Department of Pharmaceutical Sciences, Faculty of Pharmacy, Jadara University, Irbid, Jordan.
Drug Dev Ind Pharm. 2020 Dec;46(12):2098-2104. doi: 10.1080/03639045.2020.1847136. Epub 2020 Nov 19.
The solubility and solution thermodynamic properties of a weakly water-soluble compound olmesartan medoxomil (OLM) in binary 'polyethylene glycol (PEG-400) + water' cosolvent compositions were determined. The 'mole fraction solubility ( )' of OLM in binary 'PEG-400 + water' cosolvent compositions and pure solvents (PEG-400 and water) was determined at ' = 295.15-330.15 K' and ' = 0.1 MPa'. The Hansen solubility parameter (HSP) of OLM, pure PEG-400, pure water, and binary 'PEG-400 + water' cosolvent compositions free of OLM were also predicted. The obtained values of OLM were correlated using 'van't Hoff, modified Apelblat, Yalkowsky-Roseman, Jouyban-Acree and Jouyban-Acree-van't Hoff' computational models with the error values of <4.0%. The maximum and minimum value of OLM was predicted in neat PEG-400 (1.15 × 10 at = 330.15 K) and neat water (1.90 × 10 at = 295.15 K), respectively. The OLM HSP was predicted to be more close with that of neat PEG-400. The value of OLM was found increased significantly with increase in temperature and PEG-400 mass fraction in all 'PEG-400 + water' cosolvent compositions including neat PEG-400 and neat water. An 'apparent thermodynamic analysis' studies presented an 'endothermic and entropy-driven dissolution' of OLM in all 'PEG-400 + water' cosolvent compositions including pure PEG-400 and pure water.
测定了弱水溶性化合物奥美沙坦酯（OLM）在二元“聚乙二醇（PEG-400）+水”共溶剂体系中的溶解度和溶液热力学性质。在 295.15-330.15 K 和 0.1 MPa 下，测定了 OLM 在二元“PEG-400+水”共溶剂体系和纯溶剂（PEG-400 和水）中的“摩尔分数溶解度（）”。还预测了 OLM、纯 PEG-400、纯水和不含 OLM 的二元“PEG-400+水”共溶剂体系的 Hansen 溶解度参数（HSP）。用 van't Hoff、修正 Apelblat、Yalkowsky-Roseman、Jouyban-Acree 和 Jouyban-Acree-van't Hoff 计算模型对获得的 OLM 值进行了相关性研究，误差值<4.0%。在纯 PEG-400（在 330.15 K 时为 1.15×10）和纯水中（在 295.15 K 时为 1.90×10），预测了 OLM 的最大和最小溶解度。预测 OLM 的 HSP 更接近纯 PEG-400。在所有“PEG-400+水”共溶剂体系中，包括纯 PEG-400 和纯水，OLM 的溶解度值随温度和 PEG-400 质量分数的增加而显著增加。“表观热力学分析”研究表明，在所有“PEG-400+水”共溶剂体系中，包括纯 PEG-400 和纯水，OLM 的溶解是“吸热和熵驱动的”。
