International Journal of Pharmaceutics 2013-02-25

Drug-polymer intermolecular interactions in hot-melt extruded solid dispersions.

Mohammed Maniruzzaman, David J Morgan, Andrew P Mendham, Jiayun Pang, Martin J Snowden, Dennis Douroumis

文献索引：Int. J. Pharm. 443(1-2) , 199-208, (2013)

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摘要

The purpose of the study was to investigate and identify the interactions within solid dispersions of cationic drugs and anionic polymers processed by hot-melt extrusion (HME) technique. Propranolol HCl (PRP) and diphenhydramine HCl (DPD) were used as model cationic active substances while pH sensitive anionic methacrylic acid based methyl methacrylate copolymers Eudragit L100 (L100) and ethyl acrylate copolymer Eudragit L100-55 (Acryl EZE) (L100-55) were used as polymeric carriers. The extrudates were further characterised using various physicochemical characterisation techniques to determine the morphology, the drug state within the polymer matrices and the type of drug-polymer interactions. Molecular modelling predicted the existence of two possible H-bonding types while the X-ray photon spectroscopy (XPS) advanced surface analysis of the extrudates revealed intermolecular ionic interactions between the API amino functional groups and the polymer carboxylic groups through the formation of hydrogen bonding. The magnitude of the intermolecular interactions varied according to the drug-polymer miscibility.Copyright © 2012 Elsevier B.V. All rights reserved.