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.

作者简介

V. Bagratashvili

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

编辑信件的主要联系方式.
Email: victor.bagratashvili@gmail.com
俄罗斯联邦, Troitsk, Moscow, 119333; Moscow, 119991

S. Bogorodskiy

Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies

Email: victor.bagratashvili@gmail.com
俄罗斯联邦, Troitsk, Moscow, 119333

A. Egorov

Faculty of Chemistry

Email: victor.bagratashvili@gmail.com
俄罗斯联邦, Moscow, 119991

L. Krotova

Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies

Email: victor.bagratashvili@gmail.com
俄罗斯联邦, Troitsk, Moscow, 119333

A. Mironov

Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies

Email: victor.bagratashvili@gmail.com
俄罗斯联邦, Troitsk, Moscow, 119333

O. Parenago

Faculty of Chemistry; Kurnakov Institute of General and Inorganic Chemistry

Email: victor.bagratashvili@gmail.com
俄罗斯联邦, Moscow, 119991; Moscow, 119991

O. Pokrovskiy

Kurnakov Institute of General and Inorganic Chemistry

Email: victor.bagratashvili@gmail.com
俄罗斯联邦, Moscow, 119991

K. Ustinovich

Kurnakov Institute of General and Inorganic Chemistry

Email: victor.bagratashvili@gmail.com
俄罗斯联邦, Moscow, 119991

P. Chizhov

Faculty of Chemistry

Email: victor.bagratashvili@gmail.com
俄罗斯联邦, Moscow, 119991

D. Prokopchuk

Immanuel Kant Baltic Federal University

Email: victor.bagratashvili@gmail.com
俄罗斯联邦, Kaliningrad, 236016

V. Popov

Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies

Email: victor.bagratashvili@gmail.com
俄罗斯联邦, Troitsk, Moscow, 119333

S. Tsypina

Federal Research Center Crystallography and Photonics, Institute of Photonic Technologies

Email: victor.bagratashvili@gmail.com
俄罗斯联邦, Troitsk, Moscow, 119333

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