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Solvating Effects02:12

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An understanding of the solvating effect helps rationalize the relation between solvation and acidity of the compound. In addition, this also explains the relative stability of conjugate bases for compounds with different pKa values. This lesson details, in-depth, the principle of solvating effects. The strength of an acid and the stability of its corresponding conjugate base are determined using pKa values. This observed relationship is a consequence of solvation, which is the interaction...
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Compared with pure water, the solubility of an ionic compound is less in aqueous solutions containing a common ion (one also produced by dissolution of the ionic compound). This is an example of a phenomenon known as the common ion effect, which is a consequence of the law of mass action that may be explained using Le Chȃtelier’s principle. Consider the dissolution of silver iodide:
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Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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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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Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH01:21

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Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
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Solubility of Ionic Compounds02:55

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Solubility is the measure of the maximum amount of solute that can be dissolved in a given quantity of solvent at a given temperature and pressure. Solubility is usually measured in molarity (M) or moles per liter (mol/L). A compound is termed soluble if it dissolves in water.
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Solubility Equilibria03:07

Solubility Equilibria

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Solubility equilibria are established when the dissolution and precipitation of a solute species occur at equal rates. These equilibria underlie many natural and technological processes, ranging from tooth decay to water purification. An understanding of the factors affecting compound solubility is, therefore, essential to the effective management of these processes. This section applies previously introduced equilibrium concepts and tools to systems involving dissolution and precipitation.
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深層溶媒を用いたアトルバスタチンの溶解性の改善

Yoga Windhu Wardhana1,2, Insan Sunan Kurniawansyah1,2, Taofik Rusdiana1,2

  • 1Department of Pharmaceutics and Pharmaceuticals Technology, Faculty of Pharmacy, Universitas Padjadjaran (UNPAD), Jatinangor, Indonesia.

Journal of advanced pharmaceutical technology & research
|September 3, 2025
PubMed
まとめ

深層エウテクティック溶媒 (DES) はアトルバスタチンカルシウム三水素 (ATCH) の溶解性を高める. プロピレングリコール (PG) に含まれるニコチナミドは,ATCHの溶解性において最適であり,水に対する有意な改善を示した.

キーワード:
アトルバスタチンカルシウム三水素深層エウテクティック溶媒薬の溶解性

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科学分野:

  • 医薬品科学
  • 材料科学

背景:

  • ディープエウテクティック溶剤 (DES) は薬剤に潜力がありますが,安全性および使用可能性の評価が必要です.
  • 薬剤の溶解性を改善することは 薬剤の有効な投与と製剤に不可欠です

研究 の 目的:

  • アトルバスタチンカルシウム三水素 (ATCH) の溶解性を高めるためのDESの可能性を調査する.
  • DESシステム内のニコチナミド (NA) のようなコフォーマーとATCHのユーテクティックな相互作用を探求する.

主な方法:

  • 同結晶化原理を用いて ユーテクティック混合物を形成した.
  • 偏光顕微鏡,フーリエ変換赤外線光譜 (FT-IR),微分スキャン熱計 (DSC) を分析に使用した.
  • DESにおけるATCH,ニコチナミド (NA),プロピレングリコール (PG) の相互作用を評価した.

主要な成果:

  • ニコチナミド (NA) をプロピレングリコール (PG) で利用した最適のDESシステムをATCHで特定した.
  • FT-IRとDSC経由でATCHとDESの間の水素結合 (H結合) の形成が確認されました.
  • 水 (0.000597 ± 0.003 mg/mL) と比較して,DESシステムにおけるATCH溶解性の有意な増加を示した.

結論:

  • 特にニコチナミドがプロピレングリコールにおけるコフォーマーである深層エウテクティック溶媒は,アトルバスタチンカルシウム三水素の溶解性を効果的に高めます.
  • この研究は,ATCHのような溶解性の低い薬剤の溶解性を改善するための実行可能な戦略として,DESの使用を検証しています.
  • 水素結合の相互作用は,DESシステムで観察された溶解性の強化の鍵です.