{"title":"弹簧和降落伞:共晶如何提高溶解度","authors":"Dhara D. Bavishi, Chetan H. Borkhataria","doi":"10.1016/j.pcrysgrow.2016.07.001","DOIUrl":null,"url":null,"abstract":"<div><p>This article is intended to combine literature on cocrystallization – a tool for enhancing the solubility and for improving the physicochemical properties of an API (an API is the molecule which is responsible for providing the therapeutic effect) with special emphasis on the mechanism responsible for the same. The pharmaceutical industries are witnessing a developing crisis in the process of drug development due to the increasing cost of their R&D departments, the failure of some blockbuster drug candidates exhibiting poor aqueous solubility and the unavailability of newer molecules because of patent limitations. Cocrystallization is an emerging approach to improve solubility, dissolution profile, bioavailability, and other physicochemical and mechanical properties<span><span> of an API. A pharmaceutical cocrystal is now a new epitome which enables the use of a wide range of active pharmaceutical ingredients without the need to form or break the covalent bonds. The prime focus of this review article is the mechanism on how cocrystals have a solubility advantage over the </span>amorphous<span> form. This review also provides a brief introduction to the nature of cocrystals, their role, principles of crystal engineering and also highlights the nature of supramolecular synthons which are present in cocrystals.</span></span></p></div>","PeriodicalId":409,"journal":{"name":"Progress in Crystal Growth and Characterization of Materials","volume":"62 3","pages":"Pages 1-8"},"PeriodicalIF":4.5000,"publicationDate":"2016-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"https://sci-hub-pdf.com/10.1016/j.pcrysgrow.2016.07.001","citationCount":"136","resultStr":"{\"title\":\"Spring and parachute: How cocrystals enhance solubility\",\"authors\":\"Dhara D. Bavishi, Chetan H. Borkhataria\",\"doi\":\"10.1016/j.pcrysgrow.2016.07.001\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><p>This article is intended to combine literature on cocrystallization – a tool for enhancing the solubility and for improving the physicochemical properties of an API (an API is the molecule which is responsible for providing the therapeutic effect) with special emphasis on the mechanism responsible for the same. The pharmaceutical industries are witnessing a developing crisis in the process of drug development due to the increasing cost of their R&D departments, the failure of some blockbuster drug candidates exhibiting poor aqueous solubility and the unavailability of newer molecules because of patent limitations. Cocrystallization is an emerging approach to improve solubility, dissolution profile, bioavailability, and other physicochemical and mechanical properties<span><span> of an API. A pharmaceutical cocrystal is now a new epitome which enables the use of a wide range of active pharmaceutical ingredients without the need to form or break the covalent bonds. The prime focus of this review article is the mechanism on how cocrystals have a solubility advantage over the </span>amorphous<span> form. This review also provides a brief introduction to the nature of cocrystals, their role, principles of crystal engineering and also highlights the nature of supramolecular synthons which are present in cocrystals.</span></span></p></div>\",\"PeriodicalId\":409,\"journal\":{\"name\":\"Progress in Crystal Growth and Characterization of Materials\",\"volume\":\"62 3\",\"pages\":\"Pages 1-8\"},\"PeriodicalIF\":4.5000,\"publicationDate\":\"2016-09-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"https://sci-hub-pdf.com/10.1016/j.pcrysgrow.2016.07.001\",\"citationCount\":\"136\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Progress in Crystal Growth and Characterization of Materials\",\"FirstCategoryId\":\"88\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S0960897416300584\",\"RegionNum\":2,\"RegionCategory\":\"材料科学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q1\",\"JCRName\":\"CRYSTALLOGRAPHY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Progress in Crystal Growth and Characterization of Materials","FirstCategoryId":"88","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S0960897416300584","RegionNum":2,"RegionCategory":"材料科学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q1","JCRName":"CRYSTALLOGRAPHY","Score":null,"Total":0}
Spring and parachute: How cocrystals enhance solubility
This article is intended to combine literature on cocrystallization – a tool for enhancing the solubility and for improving the physicochemical properties of an API (an API is the molecule which is responsible for providing the therapeutic effect) with special emphasis on the mechanism responsible for the same. The pharmaceutical industries are witnessing a developing crisis in the process of drug development due to the increasing cost of their R&D departments, the failure of some blockbuster drug candidates exhibiting poor aqueous solubility and the unavailability of newer molecules because of patent limitations. Cocrystallization is an emerging approach to improve solubility, dissolution profile, bioavailability, and other physicochemical and mechanical properties of an API. A pharmaceutical cocrystal is now a new epitome which enables the use of a wide range of active pharmaceutical ingredients without the need to form or break the covalent bonds. The prime focus of this review article is the mechanism on how cocrystals have a solubility advantage over the amorphous form. This review also provides a brief introduction to the nature of cocrystals, their role, principles of crystal engineering and also highlights the nature of supramolecular synthons which are present in cocrystals.
期刊介绍:
Materials especially crystalline materials provide the foundation of our modern technologically driven world. The domination of materials is achieved through detailed scientific research.
Advances in the techniques of growing and assessing ever more perfect crystals of a wide range of materials lie at the roots of much of today''s advanced technology. The evolution and development of crystalline materials involves research by dedicated scientists in academia as well as industry involving a broad field of disciplines including biology, chemistry, physics, material sciences and engineering. Crucially important applications in information technology, photonics, energy storage and harvesting, environmental protection, medicine and food production require a deep understanding of and control of crystal growth. This can involve suitable growth methods and material characterization from the bulk down to the nano-scale.