Solubility and Solubilization in Aqueous Media

Solubility and Solubilization in Aqueous Media
Author: Samuel Hyman Yalkowsky
Publisher: Acs Professional Reference Boo
Total Pages: 0
Release: 1999
Genre: Medical
ISBN: 9780841235762

This book aims to provide the reader with a working knowledge of the various means of controlling the solubility or dissolution rate of a drug or other solute in an aqueous medium. The book begins with the factors which govern solubility in general and then looks at aqueous solubility in particular, including the properties of liquid mixtures and the thermodynamics of solutions formed from mixing two components. The bulk of the book is then devoted to techniques for altering solubility and dissolution rate of organic compounds in aqueous media. It discusses in detail the most commonly used solubility enhancers: buffers, cosolvents, surfactants, and complexants. Each chapter is self-contained and emphasizes the details for applying the techniques.

Handbook of Solubility Data for Pharmaceuticals

Handbook of Solubility Data for Pharmaceuticals
Author: Abolghasem Jouyban
Publisher: CRC Press
Total Pages: 554
Release: 2009-08-26
Genre: Medical
ISBN: 1439804885

Aqueous solubility is one of the major challenges in the early stages of drug discovery. One of the most common and effective methods for enhancing solubility is the addition of an organic solvent to the aqueous solution. Along with an introduction to cosolvency models, the Handbook of Solubility Data for Pharmaceuticals provides an extensive datab

Amorphous Solid Dispersions

Amorphous Solid Dispersions
Author: Navnit Shah
Publisher: Springer
Total Pages: 702
Release: 2014-11-21
Genre: Medical
ISBN: 1493915983

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.

Solubility of Polysaccharides

Solubility of Polysaccharides
Author: Zhenbo Xu
Publisher: BoD – Books on Demand
Total Pages: 140
Release: 2017-11-29
Genre: Science
ISBN: 9535136496

Sugars, with a scientific term as saccharides, are involved in various aspects in the lives of human beings, including the sense of taste, energy for daily life, etc. Recent development in polysaccharides, as well as the background knowledge in this field, further deepens insight into their roles as healthy supplements. In this book, the principles on polysaccharides' solubility and structure, methodologies and application of polysaccharides have been reviewed. The chapters in this book include the relationship between structure and solubility of polysaccharide, the experimental and computational researches on polysaccharide solubility and the common polysaccharide, which may further aid scholars and researchers in regard to solubility of polysaccharides, methodologies and modification.

Drug-like Properties: Concepts, Structure Design and Methods

Drug-like Properties: Concepts, Structure Design and Methods
Author: Li Di
Publisher: Elsevier
Total Pages: 549
Release: 2010-07-26
Genre: Science
ISBN: 0080557619

Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. - Serves as an essential working handbook aimed at scientists and students in medicinal chemistry - Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies - Discusses improvements in pharmacokinetics from a practical chemist's standpoint

Handbook of Pharmaceutical Salts Properties, Selection, and Use

Handbook of Pharmaceutical Salts Properties, Selection, and Use
Author: P. Heinrich Stahl
Publisher: John Wiley & Sons
Total Pages: 392
Release: 2008-08-04
Genre: Medical
ISBN: 9783906390581

This comprehensive up-to-date guide and information source is an instructive companion for all scientists involved in research and development of drugs and, in particular, of pharmaceutical dosage forms. The editors have taken care to address every conceivable aspect of the preparation of pharmaceutical salts and present the necessary theoretical foundations as well as a wealth of detailed practical experience in the choice of pharmaceutically active salts. Altogether, the contributions reflect the multidisciplinary nature of the science involved in selection of suitable salt forms for new drug products.

Drug Delivery Strategies for Poorly Water-Soluble Drugs

Drug Delivery Strategies for Poorly Water-Soluble Drugs
Author: Dionysios Douroumis
Publisher: John Wiley & Sons
Total Pages: 543
Release: 2012-12-19
Genre: Science
ISBN: 1118444671

Many newly proposed drugs suffer from poor water solubility, thus presenting major hurdles in the design of suitable formulations for administration to patients. Consequently, the development of techniques and materials to overcome these hurdles is a major area of research in pharmaceutical companies. Drug Delivery Strategies for Poorly Water-Soluble Drugs provides a comprehensive overview of currently used formulation strategies for hydrophobic drugs, including liposome formulation, cyclodextrin drug carriers, solid lipid nanoparticles, polymeric drug encapsulation delivery systems, self–microemulsifying drug delivery systems, nanocrystals, hydrosol colloidal dispersions, microemulsions, solid dispersions, cosolvent use, dendrimers, polymer- drug conjugates, polymeric micelles, and mesoporous silica nanoparticles. For each approach the book discusses the main instrumentation, operation principles and theoretical background, with a focus on critical formulation features and clinical studies. Finally, the book includes some recent and novel applications, scale-up considerations and regulatory issues. Drug Delivery Strategies for Poorly Water-Soluble Drugs is an essential multidisciplinary guide to this important area of drug formulation for researchers in industry and academia working in drug delivery, polymers and biomaterials.

COSMO-RS

COSMO-RS
Author: Andreas Klamt
Publisher: Elsevier
Total Pages: 247
Release: 2005-07-26
Genre: Technology & Engineering
ISBN: 0080455530

The COSMO-RS technique is a novel method for predicting the thermodynamic properties of pure and mixed fluids which are important in many areas, ranging from chemical engineering to drug design. COSMO-RS, From Quantum Chemistry to Fluid Phase Thermodynamics and Drug Design is about this novel technology, which has recently proven to be the most reliable and efficient tool for the prediction of vapour-liquid equilibria. In contrast to group contribution methods, which depend on an extremely large number of experimental data, COSMO-RS calculates the thermodynamic data from molecular surface polarity distributions, resulting from quantum chemical calculations of the individual compounds in the mixture. In this book, the author cleverly combines a vivid overview of the partly demanding theoretical steps with a deeper analysis of their scientific background and justification. Aimed at theoretical chemists, computational chemists, physical chemists, chemical engineers, thermodynamicists as well as students,academic and industrial experts, COSMO-RS, From Quantum Chemistry to Fluid Phase Thermodynamics and Drug Design provides a novel viewpoint to anyone looking to gain more insight into the theory and potential of the unique method, COSMO-RS. - The only book currently available on COSMO-RS technique - Provides a novel viewpoint for the scientific understanding and for the practical quantitative treatment of fluid phase thermodynamics - Includes illustrative examples of the COSMOtherm program

Water-Insoluble Drug Formulation

Water-Insoluble Drug Formulation
Author: Ron Liu
Publisher: CRC Press
Total Pages: 686
Release: 2008-01-18
Genre: Medical
ISBN: 1420009559

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.

Solvent Systems and Their Selection in Pharmaceutics and Biopharmaceutics

Solvent Systems and Their Selection in Pharmaceutics and Biopharmaceutics
Author: Patrick Augustijns
Publisher: Springer Science & Business Media
Total Pages: 466
Release: 2007-08-06
Genre: Medical
ISBN: 0387691545

Solvent systems are integral to drug development and pharmaceutical technology. This single topic encompasses numerous allied subjects running the gamut from recrystallization solvents to biorelevant media. The goal of this contribution to the AAPS Biotechnology: Pharmaceutical Aspects series is to generate both a practical handbook as well as a reference allowing the reader to make effective decisions concerning the use of solvents and solvent systems. To this end, the monograph was created by inviting recognized experts from a number of fields to author relevant sections. Specifically, 15 chapters have been designed covering the theoretical background of solubility, the effect of ionic equilibria and pH on solubilization, the use of solvents to effect drug substance crystallization and polymorph selection, the use of solvent systems in high throughput screening and early discovery, solvent use in preformulation, the use of solvents in bio-relevant dissolution and permeation experiments, solvents and their use as toxicology vehicles, solubilizing media and excipients in oral and parenteral formulation development, specialized vehicles for protein formulation and solvent systems for topical and pulmonary drug administration. The chapters are organized such that useful decision trees are included together with the scientific underpinning for their application. In addition, trends in the use of solvent systems and a balance of current views make this monograph useful to both the novice and experienced researcher and to scientists at all developmental stages from early discovery to late pharmaceutical operations.