READINGS IN ADVANCED PHARMACOKINETICS – THEORY, METHODS AND APPLICATIONS doc

READINGS IN ADVANCED PHARMACOKINETICS – THEORY, METHODS AND APPLICATIONS Edited by Ayman Noreddin Readings in Advanced Pharmacokinetics – Theory, Methods and Applications Edited by Ayman Noreddin Published by InTech Janeza Trdine 9, 51000 Rijeka, Croatia Copyright © 2012 InTech All chapters are Open Access distributed under the Creative Commons Attribution 3.0 license, which allows users to download, copy and build upon published articles even for commercial purposes, as long as the author and publisher are properly credited, which ensures maximum dissemination and a wider impact of our publications. After this work has been published by InTech, authors have the right to republish it, in whole or part, in any publication of which they are the author, and to make other personal use of the work. Any republication, referencing or personal use of the work must explicitly identify the original source. As for readers, this license allows users to download, copy and build upon published chapters even for commercial purposes, as long as the author and publisher are properly credited, which ensures maximum dissemination and a wider impact of our publications. Notice Statements and opinions expressed in the chapters are these of the individual contributors and not necessarily those of the editors or publisher. No responsibility is accepted for the accuracy of information contained in the published chapters. The publisher assumes no responsibility for any damage or injury to persons or property arising out of the use of any materials, instructions, methods or ideas contained in the book. Publishing Process Manager Iva Simcic Technical Editor Teodora Smiljanic Cover Designer InTech Design Team First published April, 2012 Printed in Croatia A free online edition of this book is available at www.intechopen.com Additional hard copies can be obtained from orders@intechopen.com Readings in Advanced Pharmacokinetics – Theory, Methods and Applications, Edited by Ayman Noreddin p. cm. ISBN 978-953-51-0533-6 Contents Preface IX Section 1 Advanced Concepts 1 Chapter 1 Bioequivalence Studies 3 Aisha Qayyum Chapter 2 Computer Simulations as a Tool for Optimizing Bioequivalence Trials 17 Carmen Navarro-Fontestad,Victor Mangas-Sanjuán, Isabel González-Álvarez, Alfredo García-Arieta, Carlos Fernández-Teruel, Vicente G. Casabó-Alós and Marival Bermejo Chapter 3 Evaluation of Percutaneous Drug Permeation Using a Lateral Sectioning Approach 35 Nobuhiro Goi, Katsunori Morishita, Akihito Taniguchi and Takayuki Ishii Chapter 4 Pharmacogenomics Dictate Pharmacokinetics: Polymorphisms in Drug-Metabolizing Enzymes and Drug-Transporters 55 Debasis Mondal, Samantha L. Gerlach, Amrita Datta, Geetika Chakravarty and Asim B. Abdel-Mageed Chapter 5 Genetic Variation in Drug Disposition 101 Balmukunda Regmi and Laxman Bharati Chapter 6 Application of Pharmacokinetics/Pharmacodynamics (PK/PD) in Designing Effective Antibiotic Treatment Regimens 111 Ghada F. Ahmed and Ayman M. Noreddin Chapter 7 Pharmacokinetics and Drug Interactions of Herbal Medicines: A Missing Critical Step in the Phytomedicine/Drug Development Process 127 Obiageri O. Obodozie VI Contents Chapter 8 Pharmacokinetics of Antimicrobials in Food Producing Animals 157 S. K. Bhavsar and A. M. Thaker Chapter 9 Comparative Veterinary Pharmacokinetics 179 Akos Jerzsele Section 2 Methods and Applications 199 Chapter 10 Observer-Based Strategies for Anesthesia Drug Concentration Estimation 201 Jin-Oh Hahn, Guy A. Dumont and J. Mark Ansermino Chapter 11 Optimal Pharmacokinetics of Cyclosporine and Tacrolimus Based Relationship Among AUC, Trough and Peak Concentration 217 Hironori Takeuchi Chapter 12 Pharmacokinetics and Metabolized Caroteniods in Liver of Single Dose Administration in Fancy Carp (Cyprinus carpio) 237 Bundit Yuangsoi Chapter 13 Correlation of in vitro Dissolution Profiles with in vivo Pharmacokinetic Parameters of Some Commercial Brands of Aspirin Tablets Marketed in Nigeria 251 Emmanuel Adelaja Bamigbola Chapter 14 Bioavailability of Citrus Polymethoxylated Flavones and Their Biological Role in Metabolic Syndrome and Hyperlipidemia 267 Malkanthi Evans, Prachi Sharma and Najla Guthrie Chapter 15 Role of Aldehyde Oxidase and Xanthine Oxidase in the Metabolism of Purine-Related Drugs 285 Mohammad-Reza Rashidi and Roghiyeh Pashaei-Asl Chapter 16 Pharmacokinetic/Pharmacodynamic (PK/PD) Modeling of Anti-Neoplastic Agents 315 Daniel Lexcen, Ahmed Salem, Walid M. El-Khatib, Virginia Haynes and Ayman Noreddin Chapter 17 Pharmacokinetic (PK) and Pharmacodynamic Profiles of Artemisinin Derivatives Influence Drug Neurotoxicity in Animals 323 Qigui Li and Mark Hickman Contents VII Chapter 18 One Step Closer to the Target: Intracellular Pharmacokinetics of Gemcitabine 357 Matthew Links and Peter Galettis Preface Despite the increasing attention on the topic of pharmacokinetics our understanding of advanced concepts and its applications in drug development remains limited. The intention of this book is to bridge the theory-practice gap by providing advanced pharmacokinetics concepts, methods, and applications. Graduate students as well as scientists in the area of clinical pharmacology and pharmacokinetics will find the contents of this book very enlightening and helpfull. The comprehensive coverage of topics on pharmacokinetics in this book offers readers “à la carte” choice to build their knowledge based on their scientific needs. I would like to personally thank all the authors for their excellent contributions to the book. These researchers are at the forefront of innovation in pharmacokinetics and its application to the clinical science and to drug development. Ayman Noreddin MS, PhD, RPh Associate Professor and Chair, Department of Pharmacy Practice, School of Pharmacy, Hampton University USA [...]... models of increasing complexity starting with a model considering hepatic first pass effect under linear and non linear conditions, then, adding the intestinal metabolic step and finally considering the existence of two metabolic pathways of different magnitude The latest addition to those models is the involvement 20 Readings in Advanced Pharmacokinetics – Theory, Methods and Applications of intestinal... on other data in the application For certain drug products, bioavailability or bioequivalence may be demonstrated by evidence obtained in vitro in lieu of in vivo data The FDA may waive the requirement of the submission of in vivo data if a drug product meets the following criteria: 12 Readings in Advanced Pharmacokinetics – Theory, Methods and Applications     The drug product is in the same dosage... drug products In the 2003 United States Food and Drug Administration (FDA) guidance, bioavailability is defined as: “the rate and extent to which the active ingredient or active moiety is absorbed from a drug product and becomes available at the site of action For drug products that are not 4 Readings in Advanced Pharmacokinetics – Theory, Methods and Applications intended to be absorbed into the blood... Evaluation and Research (CDER), January 2001 Available from: http://www.fda.gov/downloads/Drugs/GuidanceComplianceRegulatoryInform ation/Guidances/ucm070244.pdf FDA (2001b) Guidance for industry, Bioanalytical Method Validation U.S Department of Health and Human Services Food and Drug Administration, Center for Drug 14 Readings in Advanced Pharmacokinetics – Theory, Methods and Applications Evaluation and. .. of the active ingredient and when appropriate, its active metabolites are measured as a function of time if this effect can be measured with adequate accuracy, sensitivity and reproducibility 6   Readings in Advanced Pharmacokinetics – Theory, Methods and Applications Well-controlled clinical trials that establish the efficacy and safety of the drug product, for purpose of determining bioavailability,... combining high and low permeability (Ka) and solubility (S)  High and low intrinsic hepatic clearance (Clint,0H)  High and low inter-individual variability in intrinsic hepatic clearance (this point will be explained in detail in the model)  High and low Michaelis-Menten constant (KmH): differences between this parameter and liver drug concentrations defines the metabolic pathway saturation so when... flow (ΦH), and the intrinsic clearance at concentration C(Clint, CH) EH  Clint,CH Clint,CH   H (7) in which Clint, CH is Clint,CH  Clint, 0 H· KmH KmH  C 2 (8) Thus Clint, CH is a non-linear function of three parameters: clearance at infinite blood flow and zero hepatic concentration (Clint, 0H), the Michaelis-Menten value (KmH) and liver drug concentration (C2) Thanks to this modeling of the... metabolism and the non-linearity of the metabolic processes are the controversial aspects that require harmonization with regards to analyte selection The lack of agreement in FDA and EMEA/EMA recommendations and the changes in the new This article reflects the author’s personal opinion and not necessarily the policy or recommendations of the AEMPS * 18 Readings in Advanced Pharmacokinetics – Theory, Methods. .. gut (5) where VmE and KmE are the Michaelis-Menten parameters and Cgut is the concentration in gut wall 3 The drug is partially metabolized in the liver (E4) after its absorption: E4   H· EH·C 2 (6) 24 Readings in Advanced Pharmacokinetics – Theory, Methods and Applications The hepatic metabolic rate E4 depends on the hepatic blood flow (ΦH), the drug concentration in the liver (C2) and the hepatic... T R 8 Readings in Advanced Pharmacokinetics – Theory, Methods and Applications Under most of the conditions blood or plasma is collected rather than urine or tissue Blood samples are drawn at appropriate times to assess the absorption, distribution and elimination phases of the drug For most of the drugs 12-18 samples are recommended including pre-dose sample from each subject Generally sampling for . READINGS IN ADVANCED PHARMACOKINETICS – THEORY, METHODS AND APPLICATIONS Edited by Ayman Noreddin Readings in Advanced Pharmacokinetics – Theory, Methods and Applications. product and becomes available at the site of action. For drug products that are not Readings in Advanced Pharmacokinetics – Theory, Methods and Applications 4 intended to be absorbed into. Readings in Advanced Pharmacokinetics – Theory, Methods and Applications 6  Well-controlled clinical trials that establish the efficacy and safety of the drug product, for purpose of determining