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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 / pipeline | Process / pipeline | Process / pipeline |
| 提唱年≠ | 1971 | 1989 | 1996 |
| 提唱者≠ | William Chiou and Solomon Riegelman | Ingrid Hidalgo | James Moore and Hector Flanner |
| 種類≠ | solubility enhancement | absorption screening | similarity 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 formulation | Caco-2 assay, intestinal permeability, ADME screening | f1, f2, similarity factor |
| 関連 | 3 | 3 | 3 |
| 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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