2016, №4

сс. 4-16

Risperidone Polymorphism in SCF Proccesses of Miсronization and Encapsulation into Aliphatic Polyesters

2016, №4

сс. 4-16

Цитировать

V.N. Bagratashvili, S.E. Bogorodski, A.M. Egorov, L.I. Krotova, A.V. Mironov, O.O. Parenago, O.I. Pokrovskiy, K.B. Ustinovich, P.S. Chizhov, D.I. Prokopchuk, V.K. Popov, S.I. Tsypina

Key words: crystal polymorphism, risperidone, SCF-micronization, SCFincapsulation, rapid expansion of supercritical solutions, supercritical antisolvent preci pitation, particles from gas saturated solutions

Polymorph transformations of risperidone during its micronization and encapsulation
into aliphatic polyesters (polylactide and polylactoglycolide) using supercritical carbon
dioxide were studied. It was shown that during SAS (Supercritical Anti-Solvent) and
RESS (Rapid Expansion of Supercritical Solutions) micronization of risperidone,
which initially had polymorphic form A it crystallized into a less thermodynamically
stable form B. In case of SAS method, this transition is complete; in case of RESS, it is
partial. During PGSS (Particles from Gas Saturated Solutions), encapsulation of
micronized B-form into polylactides or polylactoglycolides as well as during
monolythization with subsequent cryomilling (MSC) B-risperidone partially turns
back into A-form. Whereas MSC-micronization of initial А-risperidone with its
subsequent PGSS or MSC encapsulation into polylactides or polylactoglycolides does
not cause any change in polymorph state of this substance, it remains in А-form.

doi:10.1134/S199079311707003X