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Physicochemical principles of controlled release solid dispersion containing a poorly water-soluble drug
journal contribution
posted on 2010-07-01, 00:00 authored by Thao Truong-Dinh Tran, Phuong TranPhuong Tran, Jisung Lim, Jun Bom Park, Soon-Kuk Choi, Beom-Jin LeeBACKGROUND: The aim of this study was to investigate the physicochemical properties of polyethylene oxide (PEO)-based controlled release solid dispersions (CR-SDs) containing aceclofenac, Gelucire 44/14, poloxamer 407 and pH modifier (Na2CO3). RESULTS: The immediate release solid dispersions containing the pH modifier greatly enhanced the drug dissolution rate to approximately 100%, while the CR-SDs with PEO showed controlled release. A bigger droplet size and a higher surface charge for the CR-SDs were observed compared with the immediate release solid dispersions. The pH modifier played an important role in modulating the release rate of the drug through changes in the drug crystallinity and the hydrogen-bonding interaction, as well as the microenvironmental pH. Near-infrared images revealed a modulation of the PEO concentration to preserve the pH modifier within the system for controlled release of the drug. CONCLUSION: The dissolution process of PEO-based solid dispersions containing a water-insoluble drug was governed by the changing net effect of the microenvironmental pH, the surface charge, the particle size and the release rate of the pH modifier, as well as the function of PEO in controlling drug release.
History
Journal
Therapeutic deliveryVolume
1Issue
1Pagination
51 - 62Publisher
Future ScienceLocation
London, Eng.Publisher DOI
ISSN
2041-5990Language
engPublication classification
C1.1 Refereed article in a scholarly journalCopyright notice
2010, Future Science LtdUsage metrics
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No categories selectedKeywords
Anti-Inflammatory Agents, Non-SteroidalChemistry, PharmaceuticalDelayed-Action PreparationsDiclofenacDrug CarriersDrug CompoundingHydrogen BondingHydrogen-Ion ConcentrationKineticsParticle SizePoloxamerPolyethylene GlycolsSodium BicarbonateSolubilitySolventsSurface PropertiesTechnology, PharmaceuticalWaterScience & TechnologyLife Sciences & BiomedicinePharmacology & Pharmacy
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