unit cell volume is 4533(3) angstrom(3) with Z = 8.

Domaines

Chimie

Dates et versions

hal-04119183 , version 1 (06-06-2023)

Identifiants

Citer

Nathalie Mahé, Bernard Do, Béatrice Nicolaï, Ivo B. Rietveld, Maria Barrio, et al.. Crystal structure and solid-state studies of aged samples of tienoxolol, an API designed against hypertension. International Journal of Pharmaceutics, 2012, 422 (1-2), pp.47-51. ⟨10.1016/j.ijpharm.2011.10.025⟩. ⟨hal-04119183⟩
2 Consultations
0 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More