Journal ArticleDOI
High-throughput crystallization: polymorphs, salts, co-crystals and solvates of pharmaceutical solids
Sherry L. Morissette,Orn Almarsson,Matthew Peterson,Julius F. Remenar,Michael Read,Anthony V. Lemmo,Steve Ellis,Michael J. Cima,Colin R. Gardner +8 more
TLDR
The impact of form diversity encompasses issues of stability and bioavailability, as well as development considerations such as process definition, formulation design, patent protection and regulatory control.About:
This article is published in Advanced Drug Delivery Reviews.The article was published on 2004-02-23. It has received 1096 citations till now.read more
Citations
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Journal ArticleDOI
Salt formation to improve drug solubility.
TL;DR: Physicochemical principles of salt solubility are presented, with special reference to the influence of pH-solubility profiles of acidic and basic drugs on salt formation and dissolution.
Journal ArticleDOI
Crystal engineering of active pharmaceutical ingredients to improve solubility and dissolution rates.
TL;DR: The concept and theory of crystal engineering is covered and the potential benefits, disadvantages and methods of preparation of co-crystals, metastable polymorphs, high-energy amorphous forms and ultrafine particles are discussed.
Journal ArticleDOI
Strategies to Address Low Drug Solubility in Discovery and Development
Hywel David Williams,Natalie L. Trevaskis,Susan A. Charman,Ravi Mysore Shanker,William N. Charman,Colin W. Pouton,Christopher J.H. Porter +6 more
TL;DR: The article provides an integrated and contemporary discussion of current approaches to solubility and dissolution enhancement but has been deliberately structured as a series of stand-alone sections to allow also directed access to a specific technology where required.
Journal ArticleDOI
Crystal engineering: from molecule to crystal.
TL;DR: This Perspective provides a brief historical introduction to crystal engineering itself and an assessment of the importance and utility of the supramolecular synthon, which is one of the most important concepts in the practical use and implementation of crystal design.
Journal ArticleDOI
Crystal engineering of the composition of pharmaceutical phases. Do pharmaceutical co-crystals represent a new path to improved medicines?
TL;DR: The evolution of crystal engineering into a form of supramolecular synthesis is discussed in this article in the context of problems and opportunities in the pharmaceutical industry, and it has become clear that a wide array of multiple component pharmaceutical phases, so called pharmaceutical co-crystals, can be rationally designed using crystal engineering, and the strategy affords new intellectual property and enhanced properties for pharmaceutical substances.
References
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Journal ArticleDOI
Drug-like properties and the causes of poor solubility and poor permeability
TL;DR: There are currently about 10000 drug-like compounds, and true diversity does not exist in experimental combinatorial chemistry screening libraries because current ADME experimental screens are multi-mechanisms, and predictions get worse as more data accumulates.
Journal ArticleDOI
Crystal growth
TL;DR: This report introduces briefly some concepts and materials on crystal growth presented by Dr. Zhen-yu Zhang from the Oak Ridge (TN) National Laboratory, and Dr. En-ge Wang from the Institute of Physics, Chinese Academy of Sciences in a session on Crystal growth at the first Chinese-American Frontiers of Science Symposium.
Book
Polymorphism in Molecular Crystals
TL;DR: This chapter discusses polymorphism in pigments and dyes, its applications in pharmaceuticals and high energy materials, and its role in patents.
Book
Polymorphism in Pharmaceutical Solids
TL;DR: Brittain et al. as mentioned in this paper applied the phase rule to the characterisation of polymorphic and solvatomorphic systems, and proposed a computational method to predict polymorphism.
Book ChapterDOI
Crystalline Polymorphism of Organic Compounds
TL;DR: A wide variety of techniques appropriate to the study of organic crystalline polymorphism and pseu-dopolymorphism is then surveyed, ranging from simple crystal density measurement to observation of polymorphic transformations using variable-temperature synchrotron X-ray diffraction methods.