Email this article Polymorphism of Risperidone in Supercritical Fluid Processes of Micronization and Encapsulation into Aliphatic Polyesters
- Authors: Bagratashvili V.N.1,2, Bogorodskiy S.E.1, Egorov A.M.2, Krotova L.I.1, Mironov A.V.1, Parenago O.O.2,3, Pokrovskiy O.I.3, Ustinovich K.B.3, Chizhov P.S.2, Prokopchuk D.I.4, Popov V.K.1, Tsypina S.I.1
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Affiliations:
- Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies
- Faculty of Chemistry
- Kurnakov Institute of General and Inorganic Chemistry
- Immanuel Kant Baltic Federal University
- Issue: Vol 11, No 7 (2017)
- Pages: 1163-1172
- Section: Article
- URL: https://journals.rcsi.science/1990-7931/article/view/200010
- DOI: https://doi.org/10.1134/S199079311707003X
- ID: 200010
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Abstract
The specific features of the transformation of risperidone polymorphs as a result of micronization and encapsulation into aliphatic polyesters (polylactides and polylactoglycolide) have been studied using supercritical (SC) carbon dioxide. It has been shown that the micronization of risperidone, which originally is polymorph A, via the rapid expansion of supercritical solutions (RESS) and the supercritical antisolvent (SAS) precipitation leads to its crystallization in less thermodynamically stable polymorph B. This transition is complete for SAS and only partial for RESS. When these micronized samples are encapsulated into polylactides and polylactoglycolides via the formation of particles from gas-saturated solutions (PGSS) and monolithization with further cryogrinding (MCG), risperidone polymorph B is partially converted back into polymorph A. At the same time, the micronization of initial risperidone polymorph A via cryogrinding and its further PGSS and MCG encapsulation into polylactides or polylactoglycolides does not result in any change in the polymorphic state of risperidone, and it always remains in initial polymorph A.
About the authors
V. N. Bagratashvili
Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies; Faculty of Chemistry
Author for correspondence.
Email: victor.bagratashvili@gmail.com
Russian Federation, Troitsk, Moscow, 119333; Moscow, 119991
S. E. Bogorodskiy
Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies
Email: victor.bagratashvili@gmail.com
Russian Federation, Troitsk, Moscow, 119333
A. M. Egorov
Faculty of Chemistry
Email: victor.bagratashvili@gmail.com
Russian Federation, Moscow, 119991
L. I. Krotova
Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies
Email: victor.bagratashvili@gmail.com
Russian Federation, Troitsk, Moscow, 119333
A. V. Mironov
Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies
Email: victor.bagratashvili@gmail.com
Russian Federation, Troitsk, Moscow, 119333
O. O. Parenago
Faculty of Chemistry; Kurnakov Institute of General and Inorganic Chemistry
Email: victor.bagratashvili@gmail.com
Russian Federation, Moscow, 119991; Moscow, 119991
O. I. Pokrovskiy
Kurnakov Institute of General and Inorganic Chemistry
Email: victor.bagratashvili@gmail.com
Russian Federation, Moscow, 119991
K. B. Ustinovich
Kurnakov Institute of General and Inorganic Chemistry
Email: victor.bagratashvili@gmail.com
Russian Federation, Moscow, 119991
P. S. Chizhov
Faculty of Chemistry
Email: victor.bagratashvili@gmail.com
Russian Federation, Moscow, 119991
D. I. Prokopchuk
Immanuel Kant Baltic Federal University
Email: victor.bagratashvili@gmail.com
Russian Federation, Kaliningrad, 236016
V. K. Popov
Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies
Email: victor.bagratashvili@gmail.com
Russian Federation, Troitsk, Moscow, 119333
S. I. Tsypina
Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies
Email: victor.bagratashvili@gmail.com
Russian Federation, Troitsk, Moscow, 119333
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