A novel lurasidone hydrochloride–shikimic acid co-amorphous system formed by hydrogen-bonding interaction with the retained pH-dependent solubility behavior,CrystEngComm

当前位置： X-MOL 学术 › CrystEngComm › 论文详情

Our official English website, www.x-mol.net, welcomes your feedback! (Note: you will need to create a separate account there.)

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

点击分享查看原文

点击收藏

阅读更多本刊最新论文本刊介绍/投稿指南11