کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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5820135 | 1557373 | 2013 | 10 صفحه PDF | دانلود رایگان |
Polymeric matrices loaded with 10-50% ketoprofen were prepared by hot-melt extrusion or spray-drying. Eudragit® E, PVP, PVPVA and HPMC were studied as matrix formers. Binary “drug-Eudragit® E” as well as ternary “drug-Eudragit® E-PVP”, “drug-Eudragit® E-PVPVA” and “drug-Eudragit® E-HPMC” combinations were investigated and characterized by optical macro/microscopy, SEM, particle size measurements, mDSC, X-ray diffraction and in vitro drug release studies in 0.1Â M HCl. In all cases ketoprofen release was much faster compared to a commercially available product and the dissolution of the drug powder (as received). Super-saturated solutions were obtained, which were stable during at least 2Â h. Importantly, not only the composition of the systems, but also their inner structure potentially significantly affected the resulting ketoprofen release kinetics: For instance, spray-drying ternary ketoprofen:Eudragit® E:HPMC combinations led to a more homogenous HPMC distribution within the systems than hot-melt extrusion, as revealed by mDSC and X-ray diffraction. This more homogenous HPMC distribution resulted in more pronounced hindrance for water and drug diffusion and, thus, slower drug release from spray-dried powder compared to hot-melt extrudates of identical composition. This “homogeneity/heterogeneity effect” even overcompensated the “system size effect”: the surface exposed to the release medium was much larger in the case of the spray-dried powder. All formulations were stable during storage at ambient conditions in open vials.
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Journal: International Journal of Pharmaceutics - Volume 457, Issue 1, 30 November 2013, Pages 298-307