Rheological and solid-state NMR assessments of copovidone/clotrimazole model solid dispersions.

作者: Fengyuan Yang , Yongchao Su , Lei Zhu , Chad D. Brown , Lawrence A. Rosen

DOI: 10.1016/J.IJPHARM.2016.01.026

关键词:

摘要: This study aims to assess several model solid dispersions by using dynamic oscillatory rheology, solid-state NMR and other phase characterization techniques, correlate their viscoelastic responses with processing methods microstructures. A active pharmaceutical ingredient (API), clotrimazole, was compounded copovidone form via various techniques different mixing capabilities. Physicochemical characterizations of the resulting demonstrated that simple physical led a poorly mixed blend manifested existence large API crystalline content heterogeneous distribution. Cryogenic milling significantly improved two components as result reduced particle size increased contact surface area, but produced limited amorphous content. In contrast, hot melt extrusion (HME) resulted in homogenous dispersion because its inherent efficiency. Storage modulus viscosities versus frequency indicated incorporation into polymer matrix plasticizing effect which viscosity. The crystalline/aggregated forms also exhibited more elastic response than amorphous/dispersed counterpart. Temperature ramps mixture high concentration captured critical temperature, at bump observed damping factor. attributed dissolution polymer. addition, heating-cooling cycles suggested cryomilling HME could homogeneous low content, whereas drug relatively unstable due supersaturation

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