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

International Journal of Pharmaceutics
Fengyuan YangKenneth J Rosenberg

Abstract

This study aims to assess several model solid dispersions by using dynamic oscillatory rheology, solid-state NMR and other solid phase characterization techniques, and correlate their viscoelastic responses with processing methods and microstructures. A model active pharmaceutical ingredient (API), clotrimazole, was compounded with copovidone to form solid dispersions via various techniques with different mixing capabilities. Physicochemical characterizations of the resulting solid dispersions demonstrated that simple physical mixing led to a poorly mixed blend manifested by existence of large API crystalline content and heterogeneous distribution. Cryogenic milling significantly improved mixing of two components as a result of reduced particle size and increased contact surface area, but produced limited amorphous content. In contrast, hot melt extrusion (HME) processing resulted in a homogenous amorphous solid dispersion because of its inherent mixing efficiency. Storage modulus and viscosities versus frequency of different solid dispersions indicated that the incorporation of API into the polymer matrix resulted in a plasticizing effect which reduced the viscosity. The crystalline/aggregated forms of API also exhibited more ...Continue Reading

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Citations

Oct 23, 2016·Journal of Pharmaceutical Sciences·Sarsvat PatelChangquan Calvin Sun
Apr 26, 2021·European Journal of Pharmaceutics and Biopharmaceutics : Official Journal of Arbeitsgemeinschaft Für Pharmazeutische Verfahrenstechnik E.V·Fengyuan YangJames DiNunzio
Mar 9, 2019·Molecular Pharmaceutics·Justyna Knapik-KowalczukMarian Paluch
Aug 2, 2017·The Journal of Physical Chemistry. B·Qing Zhe NiYongchao Su
Nov 4, 2021·AAPS PharmSciTech·Ludmila A G PinhoMarcilio Cunha-Filho

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