Polymorphism of benzylthiouracil, an active pharmaceutical ingredient against hyperthyroidism - Normandie Université Accéder directement au contenu
Article Dans Une Revue International Journal of Pharmaceutics Année : 2021

Polymorphism of benzylthiouracil, an active pharmaceutical ingredient against hyperthyroidism

Résumé

The crystal structures of dimorphic benzylthiouracil, a drug against hyperthyroidism, have been redetermined and the atom coordinates of the two independent molecules of form I have been obtained for the first time. The dimorphism convincingly demonstrates the conformational versatility of the benzylthiouracil molecule. It has been established through calorimetric studies that the low-temperature form II transforms endothermically (ΔII→IH = 5.6(1.5) J g− 1) into form I at 405.4(1.0) K. The high-temperature form I melts at 496.8(1.0) K (ΔI→LH = 152.6(4.0) J g− 1). Crystallographic and thermal expansion studies show that form II is denser than form I, leading to the conclusion that the slope of the II-I equilibrium curve in the pressure-temperature phase diagram is positive. It follows that this dimorphism corresponds to a case of overall enantiotropic behaviour, which implies that both solid phases possess their own stable phase region irrespective of the pressure. Moreover, form II is clearly the stable polymorph under ambient conditions.
Fichier principal
Vignette du fichier
S0378517321001824.pdf (4.91 Mo) Télécharger le fichier
Origine : Fichiers produits par l'(les) auteur(s)

Dates et versions

hal-03166420 , version 1 (10-03-2023)

Licence

Paternité - Pas d'utilisation commerciale

Identifiants

Citer

Ivo B. Rietveld, Hassan Allouchi, Maria Barrio, René Ceolin, Josep-Lluis Tamarit. Polymorphism of benzylthiouracil, an active pharmaceutical ingredient against hyperthyroidism. International Journal of Pharmaceutics, 2021, 598, pp.120378. ⟨10.1016/j.ijpharm.2021.120378⟩. ⟨hal-03166420⟩
59 Consultations
19 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More