Amorphous Solid Dispersions
Amorphous Solid Dispersions

Author: Navnit Shah

Publisher: Springer

Published: 2014-11-21

Total Pages: 702

ISBN-13: 1493915983

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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 and Solubilization in Aqueous Media
Solubility and Solubilization in Aqueous Media

Author: Samuel Hyman Yalkowsky

Publisher: Acs Professional Reference Boo

Published: 1999

Total Pages: 0

ISBN-13: 9780841235762

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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.

Drug-like Properties: Concepts, Structure Design and Methods
Drug-like Properties: Concepts, Structure Design and Methods

Author: Li Di

Publisher: Elsevier

Published: 2010-07-26

Total Pages: 549

ISBN-13: 0080557619

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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

Essentials of Pharmaceutical Preformulation
Essentials of Pharmaceutical Preformulation

Author: Simon Gaisford

Publisher: John Wiley & Sons

Published: 2012-10-22

Total Pages: 234

ISBN-13: 1118423240

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Essentials of Pharmaceutical Preformulation is a study guide which describes the basic principles of pharmaceutical physicochemical characterisation. Successful preformulation requires knowledge of fundamental molecular concepts (solubility, ionisation, partitioning, hygroscopicity and stability) and macroscopic properties (physical form, such as the crystalline and amorphous states, hydrates, solvates and co-crystals and powder properties), familiarity with the techniques used to measure them and appreciation of their effect on product performance, recognising that often there is a position of compromise to be reached between product stability and bioavailability. This text introduces the basic concepts and discusses their wider implication for pharmaceutical development, with reference to many case examples of current drugs and drug products. Special attention is given to the principles and best-practice of the analytical techniques that underpin preformulation (UV spectrophotometry, TLC, DSC, XRPD and HPLC). The material is presented in the typical order that would be followed when developing a medicine and maps onto the indicative pharmacy syllabus of the Royal Pharmaceutical Society of Great Britain Undergraduate-level pharmacy students and R&D / analytical scientists working in the pharmaceutical sector (with or without a pharmaceutical background) will find this text easy to follow with relevant pharmaceutical examples. Essential study guide for pharmacy and pharmaceutical science students Covers the pharmaceutical preformulation components of the Royal Pharmaceutical Society of Great Britain’s indicative syllabus Easy to follow text highlighted with relevant pharmaceutical examples Self-assessment assignments in a variety of formats Written by authors with both academic and industrial experience Companion website with further information to maximise learning

The Determination of Ionization Constants
The Determination of Ionization Constants

Author: Adrien Albert

Publisher: Springer Science & Business Media

Published: 2012-12-06

Total Pages: 223

ISBN-13: 9400955480

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This practical manual is devised for organic chemists and biochemists who, in the course of their researches and without previous experience, need to determine an ionization constant. We are gratified that earlier editions were much used for this purpose and that they also proved adequate for the in service training of technicians and technical officers to provide a Department with a pK service. The features of previous editions that gave this wide appeal have been retained, but the subject matter has been revised, extended, and brought up to date. We present two new chapters, one of which describes the determination of the stability constants of the complexes which organic ligands form with metal cations. The other describes the use of more recently introduced techniques for the determination of ionization constants, such as Raman and nuclear magnetic resonance spectroscopy, thermometric titrations, and paper electro phoresis. Chapter 1 gives enhanced help in choosing between alternative methods for determining ionization constants. The two chapters on potentiometric methods have been extensively revised in the light of newer understanding of electrode processes and of the present state of the art in instrumen tation.

Polymorphism
Polymorphism

Author: Rolf Hilfiker

Publisher: John Wiley & Sons

Published: 2006-08-21

Total Pages: 433

ISBN-13: 3527607722

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Edited by one of the leading experts in the field, this handbook emphasizes why solid-state issues are important, which approaches should be taken to avoid problems and exploit the opportunities offered by solid state properties in the pharmaceutical and agricultural industries. With its practical approach, this is at once a guideline for development chemists just entering the field as well as a high-quality source of reference material for specialists in the pharmaceutical and chemical industry, structural chemists, physicochemists, crystallographers, inorganic chemists, and patent departments.

Oral Bioavailability
Oral Bioavailability

Author: Xiaoling Li

Publisher: John Wiley & Sons

Published: 2011-08-04

Total Pages: 875

ISBN-13: 1118067584

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Understand and assess the design, delivery, and efficacy of orally administered drugs A practical guide to understanding oral bioavailability, one of the major hurdles in drug development and delivery, Oral Bioavailability: Basic Principles, Advanced Concepts, and Applications is designed to help chemists, biologists, life science researchers, pharmaceutical scientists, pharmacologists, clinicians, and graduate and students become familiar with the fundamentals and practices of the science of oral bioavailability. The difference in rate and extent between a drug taken orally and the actual amount of a drug reaching the circulatory system, oral bioavailability is an essential parameter for determining the efficacy and adverse effects of new and developing medications, as well as finding an optimal dosing regimen. This book provides a much-needed one-stop resource to help readers better understand and appreciate the many facets and complex problems of oral bioavailability, including the basic barriers to oral bioavailability, the methods used to determine relevant parameters, and the challenges of drug delivery. In addition, this comprehensive book discusses biological and physicochemical methods for improving bioavailability, integrates physicochemistry with physiology and molecular biology, and includes several state-of-the-art technologies and approaches Caco-2 cell culture model, MDCK, and other related cell culture models which are used to study the science of oral bioavailability.

Polymorphism in the Pharmaceutical Industry
Polymorphism in the Pharmaceutical Industry

Author: Rolf Hilfiker

Publisher: John Wiley & Sons

Published: 2019-01-04

Total Pages: 645

ISBN-13: 3527697853

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"Polymorphism in the Pharmaceutical Industry - Solid Form and Drug Development" highlights the relevance of polymorphism in modern pharmaceutical chemistry, with a focus on quality by design (QbD) concepts. It covers all important issues by way of case studies, ranging from properties and crystallization, via thermodynamics, analytics and theoretical modelling right up to patent issues. As such, the book underscores the importance of solid-state chemistry within chemical and pharmaceutical development. It emphasizes why solid-state issues are important, the approaches needed to avoid problems and the opportunities offered by solid-state properties. The authors include true polymorphs as well as solvates and hydrates, while providing information on physicochemical properties, crystallization thermodynamics, quantum-mechanical modelling, and up-scaling. Important analytical tools to characterize solid-state forms and to quantify mixtures are summarized, and case studies on solid-state development processes in industry are also provided. Written by acknowledged experts in the field, this is a high-quality reference for researchers, project managers and quality assurance managers in pharmaceutical, agrochemical and fine chemical companies as well as for academics and newcomers to organic solid-state chemistry.

FASTtrack Pharmaceutics
FASTtrack Pharmaceutics

Author: Yvonne Perrie

Publisher: Pharmaceutical Press

Published: 2012

Total Pages: 257

ISBN-13: 0857110594

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"Pharmaceutics - Drug delivery and targeting focuses on what pharmacy students really need to know in order to pass exams, providing concise, bulleted information, key points, tips and an all-important self-assessment section which includes MCQs."--Page 4 of cover.

Polymorphism in Molecular Crystals
Polymorphism in Molecular Crystals

Author: Joel Bernstein

Publisher: Oxford University Press

Published: 2002

Total Pages: 429

ISBN-13: 0198506058

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Polymorphism - the multiplicity of structures or forms - is a term that is used in many disciplines. In chemistry it refers to the existence of more than one crystal structure for a particular chemical substance. The properties of a substance are determined by its composition and by its structure. In the last two decades, there has been a sharp rise in the interest in polymorphic systems, as an intrinsically interesting phenomenon and as an increasingly important component in the development and marketing of a variety of materials based on organic molecules (e.g. pharmaceuticals, dyes and pigments, explosives, etc.). This book summarizes and brings up to date the current knowledge and understanding of polymorphism of molecular crystals, and concentrates it in one comprehensive source. The book will be an invaluable reference for students, researchers, and professionals in the field.