A novel lurasidone hydrochloride–shikimic acid co-amorphous system formed by hydrogen-bonding interaction with the retained pH-dependent solubility behavior. Issue 35 (20th August 2020)

• Record Type: Journal Article
• Authors: Hu, Yi; Jiang, Cuiping; Li, Bin; Zhou, Lijing; Xu, Renjie; Guo, Yujie; Cao, Yan; Cao, Guosheng; Lu, Shan
• Is Part Of: CrystEngComm. Volume 22:Issue 35(2020)
• Page Start: 5841
• Page End: 5853
• Publication Date: 2020-08-20
• Subjects: Crystals -- Periodicals; Crystal growth -- Periodicals; Crystallography -- Periodicals; Cristaux -- Périodiques; Cristaux -- Croissance -- Périodiques; Cristallographie -- Périodiques; 548
• DOI: 10.1039/d0ce00952k
• Languages: English
• ISSNs: 1466-8033

Abstract

Abstract : The current study was aimed at investigating the lurasidone hydrochloride–shikimic acid co-amorphous system using a new type of organic acid. Abstract : 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.