通过协同实验和模拟方法揭示I型强的松龙在13种纯溶剂中的固液平衡行为

IF 2 3区 工程技术 Q3 CHEMISTRY, MULTIDISCIPLINARY
Xiaofang Luo, Yuntian Xiao, Linlin Shi, Lingli Hou, Yongkang Liu, Ling Zhou* and Qiuxiang Yin*, 
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引用次数: 0

摘要

强的松龙(PDL)是一种广泛用于治疗过敏性和自身免疫性炎症疾病的皮质类固醇,由于其水溶性较差,在临床应用中受到限制。因此,掌握不同溶剂之间的固液平衡行为对于促进具有更好生物利用度的固体制剂的开发至关重要。本研究采用重量分析法测量了PDL Form I在13种纯溶剂中的溶解度,并采用分子动力学方法,包括分子静电势表面分析、Hirshfeld表面分析、基于Hirshfeld划分的独立梯度模型、径向分布函数、溶质-溶剂相互作用能计算等,探讨了PDL Form I在13种纯溶剂中的溶解度。PDL Form I在不同溶剂中的溶解度随温度的增加而增加,其中丙酮的溶解度变化最大。径向分布函数分析表明PDL分子与溶剂之间存在多重氢键相互作用。溶质-溶剂相互作用能的计算表明,乙醇与PDL的相互作用能最高,与其溶解度最高相关。通过对Apelblat方程、λh模型、van 't Hoff方程和NRTL方程的拟合,证实了固液平衡数据的有效性,平均相对偏差小于2.5,相关性较好。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Unraveling Solid–Liquid Phase Equilibrium Behavior of Prednisolone Form I in 13 Pure Solvents through Synergistic Experimental and Simulation Approaches

Unraveling Solid–Liquid Phase Equilibrium Behavior of Prednisolone Form I in 13 Pure Solvents through Synergistic Experimental and Simulation Approaches

Prednisolone (PDL), a corticosteroid extensively used in the treatment of allergic and autoimmune inflammatory diseases, faces limitations in clinical application due to its poor water solubility. Consequently, grasping the solid–liquid equilibrium behavior across diverse solvents is imperative for advancing the development of solid formulations with improved bioavailability. This study measured the solubility of PDL Form I in 13 pure solvents using gravimetric analysis and employed molecular dynamics, including molecular electrostatic potential surface analysis, Hirshfeld surface analysis, the independent gradient model based on Hirshfeld partitioning, radial distribution function, and solute–solvent interaction energy calculations, to explore the solid–liquid equilibrium behavior. The solubility of PDL Form I across various solvents exhibited a temperature-dependent increase, showing the largest variation in acetone. Radial distribution function analysis indicated multiple hydrogen-bonding interactions between the PDL molecule and the solvents tested. The calculations of solute–solvent interaction energy revealed that ethanol had the highest interaction energy with PDL, correlating with its the highest solubility. The validity of the solid–liquid equilibrium data was confirmed by fitting to the Apelblat equation, λh model, van’t Hoff equation, and NRTL equation, with an average relative deviation below 2.5, indicating good correlation.

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来源期刊
Journal of Chemical & Engineering Data
Journal of Chemical & Engineering Data 工程技术-工程:化工
CiteScore
5.20
自引率
19.20%
发文量
324
审稿时长
2.2 months
期刊介绍: The Journal of Chemical & Engineering Data is a monthly journal devoted to the publication of data obtained from both experiment and computation, which are viewed as complementary. It is the only American Chemical Society journal primarily concerned with articles containing data on the phase behavior and the physical, thermodynamic, and transport properties of well-defined materials, including complex mixtures of known compositions. While environmental and biological samples are of interest, their compositions must be known and reproducible. As a result, adsorption on natural product materials does not generally fit within the scope of Journal of Chemical & Engineering Data.
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