イブプロフェンとエンパグリフロジンの溶解を水中深層溶媒システムで調査する:実験的および熱力学モデリングの洞察
Shadi Janfaza1, Ali Haghtalab2
1Department of Processing, Faculty of Chemical Engineering, Tarbiat Modares University, P.O. Box 14115-143, Tehran, Iran.
Pharmaceutical research
|September 4, 2025
まとめ
この研究では,イブプロフェンやエンパグリフロジンなどの溶解性が低い薬剤の溶解を改善するための深層溶解剤 (DES) を調査した. より高いDES濃度と温度により,薬剤の溶解性が著しく上昇し,UNIQUACモデルはこれらの効果を正確に予測しました.
科学分野:
- 医薬品科学
- 物理化学
- 材料科学
背景:
- 水溶性の低い薬剤は,生物利用性を制限する,重要な製剤の課題を提示します.
- ディープ・ユーテクティック・ソルベンツ (DES) は,調節可能で環境に優しい薬物溶解の代替品です.
- 薬剤と溶剤の相互作用を理解することは 効果的な薬剤投与システムの開発に不可欠です
研究 の 目的:
- イブプロフェン (IBU) とエンパグリフロジン (EMPA) の溶解を促進するテトラブチルフォスフォニウムブロミド (TBPB) とデエチレングリコール (DEG) を含む新型深層溶媒 (DES) の有効性を評価する.
- 薬剤の溶解性および溶解運動に対する変化するDES濃度および温度の影響を調査する.
- 予測精度のための熱力学モデルを使用して,実験的溶解性のデータを相関させる.
主な方法:
- テトラブチルフォスフォニウムブロミド (TBPB) とダイエチレングリコール (DEG) から DESを合成する.
- 11つの質量分数と温度 (20~40°C) で水中のDES溶液におけるIBUとEMPAの表面溶解性を測定する.
- ウィルソン,NRTL,UNIQUACの熱力学モデルを用いた24時間の溶解運動のモニタリングとデータの相関.
主要な成果:
- イブプロフェンとエンパグリフロジンは,DES- 水系での溶解が強化され,イブプロフェンはより高い溶解性を示した.
- 薬剤の溶解性は,より高いDES濃度と高温の両方で増加し,内熱溶解プロセスを示した.
- UNIQUACの熱力学モデルは,実験の溶解データとの相関関係において最も高い精度を示した.
結論:
- TBPB-DEGベースのDESは,水溶性の低い薬剤,イブプロフェンおよびエンパグリフロジンの溶解性と溶解性を効果的に高める.
- 薬物の溶解に影響を与える重要なパラメータは温度とDES濃度であり,陽性相関が観察されました.
- 熱力学モデリング,特にUNIQUACモデルは,DESシステムにおける薬物溶解性を予測し理解するために価値があります.
関連する概念動画
Theories of Dissolution: The Danckwerts' Model and Interfacial Barrier Model
429
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...
429
Factors Influencing Drug Absorption: Drug Dissolution
690
The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
690
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
258
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...
258
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
1.9K
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.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
1.9K
Factors Affecting Dissolution: Particle Size and Effective Surface Area
1.0K
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...
1.0K
Theories of Dissolution: Diffusion Layer Model
919
Dissolution, the process by which drug particles dissolve in a solvent, is explained by the diffusion layer model, a theoretical framework that simulates the absorption of oral drugs and allows us to analyze experimental data.
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
919


