Polymorphism

A special issue of Pharmaceutics (ISSN 1999-4923). This special issue belongs to the section "Physical Pharmacy and Formulation".

Deadline for manuscript submissions: closed (30 September 2023) | Viewed by 2167

Special Issue Editor


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Guest Editor
G.A. Krestov Institute of Solution Chemistry of the Russian Academy of Sciences, 153045 Ivanovo, Russia
Interests: thermodynamics of sublimation; solubility and solvation processes of molecular crystals

Special Issue Information

Dear Colleagues,

Polymorphism, the property of a compound to crystallize in more than one distinct crystal form, plays an indispensable role in researching and developing pharmaceuticals, agrochemicals, materials, and food. Polymorphs exhibit different properties, such as crystal habit, solubility, dissolution rate, melting point, stability, mechanical properties, even bioavailability, which may influence the product quality. Therefore, the study of the behavior of polymorphs can provide a theoretical basis for selecting the optimal solid forms and serve in the polymorphic control and optimization of the products as a primary method. Recently, due to the progress in the crystal engineering for pharmaceutics, the multicomponent molecular crystals for the design of new-generation bioavailable drugs have been intensively applied. The development of this area gave a stimulus for the investigation of different aspects of the polymorphism of multicomponent systems. Revealing the similarity and differences between the properties of the polymorphic forms of the individual compounds and multicomponent systems will make a significant contribution to the understanding of the fundamental principles of the design of pharmaceutical materials with the desired characteristics.

I am happy to invite researchers involved in the field of polymorphism of pharmaceutical systems to present their high-quality results in this forum, which is freely available for open access and discussion. This Special Issue will cover multiple aspects connected with several pertinent topics, including but not limited to:

  • Screening the polymorphic forms of drug compounds and multicomponent molecular crystals (drug–drug, drug–coformer) by different methods and approaches (crystallization from solvent(s), sublimation, lyophilization, mechanochemistry, slurry, crystallization from melt and so on).
  • Analysis of the crystal structures (by single crystal X-ray) of polymorphic pharmaceutical systems (active pharmaceutical ingredients and their multicomponent crystals). Searching the regularities between the crystal structure characteristics and physicochemical properties/processes, which are important for the pharmaceutical industry: solubility, release, membrane permeability, phase transitions (including fusion processes of various modifications), thermodynamic stability, tabletting and so on. 
  • Theoretical calculations/evaluations (by various approaches) of the crystal lattice energies of different polymorphic forms and their relationship with the solubility characteristics and thermodynamic stability.
  • In vivo and in vitro studies of polymorphic modifications.

Prof. Dr. German L. Perlovich
Guest Editor

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Keywords

  • polymorphic forms
  • drug
  • multi-components molecular crystals
  • screening
  • solubility
  • thermodynamic stability
  • phase transitions
  • release
  • membrane permeability

Published Papers (1 paper)

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Research

18 pages, 3779 KiB  
Article
Polymorphism of Carbamazepine Pharmaceutical Cocrystal: Structural Analysis and Solubility Performance
by Artem O. Surov, Ksenia V. Drozd, Anna G. Ramazanova, Andrei V. Churakov, Anna V. Vologzhanina, Elizaveta S. Kulikova and German L. Perlovich
Pharmaceutics 2023, 15(6), 1747; https://doi.org/10.3390/pharmaceutics15061747 - 15 Jun 2023
Cited by 5 | Viewed by 1881
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 [...] Read more.
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. Full article
(This article belongs to the Special Issue Polymorphism)
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