PDF(Pubmed)
Abstract：
This review discusses the entire progress made on the anthelmintic drug praziquantel, focusing on the solid state and, therefore, on anhydrous crystalline polymorphs, amorphous forms, and multicomponent systems (i.e., hydrates, solvates, and cocrystals). Despite having been extensively studied over the last 50 years, new polymorphs and the greater part of their cocrystals have only been identified in the past decade. Progress in crystal engineering science (e.g., the use of mechanochemistry as a solid form screening tool and more strategic structure-based methods), along with the development of analytical techniques, including Synchrotron X-ray analyses, spectroscopy, and microscopy, have furthered the identification of unknown crystal structures of the drug. Also, computational modeling has significantly contributed to the prediction and design of new cocrystals by considering structural conformations and interactions energy. Whilst the insights on praziquantel polymorphs discussed in the present review will give a significant contribution to controlling their formation during manufacturing and drug formulation, the detailed multicomponent forms will help in designing and implementing future praziquantel-based functional materials. The latter will hopefully overcome praziquantel\'s numerous drawbacks and exploit its potential in the field of neglected tropical diseases.
摘要：
这篇综述讨论了驱虫药物吡喹酮的全部进展，专注于固态，因此,关于无水结晶多晶型物，无定形形式，和多组分系统(即，水合物,溶剂化物，和共晶）。尽管在过去的50年里进行了广泛的研究，新的多晶型物和大部分的共晶在过去十年才被发现。晶体工程科学的进展(例如，使用机械化学作为固体形式筛选工具和更具战略性的基于结构的方法)，随着分析技术的发展，包括同步加速器X射线分析，光谱学,和显微镜,进一步鉴定了未知的药物晶体结构。此外，通过考虑结构构象和相互作用能，计算模型为新共晶的预测和设计做出了重要贡献。虽然本综述中讨论的吡喹酮多晶型物的见解将对控制其在制造和药物配制过程中的形成做出重大贡献，详细的多组分形式将有助于设计和实施未来的吡喹酮基功能材料。后者有望克服吡喹酮的众多缺点，并在被忽视的热带病领域发挥其潜力。
