This book comprehensively reviews drug stability and chemical kinetics: how external factors can influence the stability of drugs, and the reaction rates that trigger these effects. Explaining the important theoretical concepts of drug stability and chemical kinetics, and providing numerous examples in the form of illustrations, tables and calculations, the book helps readers gain a better understanding of the rates of reactions, order of reactions, types of degradation and how to prevent it, as well as types of stability studies. It also offers insights into the importance of the rate at which the drug is degraded and/or decomposed under various external and internal conditions, including temperature, pH, humidity and light. This book is intended for researchers, PhD students and scientists working in the field of pharmacy, pharmacology, pharmaceutical chemistry, medicinal chemistry and biopharmaceutics.

This book covers the recent innovations relating to various bioactive natural products (such as alkaloids, glycosides, flavonoids, anthraquinones, steroids, polysaccharides, tannins and polyphenolic compounds, volatile oils, fixed oils, fats and waxes, proteins and peptides, vitamins, marine products, camptothecin, piperines, carvacrol, gedunin, GABA, ginsenosides) and their applications in the pharmaceutical fields related to academic, research and industry.

Conceived and edited by Nigel Dent and Ramzan Visanji, Veterinary Clinical Trials form Concept to Completion is designed for both established practitioners and novices, offering alternative ways of conducting studies and ensuring that the studies are guided by Good Clinical Practices and are in compliance with regulations. Comprehensive in scope, it provides the scientific, biological, and regulatory background invaluable to teachers, researchers, and regulatory affairs staff, as well as those directly involved in clinical trials. The book covers: -Objectives of the clinical study -Control of the study -Conduct of the study -Regulation versus compliance -Factors for success -International harmonization activities -Roles of the investigator, the monitor, and the practicing veterinarian -Setting up GCP trials with particular animal species -SOPs, the generic protocol, and the study report -Contract research farms and multi-site studies -Auditing With contributions from experts in every area of veterinary trials, the text has been organized with everyday use in mind. The chapters can be read sequentially for a comprehensive view or individually for coverage of particular topics and issues as needed. Drawing directly from the in-the-trenches experience of the editors and chapter authors, the book is a guide to methods that ensure studies meet regulatory compliance and strategies that ensure avoidance of common pitfalls.

This book presents a multidisciplinary assessment of the state of science in the use of systemic delivery technologies to deliver anti-aging therapeutics now under development. There is a gap between basic aging research and the development of intervention technologies. This major obstacle must be overcome before biogerontological interventions can be put into clinical practice. As biogerontology comes to understand aging as a systemic degenerative process, it is clear that there is a pressing need for technologies that enable cells and tissues in a fully developed adult body to be manipulated systemically to combat aging. The authors review advances in the chemistry and engineering of systemic delivery methods and analyze the strengths and limitations of each. The book is organized into six sections. The first offers an overview of the need for systemic delivery technologies alongside the development of anti-aging therapies and describes approaches that will be required for studying the properties and efficiency of carriers for systemic delivery. Sections II, III and IV describe recent advances in a range of strategies that may enable systemic delivery to help combat aging conditions ranging from cell senescence to decline in immune function and hormonal secretion. Section V discusses practical strategies to engineer and optimize the performance of delivery technologies for applications in systemic delivery, along with their working principles. The final section discusses technical and biological barriers that must be overcome as systemic delivery technologies move from research laboratory to clinical applications aimed at tackling aging and age-associated diseases.Benefiting scholars, students and a broader audience of interested readers, the book includes helpful glossary sections in each chapter, as well as sidebars that highlight important notes, and questions for future research.

Demonstrates how substitution of a variety of ligands can render albumin a versatile targeting tool for selective drug accumulation in various cell populations of the liver
This book discusses physical, chemical, and biological approaches to drug targeting technology, focusing on oral, dispersed system, topical, dermal, transdermal, and inhalation delivery, and the development of original formulations that are matched by innovative device design.
Considers the efforts in biotechnology and molecular biology to produce intelligent drug delivery devices by exploiting biological pathways
Containing over 1100 references to facilitate further study, Drug Targeting Technology
updates recent progress in oral and colonic targeting technology using pH- and enzyme-sensitive coating materials and novel polymer systems
shows how the systemic distribution of drugs can be modulated by lipid-based carriers taking alternative routes of transport, particularly lymph flow
details soft drugs that are rapidly metabolized to inactive and nontoxic metabolites and removed efficiently from the body
includes successful designs of virus-like liposomal delivery systems that offer the advantages of viral carriers
supplies examples of how viral delivery systems can be directed to cancer sites
and more
Suggesting harnessing biological processes as the ultimate approach to the delivery or expression of pharmacologically active agents, Drug Targeting Technology is a top-shelf reference for pharmacists, pharmacologists, and pharmaceutical scientists; analytical, surface, physical, and colloid chemists and biochemists; and upper-level undergraduate and graduate students in these disciplines.

Instant Notes in Medicinal Chemistry provides concise coverage for undergraduates studying medicinal chemistry as part of a science, pharmacy or medical course. It is a truly multidisciplinary subject involving such subject specialities as organic chemistry, pharmacology, biochemistry, physiology, microbiology, toxicology, genetics and computer modeling. It concentrates on the fundamental principles of medicinal chemistry and assumes no more than elementary background of chemistry or biology.

This book reviews the current state of ocular drug therapy and future therapeutic opportunities for a wide variety of conditions, including Age-related Macular Degeneration, Diabetic Retinopathy and Macular Edema, Glaucoma, and Inherited Retinal Diseases. Retinal diseases are major contributors to moderate or severe vision impairment in adults aged 50 years and older. The respective patient populations for many of these indications is expected to significantly increase as the world population continues to grow older. An improved understanding of the etiological underpinnings of ocular degenerative diseases over the past decade has significantly bolstered ophthalmic drug discovery. In this volume, contributions from leading experts explore the unique challenges faced for ocular drug discovery and delivery providing the reader with detailed information on ocular pharmacokinetics, in vitro, ex vivo and in vivo models for retinal disease pathology and emerging gene therapy treatments. The book is intended for all researchers and clinicians who wish to increase their knowledge on the latest findings in ocular drug therapy.

This comprehensive text presents a rigorous framework from within which regulators can respond strategically to the claim by the pharmaceutical industry that lower drug prices today lead to a loss for the population's future health due to less innovation. It starts with a critical review of the empirical evidence of the return to consumers on their ongoing investment into high drug prices in order to increase future innovation. The implicit, critical and unrealistic assumption inherent in these studies is identified, namely that the health budget can be expanded to purchase drugs at higher prices without an opportunity cost, for example, the foregone benefits of alternative investments in health care infrastructure. Price effectiveness analysis (PEA), is introduced. PEA informs the question of how the innovative surplus from the new drug should be allocated between the manufacturer and the consumer so as to optimise society's welfare. The method allows the decisions by the regulator and the firm to be analysed jointly by specifying the firm's production and revenue functions in terms of the clinical innovation of a new drug; the incremental effect used in the summary metric of cost effectiveness analysis. An economic value of innovation that takes into account opportunity cost under conditions of economic efficiency in the health system is proposed: the health shadow price. The limitations of the non-strategic methods that currently inform the highly contested new drug subsidy game are presented and the relative strengths of PEA are demonstrated. Health technology assessment quantifies both the clinical innovation of a new drug and its financial impact on the health system. Cost effectiveness analysis tests the relationship between the incremental cost and incremental effect of a new drug for target patients, at a given price. PEA tests the relationship between the price of a new drug and the health of the whole population, now and into the future. It achieves this by taking into account current inefficiency in both resource allocation and the displacement process, and the relationship between price and future innovation.

This extensive reference/text explores the principles, instrumentation, processes, and programs of pharmaceutical solid science as well as new aspects on one-component systems, micromeritics, polymorphism, solid-state stability, cohesion, powder flow, blending, single- unit sustained release, and tablet coating.
Reveals unique approaches in pharmaceutical solid science not previously published in any other text
Providing current data on crystallization, dissolution from particles and polydisperse populations, powder volumes and densities, comminution, wet granulation, and hard-shell capsules, Advanced Pharmaceutical Solids
describes moisture isotherms with crystalline solids
documents the effects of moisture on solid-state stability
highlights tablet physics and principles
explains sustained release by microencapsulation
presents prediction equations for solubility in binary solvents
discusses particle sizes and diameters
identifies Brunauer, Emmett, and Teller Isotherms
and more
Considering properties of solids, permeamitry and gas absorption methods, amorphates, and purification by pH-change precipitation, Advanced Pharmaceutical Solids is an essential reference for pharmacists; pharmaceutical scientists; medicinal, physical, surface, colloid, and analytical chemists and biochemists; and an effective text for upper-level undergraduate and graduate students in these disciplines.

Addressing concerns for patient welfare while protecting producer reputation, and providing a database for formulation of other products, this multiauthored reference blends fundamental theory and practical advice on drug product stability in scientific, technical, and regulatory environments, covering development of indicating assays, computer use, clinical trial materials, strategic planning, and packaging. Describing the documentation required to minimize the changes of regulatory citations, the book lists manufacturers of photostability testing chambers, stability system software, and laboratory information management systems for pharmaceutical applications.

This second edition further develops the principles of applying kinetic principles to drug metabolizing enzymes and transporters. Chapters are divided into six sections detailing fundamental principles of enzyme kinetics, enzyme and transporter structures, highlighting specific oxidative and conjugative drug metabolizing enzymes and drug transporters, modeling approaches for drug metabolizing enzymes and transporters, understanding of variability both experimental and interindividual (pharmacogenomic), and expanded case studies that provide real life examples of applying these principles. Written in the highly successful Methods in Molecular Biology series format, chapters include introductions to their respective topics, in some cases step-by-step instructions with readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls with extensive cross referencing to assist in learning. Authoritative and fully updated, Enzyme Kinetics in Drug Metabolism: Fundamentals and Applications, Second Edition serves as a practical teaching tool for novice and advanced scientists interested in the fundamental concepts.

This book highlights recently discovered aspects of "middle-size molecules," focusing on (1) their unique bio-functions on the basis of derivatives and conjugates of natural products, saccharides, peptides, and nucleotides; (2) the synthesis of structurally complex natural products; (3) special synthetic methods for -conjugated functional molecules; and (4) novel synthetic methods using flow chemistry. Given its scope, the book is of interest to industrial researchers and graduate students in the fields of organic chemistry, medicinal chemistry, and materials science.

Furthering efforts to simulate the potency and specificity exhibited by peptides and proteins in healthy cells, this remarkable reference supplies pharmaceutical scientists with a wealth of techniques for tapping the enormous therapeutic potential of these molecules-providing a solid basis of knowledge for new drug design.
Provides a broad, comprehensive overview of peptides and proteins as mediators of cell movement, proliferation, differentiation, and communication.
Written by more than 50 leading international authorities, Peptides and Protein Drug Analysis
discusses strategies for dealing with the complexity of peptides and proteins in conformational flexibility and amino acid sequence variability
analyzes drug formulations facilitated by solid-phase peptide synthesis and recombinant DNA technology
examines chemical purity analysis by high-pressure chromatographic, capillary electrophoretic, gel electrophoretic, and isoelectric focusing methods
highlights drug design elements derived from protein folding, bioinformatics, and computational chemistry
demonstrates uses of unnatural mutagenesis and combinatorial chemistry
explores mass spectrometry, protein sequence, and carbohydrate analysis
illustrates bioassays and other new functional analysis methods
surveys spectroscopic techniques such as ultraviolet, fluorescence, Fourier transform infrared, and nuclear magnetic resonance (NMR)
addresses ways of distinguishing between levels of therapeutic and endogenous agents in cells
reviews structural analysis tools such as ultracentrifugation and light, X-ray, and neutron scattering
and more
Featuring over 3400 bibliographic citations and more than 500 tables, equations, and illustrations, Peptide and Protein Drug Analysis is a must-read resource for pharmacists; pharmacologists; analytical, organic, and pharmaceutical chemists; cell and molecular biologists; biochemists; and upper-level undergraduate and graduate students in these disciplines.

The book reviews the history of current brand and generic business in pharmaceuticals manufacturing practices. Based on examples, the reader can interpolate, extrapolate and exploit mutual behavior (physical and chemical properties) of chemicals to design and commercialize processes that fulfi ll the demands, also manipulate chemical unit processes and unit operations to reduce/minimize effl uents and lower environmental impact i.e. reduce global warming. Readers will be able to simplify process development, design and commercialize economic manufacturing processes.

This collection explores detailed experimental protocols necessary for setting up a variety of in vitro cytochrome P450 (CYP) assays that are vital in selecting drug candidates in a drug discovery pipeline. Major factors affecting drug metabolism include CYP expression levels, kinetic parameters for individual CYP enzymes, CYP inhibition and induction, time-dependent inhibition (TDI), CYP stability, non-CYP stability, UDP-glucuronosyltransferases (UGT) stability, excretion mechanisms, and drug-drug interactions (DDI), all addressed in this volume. Written for the Methods in Pharmacology and Toxicology series, chapters include helpful background information on the in vitro assay, a list of all the materials, reagents, and equipment necessary to carry out the assay, a step-by-step protocol, notes containing common and unexpected experimental problems in the assay, as well as references containing important supplementary reading. Authoritative and practical, Cytochrome P450: In Vitro Methods and Protocols serves as a key guide for researchers in the area of discovery and development of new medicines.

Suppliers of pharmaceutical manufacturing equipment must ensure that their equipment is provided to their customers in a validatable state. Written in simple, clear, and concise language that gets past all the regulationese, this book covers the basics of validation, planning process equipment design and construction, documentation requirements, avoiding validation pitfalls, and the types of services the supplier should provide. The book provides insights on how to avoid the costly and time-consuming problem of reworking the equipment to develop the information that is needed to successfully complete their validation package - after the equipment has been delivered and installed. Here in one volume is all the information suppliers and manufacturers need to be able to effectively conduct business in a cost- and time-effective manner. Key areas of discussion include: o Validation and GMP issues o Why validation is so important to pharmaceutical manufacturers o The role of equipment suppliers in supporting validation o How validation affects the quality of drugs o A discussion of the importance of each phase of validation o Examples of pre-validation work o Pharmaceutical industry conventions for equipment design & construction o Questions to ask about validation, including a checklist o Regulations in plain language, including the terms and vocabulary o Computer validation o Business & cost issues

Thanks to their unique properties, chitosan and chitosan-based materials have numerous applications in the field of biomedicine, especially in drug delivery. This book examines biomedical applications of functional chitosan, exploring the various functions and applications in the development of chitosan-based biomaterials. It also describes the chemical structure of chitosan and discusses the relationship between their structure and functions, providing a theoretical basis for the design of biomaterials. Lastly, it reviews chemically modified and composite materials of chitin and chitosan derivatives for biomedical applications, such as tissue engineering, nanomedicine, drug delivery, and gene delivery.

This book explores efficient syntheses of indole alkaloids based on gold-catalyzed cascade cyclizations, presenting two strategies for total synthesis of these natural products based on gold-catalyzed reactions of conjugated diyne or ynamide. The book first describes the total and formal synthesis of dictyodendrins A-F based on direct construction of the pyrrolo[2,3-c]carbazole core using the gold-catalyzed annulation of azido-diynes and protected pyrrole. This synthetic strategy features late-stage functionalization of the pyrrolo[2,3-c]carbazole scaffold at several positions and allows diverse access to dictyodendrins and their derivatives. Secondly, the book discusses the formal synthesis of vindorosine based on the pyrrolo[2,3-d]carbazole construction using the gold-catalyzed cascade cyclization of ynamide. Importantly, the reaction using a chiral gold complex provides the optically active pyrrolo[2,3-d]carbazole. This strategy facilitates the rapid construction of the pyrrolocarbazole core structure of aspidosperma and related alkaloids, including vindorosine. These methodologies can accelerate the medicinal application of pyrrolocarbazole-type alkaloids and related compounds.

This useful reference describes the statistical planning and design of pharmaceutical experiments, covering all stages in the development process-including preformulation, formulation, process study and optimization, scale-up, and robust process and formulation development.Shows how to overcome pharmaceutical, technological, and economic constraints on experiment design!Directly comparing the advantages and disadvantages of specific techniques, Pharmaceutical Experimental DesignA* offers broad, detailed, up-to-date descriptions of designs and methods not easily accessible in other booksA* reviews screening designs for qualitative factors at different levelsA* presents designs for predictive models and their use in optimizationA* highlights optimization methods, such as steepest ascent, optimum path, canonical analysis, graphical analysis, and desirabilityA* discusses the Taguchi method for quality assurance and approaches for robust scaling up and process transferA* details nonstandard designs and mixturesA* analyzes factorial, D-optimal design, and offline quality assurance techniquesA* reveals how one experimental design evolves from anotherA* and more!Featuring over 700 references, tables, equations, and drawings, Pharmaceutical Experimental Design is suitable for industrial, research, and clinical pharmaceutical scientists, pharmacists, and pharmacologists; statisticians and biostatisticians; drug regulatory affairs personnel; biotechnologists; formulation, analytical, and synthetic chemists and engineers, quality assurance personnel; all users of statistical experimental design in research and development; and postgraduate and postdoctoral research workers in these disciplines.

Nanophytomedicine is a field that involves the application of nanomedicine-based systems to phytotherapy and phytopharmacology. This book assesses the clinical successes and failures of nanophytomedicine and also highlights emerging concepts in this field. The content is divided into three sections, the first of which describes core issues in the pharmaceuticals industry in connection with the successes, failures and prospects of nanophytomedicine. The second section highlights recent advances in phytomedicine formulation development based on nanotechnology approaches, while also discussing a variety of nanocarrier systems for the successful delivery of phytomedicines. Focusing on the clinical perspective, the third section addresses the current clinical status of nanophytomedicine as a single drug therapy or combinatorial drug therapy, pharmacovigilance, pharmacokinetics, drug interactions and toxicological profiles, while also providing concluding remarks on recent experimental findings, and considering ethical issues & regulatory challenges in nanophytomedicine. Given its scope, the book offers a valuable guide for early career researchers, young scientists, master level students, academics and industrial scientists working in various healthcare fields, e.g. the pharmaceutical and biological sciences, life sciences, biotechnology, biomedical engineering, and nanobiotechnology.

A reference on drug metabolism and metabolite safety in the development phase, this book reviews the analytical techniques and experimental designs critical for metabolite studies. It features case studies of lessons learned and real world examples, along with regulatory perspectives from the US FDA and EMA. Reviews the analytical techniques and experimental designs critical for metabolite studies Covers methods including chirality, species differences, mass spectrometry, radiolabels, and in vitro / in vivo correlation Discusses target pharmacology, in vitro systems aligned to toxicity tests, and drug-drug interactions Includes perspectives from authors with firsthand involvement in industry and the study of drug metabolites, including viewpoints that have influenced regulatory guidelines

This up-to-the-minute reference delineates-in a systematic fashion-the appropriate, sequential steps for the formulation of safe, effective, stable, and marketable liquid parenteral biopharmaceutical products-covering fundamentals and essential pathways for each phase as well as its purpose, function, and relation to other stages in the product development process.
Written by experts currently involved in state-of-the-art advances in the pharmaceutical drug industry, Development of Biopharmaceutical Parenteral Dosage Forms
details biopharmaceuticals that are licensed or undergoing clinical development, including genetically engineered cell and engineered vectors in the fermentation process
describes purification and characterization techniques for rDNA therapeutics, discussing several types of unit operations for isolation, purification, and characterization
considers preformulation and formulation requirements, such as physicochemical properties, drug delivery, stability studies programs, deactivation/denaturation routes, selection of compatible excipients, and regulatory compliance
elucidates basics of analytical techniques, methods development, separation methods using chromatographic and electrophoretic techniques, and bioactivity methods covering bioassays and immunoassays for quantifying the stability of biological activity
shows how to select the appropriate filter for maximizing compatibility and minimizing adsorption and inactivation, examining topics from basic filtration theories to future trends
reviews the selection process for compatible elastomeric closures, analyzing physical, chemical, toxicological properties, protein adsorption on elastomeric surfaces, strategies to reduce/eliminate adsorption, and specialized containers for biotechnological applications
and more
Furnished with helpful references, tables, and drawings, this practical guide is indispensable for pharmaceutical, medicinal, and protein chemists; molecular biologists; process engineers; purification scientists; biopharmaceutical and pharmaceutical formulators and product developers; quality control, quality assurance, and regulatory compliance personnel; and upper-level undergraduate and graduate students in these disciplines.

Pharmacology in Drug Discovery and Development: Understanding Drug Response, Second Edition, is an introductory resource illustrating how pharmacology can be used to furnish the tools necessary to analyze different drug behavior and trace this behavior to its root cause or molecular mechanism of action. The concepts discussed in this book allow for the application of more predictive pharmacological procedures aimed at increasing therapeutic efficacy that will lead to more successful drug development. Chapters logically build upon one another to show how to characterize the pharmacology of any given molecule and allow for more informed predictions of drug effects in all biological systems. New chapters are dedicated to the interdisciplinary drug discovery environment in both industry and academia, and special techniques involved in new drug screening and lead optimization. This edition has been fully revised to address the latest advances and research related to real time kinetic assays, pluridimensional efficacy, signaling bias, irreversible and chemical antagonism, allosterically-induced bias, pharmacokinetics and safety, target and pathway validation, and much more. With numerous valuable chapter summaries, detailed references, practical examples and case studies throughout, Dr. Kenakin successfully navigates a highly complex subject, making it accessible for students, professors, and new researchers working in pharmacology and drug discovery.

This incomparable Second Edition of a highly regarded reference has been entirely rewritten and enlarged to reflect the explosion of information and technologies that have emerged since the publication of the previous edition.
Strikes the perfect balance between proven traditional approaches and modern methods that promise to yield new products and processes
Specifically addressing microbially derived commercially important bioactive products that are currently or soon-to-be available, Biotechnology of Antibiotics, Second Edition
analyzes the use of recombinant enzymes to produce biologically active molecules, including a cholesterol-lowering agent, an anti-HIV drug for the treatment of AIDS, and b-lactam antibiotics
gives insight into the biochemistry, molecular biology, and production of antibiotics used as therapeutic agents
focuses on state-of-the-art techniques for the development of new antibiotics using novel approaches and strategies
highlights recent advances in the genetic manipulation of antibiotic biosynthesis genes to create structures from gene combinations for new biological activities
describes in detail the development and current status of newly created antibiotics and pharmacologically active natural products
and much more
Written by authorities from both industry and academia and containing nearly 4000 bibliographic citations, Biotechnology of Antibiotics, Second Edition is an outstanding resource for pharmaceutical scientists, medicinal chemists and biochemists, molecular biologists and industrial microbiologists, chemical engineers, fermentation bioengineers, bioprocess technologists, and upper-level undergraduate and graduate students in these disciplines.

This detailed book collects modern and established computer-based methods aimed at addressing the drug discovery challenge from disparate perspectives by exploiting information on ligand-protein recognition. Beginning with methods that allow for the exploration of specific areas of chemical space and the designing of virtual libraries, the volume continues with sections on methods based on docking, quantitative models, and molecular dynamics simulations, which are employed for ligand discovery or development, as well as methods exploiting an ensemble of protein structures for the identification of potential protein targets. Written for the highly successful Methods in Molecular Biology series, chapters include introductions to their respective topics, lists of the necessary materials, step-by-step, readily reproducible laboratory protocols, and tips on troubleshooting and avoiding known pitfalls. Authoritative and cutting-edge, Protein-Ligand Interactions and Drug Design provides detailed practical procedures of solid computer-aided drug design methodologies employed to rationalize and optimize protein-ligand interactions, for experienced researchers and novices alike.