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.

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.

Oral Drug Absorption, Second Edition thoroughly examines the special equipment and methods used to test whether drugs are released adequately when administered orally. The contributors discuss methods for accurately establishing and validating in vitro/in vivo correlations for both MR and IR formulations, as well as alternative approaches for MR an

The peroral application (swallowing) of a medicine means that the body must first resorb the active substance before it can begin to take effect. The efficacy of drug uptake depends on the one hand on the chemical characteristics of the active substance, above all on its solubility and membrane permeability. On the other hand, it is determined by the organism's ability to absorb pharmaceuticals by way of specific transport proteins or to excrete them. Since many pharmacologically active substances are poorly suited for oral intake, a decisive criterion for the efficacy of a medicine is its so-called bioavailability. Written by an international team from academia and the pharmaceutical industry, this book covers all aspects of the oral bioavailability of medicines. The focus is placed on methods for determining the parameters relevant to bioavailability. These range from modern physicochemical techniques via biological studies in vitro and in vivo right up to computer-aided predictions. The authors specifically address possibilities for optimizing bioavailability during the early screening stage for the active substance. Its clear structure and comprehensive coverage make this book equally suitable for researchers and lecturers in industry and teaching.

ORAL BIOAVAILABILITY AND DRUG DELIVERY Improve the performance and viability of newly-developed and approved drugs with this crucial guide Bioavailability is the parameter which measures the rate and extent to which a drug reaches a user’s circulatory system depending on the method of administration. For example, intravenous administration produces a bioavailability of 100%, since the drugs are injected directly into the circulatory system; in the case of oral administration, however, bioavailability can vary widely based on factors which, if not properly understood, can result in a failure in drug development, adverse effects, and other complications. The mechanics of oral bioavailability are therefore critical aspects of drug development. Oral Bioavailability and Drug Delivery provides a comprehensive coverage of this subject as well as its drug development applications. Beginning with basic terminology and fundamental concepts, it provides a thorough understanding of the challenges and barriers to oral bioavailability as well as the possibilities for improving this parameter. The resulting book is an indispensable tool for drug development research. Oral Bioavailability and Drug Delivery readers will also find: Discussion questions in many chapters to facilitate comprehension Detailed discussion of topics including dissolution, absorption, metabolism, and more Real-world examples of methods in actions throughout Oral Bioavailability and Drug Delivery is ideal for pharmaceutical and biotechnology scientists working in drug discovery and development; researchers in chemistry, biology, pharmacology, immunology, neuroscience, and other related fields; and graduate courses in drug development and delivery.

A comprehensive introduction to using modeling and simulation programs in drug discovery and development Biopharmaceutical modeling has become integral to the design and development of new drugs. Influencing key aspects of the development process, including drug substance design, formulation design, and toxicological exposure assessment, biopharmaceutical modeling is now seen as the linchpin to a drug's future success. And while there are a number of commercially available software programs for drug modeling, there has not been a single resource guiding pharmaceutical professionals to the actual tools and practices needed to design and test safe drugs. A guide to the basics of modeling and simulation programs, Biopharmaceutics Modeling and Simulations offers pharmaceutical scientists the keys to understanding how they work and are applied in creating drugs with desired medicinal properties. Beginning with a focus on the oral absorption of drugs, the book discusses: The central dogma of oral drug absorption (the interplay of dissolution, solubility, and permeability of a drug), which forms the basis of the biopharmaceutical classification system (BCS) The concept of drug concentration How to simulate key drug absorption processes The physiological and drug property data used for biopharmaceutical modeling Reliable practices for reporting results With over 200 figures and illustrations and a peerless examination of all the key aspects of drug research—including running and interpreting models, validation, and compound and formulation selection—this reference seamlessly brings together the proven practical approaches essential to developing the safe and effective medicines of tomorrow.

Oral lipid-based formulations are attracting considerable attention due to their capacity to facilitate gastrointestinal absorption and reduce or eliminate the effect of food on the absorption of poorly water-soluble, lipophilic drugs. Despite the obvious and demonstrated utility of these formulations for addressing a persistent and growing problem