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Title:
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Pressure-temperature phase diagram of the dimorphism of the anti-inflammatory drug nimesulide
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Author:
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Barrio Casado, María del; Huguet, Jordi; Robert, B.; Rietveld, Ivo B.; Céolin, René; Tamarit Mur, José Luis
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Other authors:
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Universitat Politècnica de Catalunya. Departament de Física; Universitat Politècnica de Catalunya. GCM - Grup de Caracterització de Materials |
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Abstract:
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Understanding the phase behavior of active pharmaceutical ingredients is important for formulations of dosage forms and regulatory reasons. Nimesulide is an anti-inflammatory drug that is known to exhibit dimorphism; however up to now its stability behavior was not clear, as few thermodynamic data were available. Therefore, calorimetric melting data have been obtained, which were found to be TI-L = 422.4 ± 1.0 K, ¿I ¿ LH = 117.5 ± 5.2 J g-1, TII-L = 419.8 ± 1.0 K and ¿II ¿ LH = 108.6 ± 3.3 J g-1. In addition, vapor-pressure data, high-pressure melting data, and specific volumes have been obtained. It is demonstrated that form II is intrinsically monotropic in relation to form I and the latter would thus be the best polymorph to use for drug formulations. This result has been obtained by experimental means, involving high-pressure measurements. Furthermore, it has been shown that with very limited experimental and statistical data, the same conclusion can be obtained, demonstrating that in first instance topological pressure-temperature phase diagrams can be obtained without necessarily measuring any high-pressure data. It provides a quick method to verify the phase behavior of the known phases of an active pharmaceutical ingredient under different pressure and temperature conditions. |
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Subject(s):
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-Àrees temàtiques de la UPC::Física
-Calorimetry
-Crystallography
-Polymorphism (Crystallography)
-Thermodynamics
-Polymorphism
-Thermodynamics
-Pressure-temperature phase diagram
-Phase behavior
-Crystallography
-Calorimetry
-Preformulation
-Termodinàmica
-Cristal·lografia
-Calorimetria
-Polimorfisme (Cristal·lografia) |
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Rights:
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Document type:
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Article - Submitted version
Article |
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