2015, №3

сс. 26-38

Supercritical Fluid Fabrication of the Components for Risperidon Sustained Release Injectable Formulation

2015, №3

сс. 26-38

Цитировать

V.N. Bagratashvili, S.E. Bogorodski, A.M. Egorov, L.I. Krotova, V.K. Popov, V.I. Sevastyanov

Key words: polymer microparticles, encapsulation of bioactive components, sustained release dosage forms, supercritical carbon dioxide

The process of supercritical fluid encapsulation of pharmaceutical grade risperidon
into bioresorbable D,L-polylactide microparticles by PGSS (Particles from Gas Saturated
Solutions) method is studied. Micronization and change of morphology of risperidon
crystals during its encapsulation into polymer plasticized by supercritical carbon dioxide
is experimentally observed. This finding enabled fabrication of polymer structures of
various dispersion (10—100 μm) and morphologies comprising up to 40 wt.% of
risperidon without any use of organic solvent. The kinetics of risperidon release from
the polymer microparticles into physiological solution is studied by UV-spectrophotometry.
It is shown that the use of different molecular weight D,L-polylactides
enables one to extend the risperidon release time from bioresorbable polymer particles
fabricated by PGSS up to 10 days in a controllable manner.

doi:10.1134/S1990793116070022