GMP,药品,药学,制药,新药,色谱,药品生产,中药,药材,原料药,医药,中间体,药用辅料

<<Pharmacokinetics and Metabolism in Drug Design>>ebook

时间: 2012-04-24 12:51:01 作者: 来源: 字号:
申请上传英文版<<在药物设计中的药物动力学及新陈代谢>>by Dennis A. Smith,Han van de Waterbeemd andDon K. Walker
Preface
The present volume of the series Methods and Principles in Medicinal Chemistry
focuses on the impact of pharmacokinetics and metabolism in Drug Design. Pharmacokineticsis the study of the kinetics of absorption, distribution, metabolism, and excretio-n of drugs and their pharmacologic, therapeutic, or toxic response in animals and ma-n.In the last 10 years drug discovery has changed rapidly. Combinatorial chemistry
and high-throughput screening have been introduced widely and now form the core
of the Discovery organizations of major pharmaceutical and many small biotech
companies. However, the hurdles between a hit, a lead, a clinical candidate, and a
successful drug can be enormous.
The main reasons for attrition during development include pharmacokinetics and
toxicity. Common to both is drug metabolism. The science of drug metabolism has
developed over the last 30 years from a purely supporting activity trying to make the
best out of a development compound, to a mature partner in drug discovery. Drug
metabolism departments are now working closely together with project teams to discover well-balanced clinical candidates with a good chance of survival during development.
The present volume draws on the long career in drug metabolism and experience
in the pharmaceutical industry of Dennis Smith. Together with his colleagues Han
van de Waterbeemd and Don Walker, all key issues in pharmacokinetics and drug
metabolism, including molecular toxicology have been covered, making the medicinal
chemist feel at home with this highly important topic.
After a short introduction on physicochemistry, a number of chapters deal with
pharmacokinetics, absorption, distribution, and clearance. Metabolism and toxicity
are discussed in depth. In a further chapter species differences are compared and inter-species scaling is introduced. The final chapter deals with high(er) throughput
ADME studies, the most recent trend to keep pace with similar paradigms in other
areas of the industry, such as chemistry.
This book is a reflection of today's knowledge in drug metabolism and pharmacokinetics.However, there is more to come, when in the future the role and function
of various transporters is better understood and predictive methods have matured
further.
As series editors we would like to thank the authors for their efforts in bringing
this book to completion. No doubt the rich experience of the authors expressed in
X Preface this volume will be of great value to many medicinal chemists, experienced or junior,and this volume will be a treasure in many laboratories engaged in the synthesis of drugs.
Last, but not least we wish to express our gratitude to Gudrun Walter and Frank
Weinreich from Wiley-VCH publishers for the fruitful collaboration.
April 2001 Raimund Mannhold, Dusseldorf
Hugo Kubinyi, Ludwigshafen
Henk Timmerman, Amsterdam




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