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A novel lurasidone hydrochloride–shikimic acid co-amorphous system formed by hydrogen-bonding interaction with the retained pH-dependent solubility behavior
CrystEngComm ( IF 2.6 ) Pub Date : 2020-08-03 , DOI: 10.1039/d0ce00952k
Yi Hu 1, 2, 3, 4 , Cuiping Jiang 4, 5, 6, 7 , Bin Li 1, 2, 3, 4 , Lijing Zhou 1, 2, 3, 4 , Renjie Xu 1, 2, 3, 4 , Yujie Guo 1, 2, 3, 4 , Yan Cao 1, 2, 3, 4 , Guosheng Cao 1, 2, 3, 4 , Shan Lu 1, 2, 3, 4
Affiliation  

In this work, we report on a novel lurasidone hydrochloride (LH)–shikimic acid (SA) co-amorphous system (LH–SA). It was formed via hydrogen-bonding interaction between LH and SA using a solvent evaporation method. The formation of the LH–SA co-amorphous system was confirmed by the powder X-ray diffraction and differential scanning calorimetry. The intermolecular interaction between LH and SA was explored by FTIR, Raman spectroscopy and molecular dynamic simulation. Interestingly, we found the pH-dependent solubility behavior of the co-amorphous system was retained in the pH range of 1.0–6.8, suggesting that the hydrogen-bonding interaction might not be the main reason for restoring the pH-dependent solubility behavior of LH. The solubility and dissolution rates of the co-amorphous LH–SA system were remarkably improved in comparison with the crystalline LH. We believe that the co-amorphous system might show great potential in enhancing the oral bioavailability of LH.

中文翻译:

通过氢键相互作用与保留的pH依赖的溶解性行为形成的新型盐酸卢拉西酮-shi草酸共非晶体系

在这项工作中,我们报告了一种新型的盐酸卢拉西酮(LH)-shi草酸(SA)共非晶体系(LH-SA)。它是通过LH和SA之间的氢键相互作用采用溶剂蒸发法。粉末X射线衍射和差示扫描量热法证实了LH-SA共非晶体系的形成。通过FTIR,拉曼光谱和分子动力学模拟研究了LH和SA之间的分子间相互作用。有趣的是,我们发现共非晶体系的pH依赖性溶解度行为保持在1.0-6.8的pH范围内,这表明氢键相互作用可能不是恢复LH的pH依赖性溶解性行为的主要原因。 。与结晶LH相比,非晶LH-SA体系的溶解度和溶解速率得到了显着提高。我们相信,该无定形体系可能在增强LH的口服生物利用度方面显示出巨大潜力。
更新日期:2020-09-14
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