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Solvates and polymorphs of rebamipide: preparation, characterization, and physicochemical analysis

机译：瑞巴派特的溶剂化物和多晶型物：制备，表征和理化分析

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This study aimed to investigate the solid forms of the peptic ulcer agent rebamipide (RBM). Four RBM solvates, including dimethyl sulfoxide solvate (RBM/DMSO), dichloromethane solvate (RBM/CH2Cl2), hydrate (RBM/H2O), and hemiethanol hemihydrate, were prepared via solvent crystallization. Single crystals of RBM/DMSO and RBM/CH2Cl2 were successfully obtained at 4 °C. These solid forms were both monoclinic with the space group P21/c. Hirshfeld surface and 2D fingerprint plot analyses indicated that RBM/DMSO and RBM/CH2Cl2 showed similarities in hydrogen bonds but exhibited differences in subtle intermolecular interactions. RBM/CH2Cl2 transformed into a novel solid form (form 3) after solvent removal and transformed into another solid form (form 4) when heated at 220 °C. RBM/H2O was converted to form 5 after dehydration. Forms 3–5 were RBM polymorphs. The stability results indicated that RBM/H2O, form 3, and form 4 showed good stability at 40 °C and 75% relative humidity. Furthermore, the three solid forms displayed higher solubility than commercial RBM (form 1) in both water and phosphate buffer solution (PBS). Compared with form 1, RBM/H2O and form 4 showed a comparable and faster dissolution rate in water and PBS, respectively.
机译：这项研究旨在调查消化性溃疡剂瑞巴派特（RBM）的固体形式。四种RBM溶剂化物，包括二甲基亚砜溶剂化物（RBM / DMSO），二氯甲烷溶剂化物（RBM / CH 2 Cl 2 ），水合物（RBM / H 2 O）和半乙醇半水合物通过溶剂结晶法制备。在4°C成功获得了RBM / DMSO和RBM / CH 2 Cl 2 的单晶。这些固体形式都是单斜的，空间群为 P 2 1 / c 。 Hirshfeld表面和二维指纹图分析表明，RBM ​​/ DMSO和RBM / CH 2 Cl 2 在氢键，但表现出细微的分子间相互作用的差异。去除溶剂后，RBM ​​/ CH 2 Cl 2 转化为新型固体形式（形式3）并转化为在220°C加热时，另一种固体形式（形式4）。脱水后，RBM ​​/ H 2 O转化为5。 3-5型是RBM多晶型物。稳定性结果表明，RBM ​​/ H 2 O（3型和4型）在40°C和75％相对湿度下显示出良好的稳定性。此外，这三种固体形式在水和磷酸盐缓冲溶液（PBS）中均显示出比市售RBM（形式1）更高的溶解度。与形式1相比，RBM ​​/ H 2 O和形式4分别在水和PBS中具有可比且更快的溶出速率。

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