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説明:

Amorphous solid dispersion (ASD) is one of the most important enabling formulation technologies for the development of poorly soluble drugs. Because of its thermodynamically unstable nature in both solid and wet states, the evaluation and optimization of the formulation performance involves some difficulties. The dissolution process is sensitively influenced by various factors, including the applied dose, medium composition, and pH. Supersaturated solutions can cause liquid–liquid phase separation (LLPS) and/or crystallization, which complicates the comprehension of the dissolution process. However, LLPS should be evaluated carefully because it is closely related to oral absorption. As LLPS concentration is analogous to amorphous solubility, it can be a key factor in predicting oral absorption from ASDs, if absorption is limited by solubility. Moreover, LLPS droplets are expected to increase transmembrane flux by increasing the drug concentration near the epithelial cell membrane. In this review, recently updated knowledge on the dissolution, membrane permeation, and oral absorption behaviors of ASDs is discussed with an emphasis on LLPS behavior.

権利情報:

• Creative Commons BY Attribution 4.0 International
  

キーワード: Amorphous solid dispersion, Crystallizaion, Supersaturation, Liquid–liquid phase separation, Membrane permeability, Oral absorption

刊行年月日: 2025-02-16

出版者: MDPI AG

掲載誌:

• Pharmaceutics (ISSN: 19994923) vol. 17 issue. 2 262

研究助成金:

原稿種別: 出版者版 (Version of record)

MDR DOI:

公開URL: https://doi.org/10.3390/pharmaceutics17020262

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更新時刻: 2025-04-30 12:30:20 +0900

MDRでの公開時刻: 2025-04-30 12:23:10 +0900