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固形分散体製剤×Caco-2細胞透過性アッセイ×f1/f2 類似度因子(Dissolution f1/f2 Similarity Factor)×
分野薬理学薬理学薬理学
系統Process / pipelineProcess / pipelineProcess / pipeline
提唱年197119891996
提唱者William Chiou and Solomon RiegelmanIngrid HidalgoJames Moore and Hector Flanner
種類solubility enhancementabsorption screeningsimilarity testing
原典Chiou, 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 ↗
別名solid solution, amorphous dispersion, polymer-based formulationCaco-2 assay, intestinal permeability, ADME screeningf1, f2, similarity factor
関連333
概要Solid 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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ScholarGate手法を比較: Solid Dispersion · Caco-2 Permeability · Dissolution f1/f2 Similarity. 2026-06-19に以下より取得 https://scholargate.app/ja/compare