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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)×リポソーム薬物送達×
分野薬理学薬理学薬理学薬理学
系統Process / pipelineProcess / pipelineProcess / pipelineProcess / pipeline
提唱年1971198919961965
提唱者William Chiou and Solomon RiegelmanIngrid HidalgoJames Moore and Hector FlannerAlec Bangham
種類solubility enhancementabsorption screeningsimilarity testingformulation technology
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 ↗Bangham, A. D., Standish, M. M., & Watkins, J. C. (1965). Diffusion of univalent ions across the lamellae of swollen phospholipid films and the determination of membrane potential. Journal of Molecular Biology, 13(1), 238-252. DOI ↗
別名solid solution, amorphous dispersion, polymer-based formulationCaco-2 assay, intestinal permeability, ADME screeningf1, f2, similarity factorliposomal formulation, vesicular delivery, lipid nanoparticles
関連3333
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.Liposomal encapsulation is a formulation technique using lipid bilayer vesicles (liposomes) to enclose drugs, improving bioavailability, reducing toxicity, and enabling targeted delivery. Developed by Alec Bangham in 1965, liposomes are now standard in pharmaceutical development, with several FDA-approved liposomal drugs on the market.
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ScholarGate手法を比較: Solid Dispersion · Caco-2 Permeability · Dissolution f1/f2 Similarity · Liposome Encapsulation. 2026-06-19に以下より取得 https://scholargate.app/ja/compare