Thermodynamic Investigation of Carbamazepine-Saccharin Co-Crystal Polymorphs.

J Pharm Sci

Centre for Pharmaceutical Engineering Science, School of Pharmacy and Medical Sciences, University of Bradford, Richmond Road, Bradford BD7 1DP, UK. Electronic address:

Published: August 2017

Polymorphism in active pharmaceutical ingredients can be regarded as critical for the potential that crystal form can have on the quality, efficacy, and safety of the final drug product. The current contribution aims to characterize thermodynamic interrelationship of a dimorphic co-crystal, FI and FII, involving carbamazepine (CBZ) and saccharin (SAC) molecules. Supramolecular synthesis of CBZ-SAC FI and FII has been performed using thermokinetic methods and systematically characterized by differential scanning calorimetry, powder X-ray diffraction, solubility, and slurry measurements. According to the heat of fusion rule by Burger and Ramberger, FI (ΔH = 121.1 J/g; melting point, 172.5°C) and FII (ΔH = 110.3 J/g; melting point, 164.7°C) are monotropically related. The solubility and van't Hoff plot results suggest FI stable and FII metastable forms. This study reveals that CBZ-SAC co-crystal phases, FI or FII, could be stable to heat-induced stresses; however, FII converts to FI during solution-mediated transformation.

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http://dx.doi.org/10.1016/j.xphs.2017.04.017DOI Listing

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