Design and properties of pharmaceutical co-crystals

About the group:

In recent years, the development of a pharmaceutical cocrystal has become a novel strategy to improve the solid state properties of an API. Usually, the solubility characteristics improve on the orders and this fact leads to essential reduction of therapeutic doses and, as a consequence, side effects. A cocrystal can be described as a supramolecular system formed by two different molecular entities where, one from the compounds is a poorly soluble API, whereas the second component presents a molecule of well soluble substance, which uptakes by body completely and takes part in enzymatic processes. The second component molecule belongs to GRAS (Generally Regarded As Save) list which includes the compounds recommended for application at pharmaceutical and food industries.

Carried out investigations:

Cocrystal screening
Characterization of cocrystal by X-ray diffraction methods
Studying cocrystal solubility processes (kinetic and thermodynamic approaches) and comparison of the obtained characteristics with individual cocrystal components
Parameters searching to obtain thermodynamic stable cocrystals with controlled stoichiometry aimed to scale-up procedure
Membrane permeability of cocrystal and comparison with analogous characteristics of individual components

Drozd Ksenia Viktorovna

Researcher

Phd in chemistry

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Manin Alexey Nikolaevich

Senior Researcher

Phd in chemistry

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Voronin Alexander Pavlovich

Senior Researcher

Phd in chemistry

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2012-2015

Manin, A.N.; Voronin, A.P.; Shishkina, A.V.; Vener, M.V.; Churakov, A.V.; Perlovich, G.L. Influence of secondary interactions on the structure, sublimation thermodynamics, and solubility of salicylate:4-hydroxybenzamide cocrystals. Combined experimental and theoretical study. The Journal of Physical Chemistry B, (2015), 119(33), 10466-10477
Surov A.O., Manin A.N., Voronin A.P., Drozd K.V., Simagina A.A., Churakov A.V., Perlovich G.L., Pharmaceutical salts of ciprofloxacin with dicarboxilic acids. European Journal of Pharmaceutical Sciences, 2015, 77, 112-121
Artem O. Surov, Alexander P. Voronin, Alex N. Manin, Nikolay G. Manin, Lyudmila G. Kuzmina, Andrei V. Churakov, and German L. Perlovich. Pharmaceutical Cocrystals of Diflunisal and Diclofenac with Theophylline. Mol. Pharmaceutics, 2014, 11 (10), pp 3707–3715.
Surov A.O., Simagina A.A., Manin N.G., Kuzmina L.G., Churakov A.V., Perlovich G.L. Fenamate Co-crystals with 4,4′-Bipyridine: Structural and Thermodynamic aspects. Crystal Growth & Design. (2015) 15(7), 228-238.
Surov A.O., Voronin A.P., Manin A.N., Manin N.G., Kuzmina L.G., Churakov A.V., Perlovich G.L. Pharmaceutical co-crystals of diflunisal and diclofenac with theophylline. Mol. Pharmaceutics. (2014) 11(10), 3707-3715.
Manin A.N., Voronin A.P., Drozd K.V., Manin N.G., Bauer-Brandl A., Perlovich G.L. Cocrystal screening of hydroxybenzamides with benzoic acid derivatives: A comparative study of thermal and solution-based methods. European Journal of Pharmaceutical Sciences (2014) 65, 56–64.
Manin A.N., Voronin A.P., Manin N.G., Vener M.V., Shishkina A.V., Lermontov A.S., Perlovich G.L. Salicylamide Cocrystals: Screening, Crystal Structure, Sublimation Thermodynamics, Dissolution, and Solid-State DFT Calculations. J. Phys. Chem. B (2014) 118 (24), 6803-6814.
Surov A.O., Solanko K.A., Bond A.D., Bauer-Brandl A., Perlovich G.L. Polymorphism of felodipine co-crystals with 4,4′-bipyridine. CrystEngComm (2014) 16, 6603-6611.
Perlovich G.L. Thermodynamic approach to improving solubility prediction of co-crystals in comparison with individual poorly soluble components. J. Chem. Thermodynamics (2014), 73, 85-89.
Surov А.O., Solanko K.A., Bond A.D., Bauer-Brandl A., Perlovich G.L. Crystal architecture and physicochemical properties of felodipine solvates. CrystEngComm (2013) 15 (30), 6054 – 6061.
Surov A.O., Solanko K.A., Bond A.D., Perlovich G.L., Bauer-Brandl A. Crystallization and Polymorphism of Felodipine. Crystal Growth & Design. (2012) 12(8):4022-4030.