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Formulation par dispersion solide×Essai de perméabilité des cellules Caco-2×Facteur de similarité f1/f2 pour la dissolution×
DomainePharmacologiePharmacologiePharmacologie
FamilleProcess / pipelineProcess / pipelineProcess / pipeline
Année d'origine197119891996
Auteur d'origineWilliam Chiou and Solomon RiegelmanIngrid HidalgoJames Moore and Hector Flanner
Typesolubility enhancementabsorption screeningsimilarity testing
Source fondatriceChiou, W. L., Riegelman, S. (1971). Pharmaceutical applications of solid dispersions. Journal of Pharmaceutical Sciences, 60(9), 1281-1302. link ↗Hidalgo, I. J., Raub, T. J., & Borchardt, R. T. (1989). Characterization of the human colon carcinoma cell line (Caco-2) as a model system for intestinal epithelial permeability. Gastroenterology, 96(3), 736-749. DOI ↗Moore, J. W., & Flanner, H. H. (1996). Mathematical comparison of dissolution profiles. Pharmaceutical Technology, 20(6), 64-74. link ↗
Aliassolid solution, amorphous dispersion, polymer-based formulationCaco-2 assay, intestinal permeability, ADME screeningf1, f2, similarity factor
Apparentées333
RésuméSolid dispersion is a formulation technique where a poorly soluble drug is molecularly dispersed in a hydrophilic polymer matrix, improving aqueous solubility and bioavailability. Introduced by Chiou and Riegelman in 1971, solid dispersions remain a key strategy for overcoming solubility-limited absorption.The Caco-2 assay is an in vitro model system using human colon carcinoma cell monolayers to screen drug intestinal permeability. Developed by Hidalgo and colleagues in 1989, Caco-2 cells differentiate into an epithelial barrier resembling intestinal mucosa, enabling rapid assessment of drug absorption potential and identification of transporter-mediated transport.The f1 and f2 factors are dimensionless statistical measures developed by Moore and Flanner to quantify the similarity between two dissolution profiles. Adopted by regulatory agencies (FDA, EMA) as the gold standard for comparing dissolution curves, these factors enable rapid assessment of whether formulation changes significantly impact drug release.
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ScholarGateComparer des méthodes: Solid Dispersion · Caco-2 Permeability · Dissolution f1/f2 Similarity. Consulté le 2026-06-19 sur https://scholargate.app/fr/compare