This is a well thought-out, highly practical text covering contemporary ‘in vitro’ techniques for drug absorption studies. Starting at the molecular level of investigation, it continues with cell monolayer models (both primary and cell lines) and culminates with in situ techniques as a final testing format. In addition, chapters on high-throughput assays, in vitro-in vivo correlation, bioinformatics and regulatory issues are covered, giving a comprehensive overview of available models and techniques. Moreover, an appendix consisting of a number of practical protocols is available online, updated as needed, and should prove very helpful to apply the techniques directly to the benchside.
Topics 1. Models for Skin Absorption and Skin Toxicity Testing. 2. Models of the Small Intestine. 3. Drug Absorption from the Colon In Situ. 4. In Vivo and In Vitro Models for Assessing Drug Absorption Across the Bucal Mucosa. 5. In Situ and Ex Vivo Nasal Models for Preclinical Drug Development Studies. 6. The Isolated Perfused Lung for Drug Absorption Studies. 7. In Vitro Models for Investigations of Buccal Drug Permeation and Metabolism. 8. In Vitro Screening Models to Assess Intestinal Drug Absorption and Metabolism. 9. In Vitro Cellular Models for Nasal Drug Absorption Studies. 10. In Vitro Models of the Tracheo-Bronchial Epithelium. 11. In Vitro Models of the Alveolar Epithelial Barrier. 12. Cell Culture Models of the Corneal Epithelium and Reconstructed Cornea Equivalents for In Vitro Drug Absorption Studies. 13. The Conjunctival Barrier in Ocular Drug Delivery. 14. Inner Blood-Retinal Barrier : Transport Biology and Methodology. 15. Regulation of Paracellular Permeability in Low-Resistance Human Vaginal-Cervical Epithelia. 16. In Vitro Models and Multidrug Resistance Mechanisms of the Placental Barrier. 17. In Vitro Models to Study Blood-Brain Barrier Function. 18. High-Throughput Screening Using Caco-2 Cell and PAMPA Systems. 19. Instrumented In Vitro Approaches to Assess Epithelial Permeability of Drugs from Pharmaceutical Formulations. 20. Modeling Trandermal Absorption. 21. Physiologically Based in Silico Models for the Prediction of Oral Drug Absorption. 22. In Silico Modeling for Blood-Brain Barrier Permeability Predictions. 23. Impact of Drug Transport Proteins. 24. Cloning and Functional Heterologous Expression of Transporters. 25. The Pharmacology of Caveolae. 26. Immortalization Strategies for Epithelial Cells in Primary Culture. 27. Binding-Uptake Studies and Cellular Targeting. 28. Drug Permeability Studies in Regulatory Biowaiver Applications.
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
This book illustrates, in a comprehensive manner, the most crucial principles involved in pharmacology and allied sciences. The title begins by discussing the historical aspects of drug discovery, with up to date knowledge on Nobel Laureates in pharmacology and their significant discoveries. It then examines the general pharmacological principles - pharmacokinetics and pharmacodynamics, with in-depth information on drug transporters and interactions. In the remaining chapters, the book covers a definitive collection of topics containing essential information on the basic principles of pharmacology and how they are employed for the treatment of diseases. Readers will learn about special topics in pharmacology that are hard to find elsewhere, including issues related to environmental toxicology and the latest information on drug poisoning and treatment, analytical toxicology, toxicovigilance, and the use of molecular biology techniques in pharmacology. The book offers a valuable resource for researchers in the fields of pharmacology and toxicology, as well as students pursuing a degree in or with an interest in pharmacology.
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.
Since publication of the Second Edition in 1989, numerous innovations have occurred that affect the way scientists look at issues in the field of percutaneous absorption. Focusing on recent advances as well as updating and expanding the scope of topics covered in the previous edition, Percutaneous Absorption, Third Edition provides thorough coverage of the skin's role as an important portal of entry for chemicals into the body. Assembles the work of nearly 80 experts-30 more than the Second Edition-into a unified, comprehensive volume that contains the latest ideas and research! Complete with nearly 600 drawings, photographs, equations, and tables and more than 1600 bibliographic citations of pertinent literature, Percutaneous Absorption, Third Edition details the applied biology of percutaneous penetration factors that affect skin permeation, such as age, vehicles, metabolism, hydration of skin, and chemical structure in vivo and in vitro techniques for measuring absorption, examining factors influencing methodology such as animal models, volatility of test compound, multiple dosage, and artificial membranes procedures for use in transdermal delivery, exploring topics such as effects of penetration enhancers on absorption, optimizing absorption, and the topical delivery of drugs to muscle tissue And presents new chapters on mathematical models cutaneous metabolism prediction of percutaneous absorption in vitro absorption methodology dermal decontamination concentration of chemicals in skin transdermal drug delivery mechanisms of absorption safety evaluation of cosmetics absorption of drugs and cosmetic ingredients nail penetration Emphasizes human applications-particularly useful for pharmacists, pharmacologists, dermatologists, cosmetic scientists, biochemists, toxicologists, public health officials, manufacturers of cosmetic and toiletry products, and graduate students in these disciplines! An invaluable reference source for readers who need to keep up with the latest developments in the field, Percutaneous Absorption, Third Edition is also an excellent experimental guide for laboratory personnel.
Handbook of Drug-Nutrient Interactions, Second Edition is an essential new work that provides a scientific look behind many drug-nutrient interactions, examines their relevance, offers recommendations, and suggests research questions to be explored. In the five years since publication of the first edition of the Handbook of Drug-Nutrient Interactions new perspectives have emerged and new data have been generated on the subject matter. Providing both the scientific basis and clinical relevance with appropriate recommendations for many interactions, the topic of drug-nutrient interactions is significant for clinicians and researchers alike. For clinicians in particular, the book offers a guide for understanding, identifying or predicting, and ultimately preventing or managing drug-nutrient interactions to optimize patient care. Divided into six sections all chapters have been revised or are new to this edition. Chapters balance the most technical information with practical discussions and include outlines that reflect the content; discussion questions that can guide the reader to the critical areas covered in each chapter, complete definitions of terms with the abbreviation fully defined and consistent use of terms between chapters. The editors have performed an outstanding service to clinical pharmacology and pharmaco-nutrition by bringing together a multi-disciplinary group of authors. Handbook of Drug-Nutrient Interactions, Second Edition is a comprehensive up-to-date text for the total management of patients on drug and/or nutrition therapy but also an insight into the recent developments in drug-nutrition interactions which will act as a reliable reference for clinicians and students for many years to come.
The highly experienced authors here present readers with step-wise, detail-conscious information to develop quality pharmaceuticals. The book is made up of carefully crafted sections introducing key concepts and advances in the areas of dissolution, BA/BE, BCS, IVIC, and product quality. It provides a specific focus on the integration of regulatory considerations and includes case histories highlighting the biopharmaceutics strategies adopted in development of successful drugs.
This Book serves to highlight the mechanisms related to the low intestinal drug absorption, the strategies to overcome the obstacles or intestinal drug absorption, and in situ, in vitro, and in silico methodologies to predict to intestinal drug absorption. This Book presents a series of drug absorption studies and related technologies that predict intestinal permeation of drugs that govern the pharmacokinetic features of therapeutic drugs. It also contains the mechanistic understanding regarding the first-pass metabolism and intestinal efflux that modulate the pharmacokinetics of drug and suggest the formulation strategies to enhance the bioavailability of investigated drugs.
It is increasingly recognized that various transporter proteins are expressed throughout the body and determine absorption, tissue distribution, biliary and renal elimination of endogenous compounds and drugs and drug effects. This book will give an overview on the transporter families which are most important for drug therapy. Most chapters will focus on one transporter family highlighting tissue expression, substrates, inhibitors, knock-out mouse models and clinical studies.
