The influence of thermal treatment and type of insoluble poly(meth)acrylates on dissolution behavior of very soluble drug from hypromellose matrix tablets evaluated by multivariate data analysis.
作者： Katerina Kubova , Daniel Peček , Kristýna Hasserová , Petr Doležel , Miroslava Pavelková
DOI: 10.1080/10837450.2016.1193191
关键词: Solubility 、 Polyvinyl alcohol 、 Hypromellose Derivatives 、 Kinetics 、 Granulation 、 Chemistry 、 Cellulose 、 Dissolution 、 Microcrystalline cellulose 、 Chromatography
摘要: Hypromellose matrices exhibit extended burst effect immediately after contact with aqueous medium, especially when a water-soluble drug is incorporated. The objective of this study was to reduce and maintain complete dissolution very soluble levetiracetam over 12 h period from hypromellose K4M obtain zero-order kinetics. Desired changes were achieved by applying water dispersions insoluble Eudragits® (NE, NM, RL, RS) as granulation liquid the drug/microcrystalline cellulose mixture during high-shear (non-thermal treated set) consequently thermally treating granules or final tablets (TT), respectively. Applying Eudragit® recognized an effective method significantly reducing release (25.4-33.7%) in comparison reference sample without Eudragit®. Multivariate data analysis showed that addition reduced effect, increased fitting kinetics, supported matrix erosion supplementary mechanism predominant diffusion. Moreover, resulting PCA sub-model revealed RL thermal treatment be most suitable all. For profile, characterized low close 100% at 12th hour, RL_TT suitable.
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