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固体分散体制剂×Caco-2 细胞渗透性测定×溶出度f1/f2相似因子×脂质体药物递送×
领域药理学药理学药理学药理学
方法族Process / pipelineProcess / pipelineProcess / pipelineProcess / pipeline
起源年份1971198919961965
提出者William Chiou and Solomon RiegelmanIngrid HidalgoJames Moore and Hector FlannerAlec Bangham
类型solubility enhancementabsorption screeningsimilarity testingformulation technology
开创性文献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 ↗
别名solid solution, amorphous dispersion, polymer-based formulationCaco-2 assay, intestinal permeability, ADME screeningf1, f2, similarity factorliposomal formulation, vesicular delivery, lipid nanoparticles
相关3333
摘要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方法对比: Solid Dispersion · Caco-2 Permeability · Dissolution f1/f2 Similarity · Liposome Encapsulation. 于 2026-06-19 检索自 https://scholargate.app/zh/compare