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Dissolution-modulating mechanism of pH modifiers in solid dispersion containing weakly acidic or basic drugs with poor water solubility
journal contribution
posted on 2010-01-01, 00:00 authored by Phuong TranPhuong Tran, Thao Truong-Dinh Tran, Kyoung-Ho Lee, Dong-Jin Kim, Beom-Jin LeeIMPORTANCE OF THE FIELD: Although the solid dispersion method has been known to increase the dissolution rate of poorly water-soluble drugs by dispersing them in hydrophilic carriers, one obstacle of the solid dispersion method is its limited solubilization capacity, especially for pH-dependent soluble drugs. AREAS COVERED IN THIS REVIEW: pH-modified solid dispersion, in which pH modifiers are incorporated, may be a useful method for increasing the dissolution rate of weakly acidic or basic drugs. Sufficient research, including the most recent reports, was undertaken in this review. WHAT THE READER WILL GAIN: How could the inclusion of the pH the pH modifiers in the solid dispersion system change drug structural behaviors, molecular interactions, microenvironmental pH, and/or release rate of pH modifiers, relating with the enhanced dissolution of weakly acidic or weakly basic drugs with poor water solubility? These questions have been investigated to determine the dissolution-modulating mechanism of pH modifiers in solid dispersion containing weakly acidic or basic drugs. TAKE HOME MESSAGE: It is believed that step-by-step mechanistic approaches could provide the ultimate solution for solubilizing several poorly water-soluble drugs with pH-dependent solubility from a solid dispersion system, as well as provide ideas for developing future dosage systems.
History
Journal
Expert opinion on drug deliveryVolume
7Issue
5Pagination
647 - 661Publisher
Taylor & FrancisLocation
Abingdon, Eng.Publisher DOI
eISSN
1744-7593Language
engPublication classification
C1.1 Refereed article in a scholarly journalCopyright notice
2010, Informa UK Ltd.Usage metrics
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Delayed-Action PreparationsExcipientsHydrogen-Ion ConcentrationPharmaceutical PreparationsSolubilityScience & TechnologyLife Sciences & BiomedicinePharmacology & PharmacyEXTENDED-RELEASE FORMULATIONDIFFUSION LAYER PHMICROENVIRONMENTAL PHMATRIX TABLETSSOLUBLE DRUGSCITRIC-ACIDPOLYETHYLENE GLYCOL-6000ENHANCED DISSOLUTIONCRYSTAL-GROWTHESTER PRODRUG
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