Mechanism of drug release from polymethacrylate-based extrudates and milled strands prepared by hot-melt extrusion.
作者： Jessica Albers , Rainer Alles , Karin Matthée , Klaus Knop , Julia Schulze Nahrup
DOI: 10.1016/J.EJPB.2008.10.002
关键词: Chemical engineering 、 Organic chemistry 、 Extrusion 、 Melting point 、 Solid solution 、 Recrystallization (geology) 、 Acrylate polymer 、 Materials science 、 Amorphous solid 、 Dissolution 、 Supersaturation
摘要: The aim of the study was formulation solid dispersions poorly water-soluble drug celecoxib and a polymethacrylate carrier by hot-melt extrusion. objectives were to elucidate mechanism release from obtained extrudates milled strands addicted solid-state properties examine eliminate stability problems occurring under storage, exposure mechanical stress, in vitro dissolution. Transparent containing up 60% could be prepared with temperature setting below melting point celecoxib. XRPD DSC measurements indicated formation glassy solution, where is molecularly dispersed carrier. amorphous state solution maintained during stress milling process, stable storage for at least 6 months. Solid-state SEM images after dissolution carrier-controlled dissolution, whereby within concentrated layer. showed 58-fold supersaturation 0.1 N HCl first 10 min, which followed recrystallization process. Recrystallization inhibited an external addition HPMC.
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