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Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

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Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
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Bioavailability Enhancement: Drug Solubility Enhancement01:16

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Body:Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
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Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

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Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
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Theories of Dissolution: The Danckwerts' Model and Interfacial Barrier Model01:09

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Various dissolution theories provide insight into the factors that influence the dissolution rate. Danckwerts' Model suggests that turbulence, rather than a stagnant layer, characterizes the dissolution medium at the solid-liquid interface. In this model, the agitated solvent contains macroscopic packets that move to the interface via eddy currents, facilitating the absorption and delivery of the drug to the bulk solution. The regular replenishment of solvent packets maintains the...
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Self-Nanoemulsification of Healthy Oils to Enhance the Solubility of Lipophilic Drugs
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マルチクリテリア決定分析と溶解性パラメータモデリングを用いたナノ結晶安定化における表面活性剤の性能の予測と検証

Tanaka Ndongwe1, Pedzisai A Makoni1, Gauta G Matlou2

  • 1Department of Pharmaceutical Sciences, School of Pharmacy, Sefako Makgatho Health Sciences University, Pretoria, South Africa.

European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences
|February 21, 2026
PubMed
まとめ

適切な安定剤の選択は,クルクミンナノ結晶を作るための鍵です. この研究では,ハンセン溶解性パラメータによって予測され,実験的に確認された部分混合性が,最適な品質とサイズに決定的であることを発見しました.

キーワード:
カルキュミンはカルキュミンの成分です.補助物質の互換性についてハンセン溶解性理論ナノ結晶 ナノ結晶トプシス (TOPSIS) とは トプシス (TOPSIS) とは

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Flash NanoPrecipitation for the Encapsulation of Hydrophobic and Hydrophilic Compounds in Polymeric Nanoparticles
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科学分野:

  • 製薬ナノテクノロジー 製薬ナノテクノロジー
  • マテリアルサイエンス 材料科学
  • コンピューティング・ケミストリー

背景:

  • カルキュミン (CUR) は水溶性の低い薬剤 (BCSクラスIV) である.
  • 安定したナノ結晶 (NCs) の開発は,CURの生物利用性を改善するために不可欠です.
  • 安定剤の合理的な選択は難しいが,ナノ結晶の製造には極めて重要です.

研究 の 目的:

  • カルクミンナノ結晶 (CUR-NC) 生産における合理的な安定剤選択のための統合的枠組みを開発する.
  • ハンセン溶解性パラメータ (HSP) 理論と実験的検証を使用して7つの表面活性物質の有効性を評価する.
  • 望ましい粒子のサイズと低ポリ分散性を有する高品質のCUR-NCを生産するための最適な条件を特定する.

主な方法:

  • ハンセン溶解性パラメータ (HSP) 理論を薬-表面活性剤の混合性を予測するために適用する.
  • 表面活性物質の体系的な実験評価のための一般因数学的設計 (DoE).
  • 表面活性剤の濃度が異なるCUR-NCを生産するための湿地加工技術.
  • 粒子サイズ (PS) とポリ分散度指数 (PDI) を重要な品質属性 (CQA) として評価する.
  • 累積加重TOPSISスコア (CWTS) を使用した多基準決定分析.

主要な成果:

  • HSPと相対エネルギー差 (RED) の値は,安定剤と薬物の相互作用を効果的に予測しました.
  • 最適なCUR-NC品質のために,中間混合性/溶解性窓 (ΔδT ≈ 3-6 MPa1⁄2,RED ≈ 0.7-1.0) が特定されました.
  • TPGS 1000とTween 20は,CUR-NC製造のための最も効果的な安定剤として特定されました.
  • 部分混合性は,ナノ結晶の安定化に成功するための重要な要因として確認されました.

結論:

  • in silico HSPモデリングと実験的実験設計 (DoE) の統合は,製薬ナノ結晶開発のための資源効率的な戦略を提供します.
  • このフレームワークは,合理的な安定剤選択を可能にし,水溶性の低い薬物ナノ結晶の生産を最適化します.
  • この発見は,上から下へのナノ結晶化における安定剤の選択を導くための重要なパラメータとして,部分混合性の使用を支持する.