Oral Bioavailability Assessment

Specifically geared to personnel in the pharmaceutical and biotechnology industries, this book describes the basics and challenges of oral bioavailability – one of the most significant hurdles in drug discovery and development. • Describes approaches to assess pharmacokinetics and how drug efflux and uptake transporters impact oral bioavailability • Helps readers reduce the failure rate of drug candidates when transitioning from the bench to the clinic during development • Explains how preclinical animal models – used in preclinical testing – and in vitro tools translate to humans, which is an underappreciated and complicated area of drug development • Includes chapters about pharmacokinetic modelling, the Biopharmaceutics Drug Disposition Classification System (BDDCS), and the Extended Clearance Classification System (ECCS) • Has tutorials for applying strategies to medicinal chemistry practices of drug discovery/development

The book also illustrates how bioavailability adjustments can be incorporated into risk assessments to generate risk-based cleanup values that are more site specific than those based on the default assumption of complete bioavailability. Although the book focuses on oral bioavailability of metals to human receptors, many of the basic principles described herein also can be applied to assessing bioavailability of organic compounds and for assessing bioavailability to ecological receptors."--BOOK JACKET.

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

A practical, hands-on guide for successfully developing oral drug products, this comprehensive reference runs the gamut from theoretical stages of computer-based calculations to practical guidelines for establishing in vitro/in vivo correlations. Coverage details the interrelationship between the physiology of the gastrointestinal tract and oral drug formulations and absorption, and progresses to the latest applications of pharmacokinetic analysis. Includes chapters by the innovators of the Biopharmaceutical Classification Scheme (BCS), human perfusions, and biorelevant dissolution testing! With over 600 literature references, equations, drawings, and photographs, Oral Drug Absorption offers multiple methods for predicting permeability, solubility, and dissolution for oral bioavailability and bioequivalence facilitates selection of appropriate drug candidates for development fully elaborates on the experimental and data analysis techniques of in vitro/in vivo correlations provides guidance to the Federal Drug Administration's BCS and its applications appends helpful case studies to the concepts discussed and much more! Contributions by more than 20 international specialists on the latest research make Oral Drug Absorption an invaluable tool and useful reference in the hands of pharmaceutical scientists, medicinal chemists, pharmacists, pharmacologists, toxicologists, biochemists, gastroenterologists, regulatory personnel, and graduate school students in these disciplines.

This book casts new light on the field of oral drug absorption. It outlines both the concept of the past and the novel concept of Finite Absorption Time (FAT). In addition, the authors explore the correlated need for re-definition of bioavailability, bioequivalence providing a plethora of experimental data. Accordingly, this book is intended for academics/students or scientists working in pharmaceutical industries, regulatory agencies, and contract research organizations. It can be used for teaching purposes in under- and post-graduate courses dealing with biopharmaceutics, pharmacokinetics and biomedical engineering.

Drug Discovery and Evaluation has become a more and more difficult, expensive and time-consuming process. The effect of a new compound has to be detected by in vitro and in vivo methods of pharmacology. The activity spectrum and the potency compared to existing drugs have to be determined. As these processes can be divided up stepwise we have designed a book series "Drug Discovery and Evaluation" in the form of a recommendation document. The methods to detect drug targets are described in the first volume of this series "Pharmacological Assays" comprising classical methods as well as new technologies. Before going to man, the most suitable compound has to be selected by pharmacokinetic studies and experiments in toxicology. These preclinical methods are described in the second volume „Safety and Pharmacokinetic Assays". Only then are first studies in human beings allowed. Special rules are established for Phase I studies. Clinical pharmacokinetics are performed in parallel with human studies on tolerability and therapeutic effects. Special studies according to various populations and different therapeutic indications are necessary. These items are covered in the third volume: „Methods in Clinical Pharmacology".

This book discusses bioavailability concepts and methods, summarizing the current knowledge on bioavailability science, as well as possible pathways for integrating bioavailability into risk assessment and the regulation of organic chemicals. Divided into 5 parts, it begins with an overview of chemical distribution in soil and sediment, as well as the bioavailability and bioaccumulation of chemicals in plants, soil, invertebrates and vertebrates (including humans). It then focuses on the impact of sorption processes and reviews bioavailability measurement methods. The closing chapters discuss the impact of bioavailability studies on chemical risk assessment, and highlights further research needs. Written by a multi-disciplinary team of authors, it is an essential resource for scientists in academia and industry, students, as well as for authorities.

Since bioavailability can alter health risk estimates by a factor of 10, 100 or more, its importance in risk assessment cannot be underestimated. Presenting the basic principles that govern bioavailability and how it is measured, this very unique and timely book fills a void in the existing literature on toxicology and toxicokinetics. It contains clear and concise discussions on the behavior of environmental contaminants and how they reach the bloodstream in living organisms. It also presents an exhaustive review of measured bioavailability factors for environmental contaminants most frequently encountered at contaminated sites.