Download or read book Stability of Amorphous Pharmaceuticals Prediction of Onset of Crystallization Using Experimental Relaxation Times written by Chandan Bhugra and published by . This book was released on 2007 with total page 275 pages. Available in PDF, EPUB and Kindle. Book excerpt: Onset times to crystallization were coupled with dielectric relaxation times in the above Tg temperature range for all compounds (indomethacin, felodipine and flopropione) except nifedipine. Good quantitative agreement between predicted and experimental crystallization onset times was obtained for two compounds (indomethacin and flopropione) at two temperature points below Tg. Crystallization growth rates also coupled with the measured dielectric relaxation times. Though the above protocol may be used as a first step in developing the stability testing protocol for crystallization from amorphous state, clearly compound specific characteristics and critical processing conditions play a significant role in successful use of the protocol.
Download or read book Relaxation Dynamics and Crystallization Kinetics of Glass forming Drugs written by Guadalupe Natalia Ruiz and published by . This book was released on 2018 with total page 162 pages. Available in PDF, EPUB and Kindle. Book excerpt: Glassy phases play an important role in our daily life and in many industries such as the food, pharmaceutical, and construction and are responsible for certain vital mechanisms in living species. Whereas crystals are solid phases that show periodicity of the constituent atoms or molecules, glasses are disordered solids that lack long-range positional order but behave mechanically like solids. Chapter 1 of the current thesis presents an introduction to the characteristics and dynamics of glassy phases. How they are derived from the liquid phase, and how they transform into the crystalline solid phase, thermodynamically more stable. The temperature at which a liquid transforms to the amorphous (glassy) phase is called the glass transition temperature, Tg. Along this thesis the relaxation dynamics of prilocaine (PLC) and stiripentol (STP), and the isothermal crystallization process of the latter have been experimentally studied. Both PLC and STP are drugs used in medical applications mainly as anesthesia and for the treatment of epilepsy, respectively. The studied materials have been analyzed by Broadband Dielectric Spectroscopy (BDS), Differential Scanning Calorimetry, X-Ray diffraction, Raman and I.R spectroscopy and confocal microscopy. The physical principles of BDS, the main experimental tool employed, are presented in Chapter 2. The details of the experimental set-ups are stated in Chapter 3. In the case of a pharmaceutical product, being able to control and foresee the aggregation phase and dissolution rate of the substance is vital. Many drugs are poorly soluble in water and thus, in biological media. The glass state of a drug is a non-equilibrium state that presents higher free energy than the crystal. This implies, that a glassy drug dissolves more rapidly and can be absorbed in larger amounts. Nevertheless, the higher free energy of glassy phases represents at the same time a major problem for shelf-life, since metastable phases are prone to spontaneously transforming into the stable crystalline state. This is a major problem, since wrong dosage or agglomeration of a drug could render it useless or toxic for the human body. Understanding the glass and crystallization dynamics of drugs, and their interaction with water is key to develop more efficient products. Water is the universal biological solvent. For most materials the addition of water leads to a decrease in viscosity, or equivalently, an increase of molecular mobility, resulting in a lower glass transition temperature Tg (the higher the water content the lower the Tg). This is referred to as the plasticizing effect of water. Chapter 4 presents a detailed analysis of both pure and hydrated prilocaine. Results show that the addition of water to PLC leads to the formation of PLC-water complexes, possibly water-bridged monomers or dimers that increase Tg. This antiplasticizing effect of water on the molecular mobility of a simple glass former represents a significant exception to the alleged universality of water as drug plasticizer. The physico-chemical origins of this behavior have been confirmed by studying the effect of confinement of the pure and hydrated drug in the pores of a nonporous structure (Chapter 5). In the case of STP, not only the glassy dynamics were studied, but also the crystallization process (Chapter 6). A sublinear correlation between the characteristic crystal-growth time and the relaxation time of the cooperative relaxation dynamics of stiripentol was found. This correlation was observed also in other substances, which suggests that it is a general correlation at temperatures above Tg. This may allow predicting a substance's crystallization time as a function of temperature. The results of this thesis provide valuable insight into the kinetics and relaxation dynamics, as well as the phase stability, of both studied drugs that could be general to other amorphous drugs. Global conclusions are outlined in Chapter 7.
Download or read book Pharmaceutical Amorphous Solid Dispersions written by Ann Newman and published by John Wiley & Sons. This book was released on 2015-02-27 with total page 505 pages. Available in PDF, EPUB and Kindle. Book excerpt: Providing a roadmap from early to late stages of drug development, this book overviews amorphous solid dispersion technology – a leading platform to deliver poorly water soluble drugs, a major hurdle in today’s pharmaceutical industry. • Helps readers understand amorphous solid dispersions and apply techniques to particular pharmaceutical systems • Covers physical and chemical properties, screening, scale-up, formulation, drug product manufacture, intellectual property, and regulatory considerations • Has an appendix with structure and property information for polymers commonly used in drug development and with marketed drugs developed using the amorphous sold dispersion approach • Addresses global regulatory issues including USA regulations, ICH guidelines, and patent concerns around the world
Download or read book Amorphous Solid Dispersions written by Navnit Shah and published by Springer. This book was released on 2014-11-21 with total page 702 pages. Available in PDF, EPUB and Kindle. Book excerpt: This volume offers a comprehensive guide on the theory and practice of amorphous solid dispersions (ASD) for handling challenges associated with poorly soluble drugs. In twenty-three inclusive chapters, the book examines thermodynamics and kinetics of the amorphous state and amorphous solid dispersions, ASD technologies, excipients for stabilizing amorphous solid dispersions such as polymers, and ASD manufacturing technologies, including spray drying, hot melt extrusion, fluid bed layering and solvent-controlled micro-precipitation technology (MBP). Each technology is illustrated by specific case studies. In addition, dedicated sections cover analytical tools and technologies for characterization of amorphous solid dispersions, the prediction of long-term stability, and the development of suitable dissolution methods and regulatory aspects. The book also highlights future technologies on the horizon, such as supercritical fluid processing, mesoporous silica, KinetiSol®, and the use of non-salt-forming organic acids and amino acids for the stabilization of amorphous systems. Amorphous Solid Dispersions: Theory and Practice is a valuable reference to pharmaceutical scientists interested in developing bioavailable and therapeutically effective formulations of poorly soluble molecules in order to advance these technologies and develop better medicines for the future.
Download or read book Amorphous Drugs written by Marzena Rams-Baron and published by Springer. This book was released on 2018-02-09 with total page 234 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book explains theoretical and technological aspects of amorphous drug formulations. It is intended for all those wishing to increase their knowledge in the field of amorphous pharmaceuticals. Conversion of crystalline material into the amorphous state, as described in this book, is a way to overcome limited water solubility of drug formulations, in this way enhancing the chemical activity and bioavailability inside the body. Written by experts from various fields and backgrounds, the book introduces to fundamental physical aspects (explaining differences between the ordered and the disordered solid states, the enhancement of solubility resulting from drugs amorphization, physical instability and how it can be overcome) as well as preparation and formulation procedures to produce and stabilize amorphous pharmaceuticals. Readers will thus gain a well-funded understanding and find a multi-faceted discussion of the properties and advantages of amorphous drugs and of the challenges in producing and stabilizing them. The book is an ideal source of information for researchers and students as well as professionals engaged in research and development of amorphous pharmaceutical products.
Download or read book Discovering and Developing Molecules with Optimal Drug Like Properties written by Allen C Templeton and published by Springer. This book was released on 2014-10-31 with total page 510 pages. Available in PDF, EPUB and Kindle. Book excerpt: This authoritative volume provides a contemporary view on the latest research in molecules with optimal drug-like properties. It is a valuable source to access current best practices as well as new research techniques and strategies. Written by leading scientists in their fields, the text consists of fourteen chapters with an underlying theme of early collaborative opportunities between pharmaceutical and discovery sciences. The book explores the practical realities of performing physical pharmaceutical and biopharmaceutical research in the context of drug discovery with short timelines and low compound availability. Chapters cover strategies and tactics to enable discovery as well as predictive approaches to establish, understand and communicate risks in early development. It also examines the detection, characterization, and assessment of risks on the solid state properties of advanced discovery and early development candidates, highlighting the link between solid state properties and critical development parameters such as solubility and stability. Final chapters center on techniques to improve molecular solubilization and prevent precipitation, with particularly emphasis on linking physiochemical properties of molecules to formulation selection in preclinical and clinical settings.
Download or read book The Vitreous State written by Ivan S. Gutzow and published by Springer Science & Business Media. This book was released on 2013-11-11 with total page 483 pages. Available in PDF, EPUB and Kindle. Book excerpt: The present book is devoted to problems of a physically important state of condensed matter - the vitreous state. We tried to summarize here the experimental evidence and the different theoretical approaches - structural, thermodynamic and those of statistical physics - connected with the formation, the kinetic stability and with the general nature of glasses as a particular physical state. In addition, a summary is given on the information available concerning proces ses of nucleation and crystallization of glass-forming systems, on methods of preventing or, in contrast, catalyzing crystallization in vitrifying liquids, on the kinetics of nucleation, the modes of crystal growth in undercooled melts and the devitrification of glasses. It was our aim to summarize in the present volume the basic principles and the most significant developments of a newly emerging science - glass science - and to show that, at least, in principle, any substance can exist in the vitreous state. Moreover, we have tried to demonstrate that the characteristic properties of the vitreous state may be attributed under certain conditions not only to systems with an amorphous structure (like the common glasses) but also to a number of other states of condensed matter including the crystalline one.
Download or read book Computational Pharmaceutics written by Defang Ouyang and published by John Wiley & Sons. This book was released on 2015-05-19 with total page 350 pages. Available in PDF, EPUB and Kindle. Book excerpt: Molecular modeling techniques have been widely used in drug discovery fields for rational drug design and compound screening. Now these techniques are used to model or mimic the behavior of molecules, and help us study formulation at the molecular level. Computational pharmaceutics enables us to understand the mechanism of drug delivery, and to develop new drug delivery systems. The book discusses the modeling of different drug delivery systems, including cyclodextrins, solid dispersions, polymorphism prediction, dendrimer-based delivery systems, surfactant-based micelle, polymeric drug delivery systems, liposome, protein/peptide formulations, non-viral gene delivery systems, drug-protein binding, silica nanoparticles, carbon nanotube-based drug delivery systems, diamond nanoparticles and layered double hydroxides (LDHs) drug delivery systems. Although there are a number of existing books about rational drug design with molecular modeling techniques, these techniques still look mysterious and daunting for pharmaceutical scientists. This book fills the gap between pharmaceutics and molecular modeling, and presents a systematic and overall introduction to computational pharmaceutics. It covers all introductory, advanced and specialist levels. It provides a totally different perspective to pharmaceutical scientists, and will greatly facilitate the development of pharmaceutics. It also helps computational chemists to look for the important questions in the drug delivery field. This book is included in the Advances in Pharmaceutical Technology book series.
Download or read book Polymorphism in Pharmaceutical Solids written by Harry G. Brittain and published by CRC Press. This book was released on 2018-11-12 with total page 656 pages. Available in PDF, EPUB and Kindle. Book excerpt: Using clear and practical examples, Polymorphism of Pharmaceutical Solids, Second Edition presents a comprehensive examination of polymorphic behavior in pharmaceutical development that is ideal for pharmaceutical development scientists and graduate students in pharmaceutical science. This edition focuses on pharmaceutical aspects of polymorphism a
Download or read book Recent Progress in Solid Dispersion Technology written by Kohsaku Kawakami and published by MDPI. This book was released on 2019-10-01 with total page 202 pages. Available in PDF, EPUB and Kindle. Book excerpt: Amorphous solid dispersion (ASD) is a powerful formulation technology to improve oral absorption of poorly soluble drugs. Despite their being in existence for more than half a century, controlling ASD performance is still regarded as difficult because of ASD’s natural non-equilibrium. However, recent significant advances in ASD knowledge and technology may enable a much broader use of ASD technology. This Special Issue, which includes 3 reviews and 6 original articles, focuses on recent progresses in ASD technology in hopes of helping to accelerate developmental studies in the pharmaceutical industry. In striving for a deep understanding of ASD non-equilibrium behavior, the Special issue also delves into and makes progress in the theory of soft-matter dynamics.
Download or read book Dissertation Abstracts International written by and published by . This book was released on 2007 with total page 960 pages. Available in PDF, EPUB and Kindle. Book excerpt:
Download or read book Formulation and Process Development Strategies for Manufacturing Biopharmaceuticals written by Feroz Jameel and published by John Wiley & Sons. This book was released on 2010-08-09 with total page 978 pages. Available in PDF, EPUB and Kindle. Book excerpt: A real-world guide to the production and manufacturing of biopharmaceuticals While much has been written about the science of biopharmaceuticals, there is a need for practical, up-to-date information on key issues at all stages of developing and manufacturing commercially viable biopharmaceutical drug products. This book helps fill the gap in the field, examining all areas of biopharmaceuticals manufacturing, from development and formulation to production and packaging. Written by a group of experts from industry and academia, the book focuses on real-world methods for maintaining product integrity throughout the commercialization process, clearly explaining the fundamentals and essential pathways for all development stages. Coverage includes: Research and early development phase–appropriate approaches for ensuring product stability Development of commercially viable formulations for liquid and lyophilized dosage forms Optimal storage, packaging, and shipping methods Case studies relating to therapeutic monoclonal antibodies, recombinant proteins, and plasma fractions Useful analysis of successful and failed products Formulation and Process Development Strategies for Manufacturing Biopharma-ceuticals is an essential resource for scientists and engineers in the pharmaceutical and biotech industries, for government and regulatory agencies, and for anyone with an interest in the latest developments in the field.
Download or read book Advances in Organic Crystal Chemistry written by Masami Sakamoto and published by Springer Nature. This book was released on 2020-07-10 with total page 532 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book summarizes and records the recent notable advances in diverse topics in organic crystal chemistry, which has made substantial progress along with the rapid development of a variety of analysis and measurement techniques for solid organic materials. This review book is one of the volumes that are published periodically on this theme. The previous volume, published in 2015, systematically summarized the remarkable progress in assorted topics of organic crystal chemistry using organic solids and organic–inorganic hybrid materials during the previous 5 years, and it has been widely read. The present volume also shows the progress of organic solid chemistry in the last 5 years, with contributions mainly by invited members of the Division of Organic Crystal Chemistry of the Chemical Society of Japan (CSJ), together with prominent invited authors from countries other than Japan.
Download or read book Water Insoluble Drug Formulation written by Ron Liu and published by CRC Press. This book was released on 2008-01-18 with total page 686 pages. Available in PDF, EPUB and Kindle. Book excerpt: Scientists have attributed more than 40 percent of the failures in new drug development to poor biopharmaceutical properties, particularly water insolubility. Issues surrounding water insolubility can postpone, or completely derail, important new drug development. Even much-needed reformulation of currently marketed products can be significantly affected by these challenges. Water Insolubility is the Primary Culprit in over 40% of New Drug Development Failures The most comprehensive resource on the topic, this second edition of Water Insoluble Drug Formulation brings together a distinguished team of experts to provide the scientific background and step-by-step guidance needed to deal with solubility issues in drug development. Twenty-three chapters systematically describe solubility properties and their impact on formulation, from theory to industrial practice. With detailed discussion on how these properties contribute to solubilization and dissolution, the text also features six brand new chapters on water-insoluble drugs, exploring regulatory aspects, pharmacokinetic behavior, early phase formulation strategies, lipid based systems for oral delivery, modified release of insoluble drugs, and scalable manufacturing aspects. The book includes more than 15 water-insoluble drug delivery systems or technologies, illustrated with case studies featuring oral and parenteral applications. Highlighting the most current information and data available, this seminal volume reflects the significant progress that has been made in nearly all aspects of this field.
Download or read book Disordered Pharmaceutical Materials written by Marc Descamps and published by John Wiley & Sons. This book was released on 2016-03-28 with total page 544 pages. Available in PDF, EPUB and Kindle. Book excerpt: A one-stop resource for researchers, developers, and post graduate students in pharmaceutical science. This handbook and ready reference provides detailed, but not overloaded information -- presenting the topic without unnecessarily complex formalism. As such, it gives a systematic and coherent overview of disordered materials for pharmaceutical applications, covering fundamental aspects, as well as preparation and characterization techniques for the target-oriented development of drug delivery systems based on disordered crystals and amorphous solids. Special attention is paid to examine the different facets and levels of disorder in their structural and dynamic aspects as well as the effect of disorder on dissolution and stability. Chapters on processing induced disorder and on patenting issues round off the book. As a result the book helps overcoming the challenges of using these materials in the pharmaceutical industry. For pharmaceutical and medicinal chemists, materials scientists, clinical physicists, and pharmaceutical laboratories looking to make better and more potent pharmaceuticals.
Download or read book Amorphous Food and Pharmaceutical Systems written by Harry Levine and published by Royal Society of Chemistry. This book was released on 2007-10-31 with total page 397 pages. Available in PDF, EPUB and Kindle. Book excerpt: During the past decade, the importance of amorphous water-soluble substances has been increasingly recognised within the food and pharmaceutical industries. In response, Amorphous Food and Pharmaceutical Systems brings together current leading experts to contribute to this unique cross-disciplinary account of the subject. Coverage includes: water-compatible amorphous solids (physical, chemical behaviour), low water content systems (water as plasticizer); applications in food and pharmaceutical sciences and industries (processing and stability) along with state-of-the-art technology in food and pharmaceutical systems. This timely publication will be welcomed by academic and industrial researchers and professionals in the pharmaceuticals, food, materials and polymer sciences.
Download or read book Freeze Drying Lyophilization of Pharmaceutical and Biological Products written by Louis Rey and published by CRC Press. This book was released on 2016-04-19 with total page 580 pages. Available in PDF, EPUB and Kindle. Book excerpt: Freeze-drying, or lyophilization, is a well established technology used in the preservation of numerous pharmaceutical and biological products. This highly effective dehydration method involves the removal of water from frozen materials via the direct sublimation of ice. In recent years, this process has met with many changes, as have the regulatio
