2011, №4

сс. 88-102

Supercritical fluid micronization of risperidone

2011, №4

сс. 88-102

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V.N. Bagratashvili, A.M. Egorov, L.I. Krotova, A.V. Mironov, V.Ya. Panchenko, O.O. Parenago, V.K. Popov, I.A. Revelsky, P.S. Timashev, S.I. Tsypina

Key words: SCF micronization, risperidone, polymorphism

Comparative  studies of supercritical fluid micro nization processes of 50-100 mm size  risperidone pharmaceutical substrate using RESS and SAS approaches are  performed to enhance its bioavailability in human body. Both micronization  approaches allow obtaining risperidone microparticles of 5-20 mm size. SAS  approach, however, is more preferable for effective risperidone micronization,  since unlike RESS it doesn't cause any detectable contamination of risperidone  with organic co-solvent residuals (used in these processes) and also allows  obtaining risperidone microparticles of different shapes. It was revealed that  SAS micronization process causes a change of risperidone polymorphous form from  triclinic to monoclinic.

doi:10.1134/S1990793112070019