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| Author | : |
| Publisher | : |
| Total Pages | : 230 |
| Release | : 2005 |
| Genre | : |
| ISBN | : |
Download Solubilization of Poorly Water-Soluble Drugs: Theory and Applications Book in PDF, ePub and Kindle
This dissertation is based on the theory and applications of the most commonly used solubilization techniques: pH adjustment, cosolvency, micellization, complexation, and the combinations of pH adjustment with one of the other techniques. Chapter 1 provides an overview for the methods which are available to formulate a poorly water-soluble drug based on its administration route. Chapter 2 applies these commonly used techniques to solubilize two structurally related anticancer drugs. The efficiency of each technique is compared for both drugs side by side. It is observed that each technique is more efficient on the drug which has less polarity. However, the achievable final drug concentration in a formulation depends not only on the efficiency of the applied technique, but also on the drug's water solubility. Chapter 3 emphasizes the overall effectiveness of each technique on drugs which have different physicochemical properties. Solubilization profiles for the above techniques are generated for twelve compounds, eight of which are ionizable and studied under both unionized and ionized conditions. This chapter illustrates that the efficiency of the cosolvency, micellization, and complexation on both unionized and ionized drug species can be predicted from their polarities. Thus, the solubility of an ionizable drug can be estimated by using a given solubilizing excipient at any pH to meet the dose requirement. Chapter 4 studies the effect of cosolvent on complex stability. A series of alcohols were used to illustrate the effect of cosolvent size and polarity on the solubilization of a compound. It is proposed that a ternary drug-ligand-cosolvent complex is formed in these combined systemsThis dissertation provides guidance for the selection of a solubilization technique for a compound based on the physicochemical properties and the dose requirement.
| Author | : Robert O. Williams III |
| Publisher | : Springer Science & Business Media |
| Total Pages | : 656 |
| Release | : 2011-12-04 |
| Genre | : Medical |
| ISBN | : 1461411440 |
Download Formulating Poorly Water Soluble Drugs Book in PDF, ePub and Kindle
This volume is intended to provide the reader with a breadth of understanding regarding the many challenges faced with the formulation of poorly water-soluble drugs as well as in-depth knowledge in the critical areas of development with these compounds. Further, this book is designed to provide practical guidance for overcoming formulation challenges toward the end goal of improving drug therapies with poorly water-soluble drugs. Enhancing solubility via formulation intervention is a unique opportunity in which formulation scientists can enable drug therapies by creating viable medicines from seemingly undeliverable molecules. With the ever increasing number of poorly water-soluble compounds entering development, the role of the formulation scientist is growing in importance. Also, knowledge of the advanced analytical, formulation, and process technologies as well as specific regulatory considerations related to the formulation of these compounds is increasing in value. Ideally, this book will serve as a useful tool in the education of current and future generations of scientists, and in this context contribute toward providing patients with new and better medicines.
| Author | : Gregory K. Webster |
| Publisher | : CRC Press |
| Total Pages | : 578 |
| Release | : 2017-01-06 |
| Genre | : Medical |
| ISBN | : 1315340860 |
Download Poorly Soluble Drugs Book in PDF, ePub and Kindle
This book is the first text to provide a comprehensive assessment of the application of fundamental principles of dissolution and drug release testing to poorly soluble compounds and formulations. Such drug products are, vis-à-vis their physical and chemical properties, inherently incompatible with aqueous dissolution. However, dissolution methods are required for product development and selection, as well as for the fulfillment of regulatory obligations with respect to biopharmaceutical assessment and product quality understanding. The percentage of poorly soluble drugs, defined in classes 2 and 4 of the Biopharmaceutics Classification System (BCS), has significantly increased in the modern pharmaceutical development pipeline. This book provides a thorough exposition of general method development strategies for such drugs, including instrumentation and media selection, the use of compendial and non-compendial techniques in product development, and phase-appropriate approaches to dissolution development. Emerging topics in the field of dissolution are also discussed, including biorelevant and biphasic dissolution, the use on enzymes in dissolution testing, dissolution of suspensions, and drug release of non-oral products. Of particular interest to the industrial pharmaceutical professional, a brief overview of the formulation and solubilization techniques employed in the development of BCS class 2 and 4 drugs to overcome solubility challenges is provided and is complemented by a collection of chapters that survey the approaches and considerations in developing dissolution methodologies for enabling drug delivery technologies, including nanosuspensions, lipid-based formulations, and stabilized amorphous drug formulations.
| Author | : Ron Liu |
| Publisher | : CRC Press |
| Total Pages | : 736 |
| Release | : 2018-03-12 |
| Genre | : Medical |
| ISBN | : 1498729428 |
Download Water-Insoluble Drug Formulation Book in PDF, ePub and Kindle
Properties and Formulation: From Theory to Real-World Application 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 the much-needed reformulation of currently marketed products can be significantly affected by these challenges. More recently it was reported that the percentage increased to 90% for the candidates of new chemical entities in the discovery stage and 75% for compounds under development. In the most comprehensive resource on the topic, this third 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 the detailed discussion on solubility theories, solubility prediction models, the aspects of preformulation, biopharmaceutics, pharmacokinetics, regulatory, and discovery support of water-insoluble drugs to various techniques used in developing delivery systems for water-insoluble drugs. This book includes more than 15 water-insoluble drug delivery systems or technologies, illustrated with case studies and 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. The aim of this book is to provide a handy reference for pharmaceutical scientists in the handling of formulation issues related to water-insoluble drugs. In addition, this book may be useful to pharmacy and chemistry undergraduate students and pharmaceutical and biopharmaceutical graduate students to enhance their knowledge in the techniques of drug solubilization and dissolution enhancement.
| Author | : Lino Messana |
| Publisher | : |
| Total Pages | : 300 |
| Release | : 2018 |
| Genre | : |
| ISBN | : 9781681177014 |
Download Poorly Soluble Drugs Book in PDF, ePub and Kindle
Solubility is the property of a solid, liquid, or gaseous chemical substance called solute to dissolve in a solid, liquid, or gaseous solvent to form a homogeneous solution of the solute in the solvent. The solubility of a substance fundamentally depends on the solvent used as well as on temperature and pressure. The extent of solubility of a substance in a specific solvent is measured as the saturation concentration where adding more solute does not increase its concentration in the solution. Solubility also plays a major role for other dosage forms like parenteral formulations as well. 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. This book provides a comprehensive overview of currently used formulation strategies for hydrophobic drugs discusses the main instrumentation, operation principles and theoretical background, with a focus on critical formulation features and clinical studies. It provides a comprehensive assessment of the application of fundamental principles of dissolution and drug release testing to poorly soluble compounds and formulations. Over 40% of new chemical entities developed in pharmaceutical industry are practically insoluble in water. These poorly water soluble drugs having slow drug absorption leads to inadequate and variable bioavailability and gastrointestinal mucosal toxicity. For orally administered drugs solubility is the most important one rate limiting parameter to achieve their desired concentration in systemic circulation for pharmacological response. Problem of solubility is a major challenge for formulation scientist. The improvement of drug solubility thereby its oral bioavailability remains one of the most challenging aspects of drug development process especially for oral-drug delivery system.
| Author | : Dionysios Douroumis |
| Publisher | : John Wiley & Sons |
| Total Pages | : 543 |
| Release | : 2012-12-19 |
| Genre | : Science |
| ISBN | : 1118444671 |
Download Drug Delivery Strategies for Poorly Water-Soluble Drugs Book in PDF, ePub and Kindle
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.
| Author | : Robert O. Williams III |
| Publisher | : |
| Total Pages | : 0 |
| Release | : 2022 |
| Genre | : |
| ISBN | : 9783030887209 |
Download Formulating Poorly Water Soluble Drugs Book in PDF, ePub and Kindle
The objective of this third edition is to consolidate within a single text the most current knowledge, practical methods, and regulatory considerations pertaining to formulations development with poorly water-soluble molecules. A pharmaceutical scientist's approach toward solubility enhancement of a poorly water-soluble molecule typically includes detailed characterization of the compound's physiochemical properties, solid-state modifications, advanced formulation design, non-conventional process technologies, advanced analytical characterization, and specialized product performance analysis techniques. The scientist must also be aware of the unique regulatory considerations pertaining to the non-conventional approaches often utilized for poorly water-soluble drugs. One faced with the challenge of developing a drug product from a poorly soluble compound must possess at a minimum a working knowledge of each of the above mentioned facets and detailed knowledge of most. In light of the magnitude of the growing solubility problem to drug development, this is a significant burden especially when considering that knowledge in most of these areas is relatively new and continues to develop. Highlights the most recent advancements reported in the literature on technologies to improve the dissolution and bioavailability of poorly water soluble drugs Provides a comprehensive discussion of new technologies developed and recently over 40% updated new content Essential read for scientists and researchers in pharmaceutical, chemical, and agricultural industries since over 80% of newly discovered drugs are poorly water soluble.
| Author | : Lin Song |
| Publisher | : |
| Total Pages | : |
| Release | : 2011 |
| Genre | : |
| ISBN | : |
Download Studies of Solubilization of Poorly Water-soluble Drugs During in Vitro Lipolysis of a Model Lipid-based Drug Delivery System and in Mixed Micelles Book in PDF, ePub and Kindle
| Author | : Navnit Shah |
| Publisher | : Springer |
| Total Pages | : 702 |
| Release | : 2014-11-21 |
| Genre | : Medical |
| ISBN | : 1493915983 |
Download Amorphous Solid Dispersions Book in PDF, ePub and Kindle
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.
| Author | : Ankita V. Shah |
| Publisher | : |
| Total Pages | : 286 |
| Release | : 2016 |
| Genre | : |
| ISBN | : |
Download Solubility and Dissolution Enhancement of Poorly Water-soluble Drugs by Supersolubilization Using Weak Counter-Ions Book in PDF, ePub and Kindle
