In this study, we investigated the release mechanism of the poorly water soluble drug aprepitant from different amorphous solid dispersions using confocal Raman microscopy (CRM). Solid dispersions were fabricated based on either Soluplus®, as an amphiphilic copolymer and solubilizer, or on polyvinylpyrrolidone, as a hydrophilic polymer, in order to elucidate the influence of the polymer characteristics on the drug form and dissolution mechanisms. Aprepitant exhibited its amorphous form in both solid dispersions. However, the release differed depending on the polymer. The high complexation effect of Soluplus was shown to be a crucial factor for stabilization of the amorphous drug, resulting in continuous release without any recrystallization of aprepitant. In contrast, solid dispersions based on polyvinylpyrrolidone showed a different mechanism of dissolution; due to the good affinity of PVP and water, the polymer is dissolving fast, leading to phase separation and local recrystallization of the drug. The study highlights the complexity of release processes from solid dispersions and elucidates the influence of the polymer on drug release kinetics.

Department of Biopharmaceutics and Pharmaceutical Technology Saarland University Saarbruecken Germany; Helmholtz Centre for Infection Research Department of Drug Delivery Saarbruecken Germany

Department of Chemical Engineering University of Chemistry and Technology Prague Prague 6 Czech Republic

Department of Chemical Engineering University of Chemistry and Technology Prague Prague 6 Czech Republic; Zentiva k s U Kabelovny 130 Prague 10 Czech Republic

Zentiva k s U Kabelovny 130 Prague 10 Czech Republic

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The Combined Use of Imaging Approaches to Assess Drug Release from Multicomponent Solid Dispersions