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Cover image for Oral bioavailability assessment : basics and strategies for drug discovery and development
Title:
Oral bioavailability assessment : basics and strategies for drug discovery and development
Author:
El-Kattan, Ayman F., author.
ISBN:
9781118916940

9781118916933

9781118916926
Physical Description:
1 online resource
Contents:
Drug pharmacokinetics and toxicokinetics -- GIT anatomy and physiology and drug oral bioavailability : impact of species differences -- Drug routes of excretion -- Physicochemical and biopharmaceutical properties that affect drug absorption of compounds absorbed by passive diffusion -- Physicochemical and biopharmaceutical factors affecting hepatic/intestinal first pass effect -- Impact of intestinal efflux transporters on oral absorption -- Impact of influx transporters on drug -- Extended Clearance Classification System (ECCS) and its utility in predicting clearance rate determining step in drug discovery -- In vitro and in situ approaches to measure intestinal permeability and efflux transporters -- In silico approaches to predict intestinal permeability -- In vivo preclinical approaches to deconvolute the contribution of first pass effect from oral absorption -- In vitro approaches to assess haptic metabolism and first pass effect -- The utility of ECCS as a roadmap to improve oral bioavailability of new molecular entities : industrial perspective.
Abstract:
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.
Local Note:
John Wiley and Sons
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