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Dissolution enhancement of poorly water-soluble APIs processed by hot-melt extrusion using hydrophilic polymers

Dissolution enhancement of poorly water-soluble APIs processed by hot-melt extrusion using hydrophilic polymers

Maniruzzaman, M., Rana, M.M., Boateng, J. S. ORCID: 0000-0002-6310-729X, Mitchell, J. C. ORCID: 0000-0003-2945-3292 and Douroumis, D. (2013) Dissolution enhancement of poorly water-soluble APIs processed by hot-melt extrusion using hydrophilic polymers. Drug Development and Industrial Pharmacy, 39 (2). pp. 218-227. ISSN 0363-9045 (Print), 1520-5762 (Online) (doi:10.3109/03639045.2012.670642)

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Abstract

The aim of this study was to investigate the efficiency of hydrophilic polymers to enhance the dissolution rate of poorly water-soluble active pharmaceutical ingredients (APIs) processed by hot-melt extrusion (HME). Indomethacin (INM) and famotidine (FMT) were selected as model active substances while polyvinyl caprolactam graft copolymer, soluplus (SOL) and vinylpyrrolidone-vinyl acetate copolymer grades, Kollidon VA64 (VA64) and Plasdone S630 (S630) were used as hydrophilic polymeric carriers. For the purpose of the study, drug–polymer binary blends at various ratios were processed by a Randcastle single screw extruder. The physicochemical properties and the morphology of the extrudates were evaluated through X-ray diffraction (XRD), differential scanning calorimetry (DSC) and scanning electron microscopy (SEM). Increased drug loadings of up to 40% were achieved in the extruded formulations for both drugs. INM and FMT exhibited strong plasticization effects with increasing concentrations and were found to be molecularly dispersed within the polymer blends. The in vitro dissolution studies showed increased INM/FMT release rates for all formulations compared to that of pure APIs alone.

Item Type: Article
Uncontrolled Keywords: hot-melt extrusion, dissolution enhancement, solid dispersions, hydrophilic polymers, insoluble drugs
Subjects: R Medicine > RS Pharmacy and materia medica
Faculty / Department / Research Group: Faculty of Engineering & Science > Department of Pharmaceutical, Chemical & Environmental Sciences
Related URLs:
Last Modified: 06 Dec 2016 12:05
Selected for GREAT 2016: None
Selected for GREAT 2017: None
Selected for GREAT 2018: None
URI: http://gala.gre.ac.uk/id/eprint/8237

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