Tags

Type your tag names separated by a space and hit enter

Dissolution enhancement of poorly water-soluble APIs processed by hot-melt extrusion using hydrophilic polymers.
Drug Dev Ind Pharm. 2013 Feb; 39(2):218-27.DD

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.

Authors+Show Affiliations

School of Science, University of Greenwich, Chatham, Kent, UK.No affiliation info availableNo affiliation info availableNo affiliation info availableNo affiliation info available

Pub Type(s)

Journal Article

Language

eng

PubMed ID

22452601

Citation

Maniruzzaman, M, et al. "Dissolution Enhancement of Poorly Water-soluble APIs Processed By Hot-melt Extrusion Using Hydrophilic Polymers." Drug Development and Industrial Pharmacy, vol. 39, no. 2, 2013, pp. 218-27.
Maniruzzaman M, Rana MM, Boateng JS, et al. Dissolution enhancement of poorly water-soluble APIs processed by hot-melt extrusion using hydrophilic polymers. Drug Dev Ind Pharm. 2013;39(2):218-27.
Maniruzzaman, M., Rana, M. M., Boateng, J. S., Mitchell, J. C., & 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), 218-27. https://doi.org/10.3109/03639045.2012.670642
Maniruzzaman M, et al. Dissolution Enhancement of Poorly Water-soluble APIs Processed By Hot-melt Extrusion Using Hydrophilic Polymers. Drug Dev Ind Pharm. 2013;39(2):218-27. PubMed PMID: 22452601.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Dissolution enhancement of poorly water-soluble APIs processed by hot-melt extrusion using hydrophilic polymers. AU - Maniruzzaman,M, AU - Rana,M M, AU - Boateng,J S, AU - Mitchell,J C, AU - Douroumis,D, Y1 - 2012/03/28/ PY - 2012/3/29/entrez PY - 2012/3/29/pubmed PY - 2013/7/26/medline SP - 218 EP - 27 JF - Drug development and industrial pharmacy JO - Drug Dev Ind Pharm VL - 39 IS - 2 N2 - 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. SN - 1520-5762 UR - https://www.unboundmedicine.com/medline/citation/22452601/Dissolution_enhancement_of_poorly_water_soluble_APIs_processed_by_hot_melt_extrusion_using_hydrophilic_polymers_ L2 - https://www.tandfonline.com/doi/full/10.3109/03639045.2012.670642 DB - PRIME DP - Unbound Medicine ER -