Solid-state study of polymorphic drugs: carbamazepine

Polymorphs of a compound have solid crystalline phases with different internal crystal lattices; in pharmaceuticals, differences due to polymorphism and pseudopolymorphism can affect bioavailability and effective clinical use. The aim of this work was to obtain the different polymorphic modification...

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Bibliographic Details
Published in:Journal of pharmaceutical and biomedical analysis 2000-08, Vol.23 (1), p.41-54
Main Authors: Rustichelli, C, Gamberini, G, Ferioli, V, Gamberini, M.C, Ficarra, R, Tommasini, S
Format: Article
Language:English
Subjects:
Anticonvulsants - chemistry
Biological and medical sciences
Calorimetry, Differential Scanning
Carbamazepine
Carbamazepine - chemistry
Differential scanning calorimetry
General pharmacology
Hot Stage FT-IR thermomicroscopy
Medical sciences
Microscopy - methods
Molecular Structure
Pharmacology. Drug treatments
Physicochemical properties. Structure-activity relationships
Polymorphism
Solid state characterisation
Spectroscopy, Fourier Transform Infrared
X-Ray powder diffraction
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Summary:Polymorphs of a compound have solid crystalline phases with different internal crystal lattices; in pharmaceuticals, differences due to polymorphism and pseudopolymorphism can affect bioavailability and effective clinical use. The aim of this work was to obtain the different polymorphic modifications of the anticonvulsant drug, carbamazepine, and to characterise them by means of typical structure-sensitive analytical techniques, such as FT-IR spectroscopy, XRPD and DSC. Further investigations were also performed by Hot Stage FT-IR thermomicroscopy, which permitted the visible and spectroscopic characterisation of the polymorphic forms during heating. Our results confirm the existence of three different polymorphic forms for anhydrous carbamazepine: Form III, the commercial one, Form I, obtained by heating Form III and Form II, crystallised from ethanolic solution. Substantial differences were detected among the polymorphs with regard to solid-state properties. Moreover, Hot Stage FT-IR thermomicroscopy proved its analytical potential to characterise the drug's polymorphism.
ISSN:0731-7085
1873-264X
DOI:10.1016/S0731-7085(00)00262-4