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Volume 15
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Article

Polymorphism of Carbamazepine Pharmaceutical Cocrystal: Structural Analysis and Solubility Performance

by
Artem O. Surov
1,
Ksenia V. Drozd
1,
Anna G. Ramazanova
1,
Andrei V. Churakov
2,
Anna V. Vologzhanina
3,
Elizaveta S. Kulikova
4 and
German L. Perlovich
1,*
1
G.A. Krestov Institute of Solution Chemistry RAS, Akademicheskaya Str. 1, 153045 Ivanovo, Russia
2
N.S. Kurnakov Institute of General and Inorganic Chemistry RAS, Leninsky Prosp. 31, 119991 Moscow, Russia
3
A.N. Nesmeyanov Institute of Organoelement Compounds RAS, Vavilova Str. 28, 119334 Moscow, Russia
4
National Research Center Kurchatov Institute, 1 Kurchatova pl., 123098 Moscow, Russia
*
Author to whom correspondence should be addressed.
Pharmaceutics 2023, 15(6), 1747; https://doi.org/10.3390/pharmaceutics15061747
Submission received: 15 May 2023 / Revised: 31 May 2023 / Accepted: 14 June 2023 / Published: 15 June 2023
(This article belongs to the Special Issue Polymorphism)
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Abstract

Polymorphism is a common phenomenon among single- and multicomponent molecular crystals that has a significant impact on the contemporary drug development process. A new polymorphic form of the drug carbamazepine (CBZ) cocrystal with methylparaben (MePRB) in a 1:1 molar ratio as well as the drug’s channel-like cocrystal containing highly disordered coformer molecules have been obtained and characterized in this work using various analytical methods, including thermal analysis, Raman spectroscopy, and single-crystal and high-resolution synchrotron powder X-ray diffraction. Structural analysis of the solid forms revealed a close resemblance between novel form II and previously reported form I of the [CBZ + MePRB] (1:1) cocrystal in terms of hydrogen bond networks and overall packing arrangements. The channel-like cocrystal was found to belong to a distinct family of isostructural CBZ cocrystals with coformers of similar size and shape. Form I and form II of the 1:1 cocrystal appeared to be related by a monotropic relationship, with form II being proven to be the thermodynamically more stable phase. The dissolution performance of both polymorphs in aqueous media was significantly enhanced when compared with parent CBZ. However, considering the superior thermodynamic stability and consistent dissolution profile, the discovered form II of the [CBZ + MePRB] (1:1) cocrystal seems a more promising and reliable solid form for further pharmaceutical development.
Keywords: carbamazepine; methylparaben; cocrystal; polymorphism; crystal structure; stability; dissolution carbamazepine; methylparaben; cocrystal; polymorphism; crystal structure; stability; dissolution
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MDPI and ACS Style

Surov, A.O.; Drozd, K.V.; Ramazanova, A.G.; Churakov, A.V.; Vologzhanina, A.V.; Kulikova, E.S.; Perlovich, G.L. Polymorphism of Carbamazepine Pharmaceutical Cocrystal: Structural Analysis and Solubility Performance. Pharmaceutics 2023, 15, 1747. https://doi.org/10.3390/pharmaceutics15061747

AMA Style

Surov AO, Drozd KV, Ramazanova AG, Churakov AV, Vologzhanina AV, Kulikova ES, Perlovich GL. Polymorphism of Carbamazepine Pharmaceutical Cocrystal: Structural Analysis and Solubility Performance. Pharmaceutics. 2023; 15(6):1747. https://doi.org/10.3390/pharmaceutics15061747

Chicago/Turabian Style

Surov, Artem O., Ksenia V. Drozd, Anna G. Ramazanova, Andrei V. Churakov, Anna V. Vologzhanina, Elizaveta S. Kulikova, and German L. Perlovich. 2023. "Polymorphism of Carbamazepine Pharmaceutical Cocrystal: Structural Analysis and Solubility Performance" Pharmaceutics 15, no. 6: 1747. https://doi.org/10.3390/pharmaceutics15061747

APA Style

Surov, A. O., Drozd, K. V., Ramazanova, A. G., Churakov, A. V., Vologzhanina, A. V., Kulikova, E. S., & Perlovich, G. L. (2023). Polymorphism of Carbamazepine Pharmaceutical Cocrystal: Structural Analysis and Solubility Performance. Pharmaceutics, 15(6), 1747. https://doi.org/10.3390/pharmaceutics15061747

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