Polymorphism of Risperidone in Supercritical Fluid Processes of Micronization and Encapsulation into Aliphatic Polyesters


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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.

Sobre autores

V. Bagratashvili

Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies; Faculty of Chemistry

Autor responsável pela correspondência
Email: victor.bagratashvili@gmail.com
Rússia, Troitsk, Moscow, 119333; Moscow, 119991

S. Bogorodskiy

Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies

Email: victor.bagratashvili@gmail.com
Rússia, Troitsk, Moscow, 119333

A. Egorov

Faculty of Chemistry

Email: victor.bagratashvili@gmail.com
Rússia, Moscow, 119991

L. Krotova

Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies

Email: victor.bagratashvili@gmail.com
Rússia, Troitsk, Moscow, 119333

A. Mironov

Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies

Email: victor.bagratashvili@gmail.com
Rússia, Troitsk, Moscow, 119333

O. Parenago

Faculty of Chemistry; Kurnakov Institute of General and Inorganic Chemistry

Email: victor.bagratashvili@gmail.com
Rússia, Moscow, 119991; Moscow, 119991

O. Pokrovskiy

Kurnakov Institute of General and Inorganic Chemistry

Email: victor.bagratashvili@gmail.com
Rússia, Moscow, 119991

K. Ustinovich

Kurnakov Institute of General and Inorganic Chemistry

Email: victor.bagratashvili@gmail.com
Rússia, Moscow, 119991

P. Chizhov

Faculty of Chemistry

Email: victor.bagratashvili@gmail.com
Rússia, Moscow, 119991

D. Prokopchuk

Immanuel Kant Baltic Federal University

Email: victor.bagratashvili@gmail.com
Rússia, Kaliningrad, 236016

V. Popov

Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies

Email: victor.bagratashvili@gmail.com
Rússia, Troitsk, Moscow, 119333

S. Tsypina

Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies

Email: victor.bagratashvili@gmail.com
Rússia, Troitsk, Moscow, 119333

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