Thông tin tài liệu
APPLICATIONS
OF MICRODIALYSIS
IN PHARMACEUTICAL
SCIENCE
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APPLICATIONS
OF MICRODIALYSIS
IN PHARMACEUTICAL
SCIENCE
Edited by
TUNG-HU TSAI
National Yang-Ming University
Taipei, Taiwan
A JOHN WILEY & SONS, INC., PUBLICATION
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Copyright © 2011 by John Wiley & Sons, Inc. All rights reserved.
Published by John Wiley & Sons, Inc., Hoboken, New Jersey.
Published simultaneously in Canada.
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Library of Congress Cataloging-in-Publication Data:
Applications of microdialysis in pharmaceutical science / [edited by] Tung-Hu Tsai.
p. ; cm.
Includes bibliographical references and index.
ISBN 978-0-470-40928-2 (cloth : alk. paper)
1. Pharmaceutical chemistry. 2. Drug development. 3. Brain macrodialysis.
I. Tsai, Tung-Hu.
[DNLM: 1. Chemistry, Pharmaceutical–methods. 2. Microdialysis–methods. QV 744]
RM301.25.A67 2011
615'.19–dc22
2011010963
Printed in Singapore
oBook ISBN: 9781118011294
ePDF ISBN: 9781118011270
ePub ISBN: 9781118011287
10 9 8 7 6 5 4 3 2 1
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CONTENTS
CONTRIBUTORS xi
1 Introduction to Applications of Microdialysis in
Pharmaceutical Science 1
Tung-Hu Tsai
2 Microdialysis in Drug Discovery 7
Christian Höcht
1. Introduction, 7
2. Phases of Drug Development, 8
3. Role of Biomarkers in Drug Development, 11
4. Role of Pharmacokinetic–Pharmacodynamic Modeling
in Drug Development, 12
5. Role of Microdialysis in Drug Development, 15
6. Microdialysis Sampling in the Drug Development of
Specifi c Therapeutic Groups, 20
7. Regulatory Aspects of Microdialysis Sampling in
Drug Development, 29
8. Conclusions, 30
3 Analytical Considerations for Microdialysis Sampling 39
Pradyot Nandi, Courtney D. Kuhnline, and Susan M. Lunte
1. Introduction, 39
2. Analytical Methodologies, 49
3. Conclusions, 75
v
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vi CONTENTS
4 Monitoring Dopamine in the Mesocorticolimbic and Nigrostriatal
Systems by Microdialysis: Relevance for Mood Disorders and
Parkinson’s Disease 93
Giuseppe Di Giovanni, Massimo Pierucci, and Vincenzo Di Matteo
1. Introduction, 93
2. Pathophysiology of Serotonin–Dopamine Interaction:
Implication for Mood Disorders, 94
3. Dopamine Depletion in the Nigrostriatal System:
Parkinson’s Disease, 109
4. Conclusions, 120
5 Monitoring Neurotransmitter Amino Acids by Microdialysis:
Pharmacodynamic Applications 151
Sandrine Parrot, Bernard Renaud, Luc Zimmer, and Luc Denoroy
1. Introduction, 151
2. Monitoring Neurotransmitter Amino Acids
by Microdialysis, 152
3. Basic Research on Receptors, 162
4. Psychostimulants and Addictive Drugs, 168
5. Analgesia, 177
6. Ischemia–Anoxia, 182
7. Conclusions and Perspectives, 188
6 Microdialysis as a Tool to Unravel Neurobiological
Mechanisms of Seizures and Antiepileptic Drug Action 207
Ilse Smolders, Ralph Clinckers, and Yvette Michotte
1. Introduction, 207
2. Microdialysis to Characterize Seizure-Related
Neurobiological and Metabolic Changes in Animal Models
and in Humans, 209
3. Microdialysis as a Chemoconvulsant Delivery Tool in
Animal Seizure Models, 217
4. Microdialysis Used to Elucidate Mechanisms of
Electrical Brain Stimulation and Neuronal Circuits
Involved in Seizures, 218
5. Microdialysis Used to Unravel the Mechanisms of
Action of Established Antiepileptic Drugs and
New Therapeutic Strategies, 219
6. Microdialysis Studies in the Search for Mechanisms
of Adverse Effects of Clinically Used Drugs, Drugs of
Abuse, and Toxins, 224
7. Combining Microdialysis with Other Complementary
Neurotechniques to Unravel Mechanisms of Seizures
and Epilepsy, 226
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CONTENTS vii
8. The Advantage of Microdialysis Used to Sample Biophase
Antiepileptic Drug Levels and to Monitor Neurotransmitters
as Markers for Anticonvulsant Activity, 228
9. Microdialysis Used to Study Relationships Between
Epilepsy and Its Comorbidities, 236
7 Microdialysis in Lung Tissue: Monitoring of Exogenous
and Endogenous Compounds 255
Thomas Feurstein and Markus Zeitlinger
1. Introduction, 255
2. Special Aspects Associated with Lung Microdialysis
Compared to Microdialysis in Other Tissues, 255
3. Insertion of Microdialysis Probes into Lung Tissue, 256
4. Insertion of Microdialysis Probes into the
Bronchial System, 257
5. Types of Probes, 258
6. Endogenous Compounds, 258
7. Exogenous Drugs, 259
8. Animal Data, 260
9. Clinical Data, 262
10. Comparison of Pharmacokinetic Data in
Lung Obtained by Microdialysis and Other Techniques, 264
11. Predictability of Lung Concentrations by Measurements
in Other Tissues, 265
8 Microdialysis in the Hepatobiliary System: Monitoring
Drug Metabolism, Hepatobiliary Excretion, and
Enterohepatic Circulation 275
Yu-Tse Wu and Tung-Hu Tsai
1. Introduction, 275
2. Experimental Considerations of Pharmacokinetic
Studies, 279
3. Pharmacokinetic and Hepatobiliary Excretion Studies
Employing Microdialysis, 284
4. Conclusions, 287
9 Microdialysis Used to Measure the Metabolism of Glucose,
Lactate, and Glycerol 295
Greg Nowak
1. Introduction, 295
2. Glucose, 299
3. Lactate, 301
4. Lactate/Pyruvate Ratio, 303
5. Glycerol, 303
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viii CONTENTS
10 Clinical Microdialysis in Skin and Soft Tissues 313
Martina Sahre, Runa Naik, and Hartmut Derendorf
1. Introduction, 313
2. Tissue Bioavailability, 314
3. PK–PD Indices, 323
4. Topical Bioequivalence, 329
5. Endogenous Compounds, 330
6. Conclusions, 331
11 Microdialysis on Adipose Tissue: Monitoring Tissue
Metabolism and Blood Flow in Humans 335
Gijs H. Goossens, Wim H. M. Saris, and Ellen E. Blaak
1. Introduction, 335
2. Principles and Practical Considerations in the Use of
Microdialysis on Adipose Tissue, 336
3. Use of Microdialysis on Adipose Tissue in Humans, 342
4. Summary and Conclusions, 353
12 Microdialysis as a Monitoring System for Human Diabetes 359
Anna Ciechanowska, Jan M. Wojcicki, Iwona Maruniak-Chudek,
Piotr Ladyzynski, and Janusz Krzymien
1. Introduction, 359
2. Monitoring Acute Complications of Diabetes, 362
13 Microdialysis Use in Tumors: Drug Disposition and
Tumor Response 403
Qingyu Zhou and James M. Gallo
1. Introduction, 403
2. Microdialysis as a Sampling Technique in Oncology, 404
3. Experimental Considerations, 408
4. Examples of the Use of Microdialysis to Characterize Drug
Disposition in Tumor, 414
5. Use of Microdialysis in the Evaluation of Tumor Response
to Therapy, 423
6. Conclusions and Future Perspectives, 423
14 Microdialysis Versus Imaging Techniques for In Vivo
Drug Distribution Measurements 431
Martin Brunner
1. Introduction, 431
2. Microdialysis, 432
3. Imaging Techniques, 434
4. Magnetic Resonance Imaging and Magnetic Resonance
Spectroscopy, 434
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CONTENTS ix
5. Positron–Emission Tomography, 435
6. Combination of Microdialysis and Imaging Techniques, 436
7. Summary and Conclusions, 438
15 In Vitro Applications of Microdialysis 445
Wen-Chuan Lee and Tung-Hu Tsai
1. Introduction, 445
2. Microdialysis Used in Culture Systems, 446
3. Microdialysis Used in Enzyme Kinetics, 453
4. Microdialysis Used in Protein Binding, 455
5. Conclusions, 456
16 Microdialysis in Drug–Drug Interaction 465
Mitsuhiro Wada, Rie Ikeda, and Kenichiro Nakashima
1. Introduction, 465
2. Pharmacokinetic Drug–Drug Interaction, 472
3. Pharmacodynamic Drug–Drug Interaction, 487
4. Conclusions, 501
17 Microdialysis in Environmental Monitoring 509
Manuel Miró and Wolfgang Frenzel
1. Introduction, 509
2. In Vivo and In Situ Sampling: Similarities and Differences, 510
3. Critical Parameters Infl uencing Relative Recoveries, 513
4. Detection Techniques, 518
5. Calibration Methods, 519
6. Environmental Applications of Microdialysis, 520
7. Conclusions and Future Trends, 524
INDEX 531
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CONTRIBUTORS
Ellen E. Blaak, Maastricht University Medical Centre, Maastricht, The
Netherlands
Martin Brunner, Medical University of Vienna, Vienna, Austria
Anna Ciechanowska, Polish Academy of Sciences, Warsaw, Poland
Ralph Clinckers, Vrije Universiteit Brussels, Brussels, Belgium
Luc Denoroy, Universit é de Lyon and Lyon Neuroscience Research Center,
BioRaN Team, Lyon, France; Universit é Lyon 1, Villeurbanne, France
Hartmut Derendorf, University of Florida, Gainesville, Florida
Giuseppe Di Giovanni, University of Malta, Msida, Malta; Cardiff University,
Cardiff, UK
Vincenzo Di Matteo, Istituto di Richerche Farmacologiche Consorzio Mario
Negri Sud, Santa Maria Imbaro, Italy
Thomas Feurstein, Medical University of Vienna, Vienna, Austria
Wolfgang Frenzel, Technical University of Berlin, Berlin, Germany
James M. Gallo, Mount Sinai School of Medicine, New York, New York
Gijs H. Goossens, Maastricht University Medical Centre, Maastricht, The
Netherlands
Christian H ö cht, Universidad de Buenos Aires, Buenos Aires, Argentina
Rie Ikeda, Nagasaki University, Nagasaki, Japan
Janusz Krzymien, Medical University of Warsaw, Warsaw, Poland
xi
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xii CONTRIBUTORS
Courtney D. Kuhnline, University of Kansas, Lawrence, Kansas
Piotr Ladyzynski, Polish Academy of Sciences, Warsaw, Poland
Wen - Chuan Lee, National Yang - Ming University, Taipei, Taiwan
Susan M. Lunte, University of Kansas, Lawrence, Kansas
Iwona Maruniak - Chudek, Medical University of Silesia, Katowice, Poland
Yvette Michotte, Vrije Universiteit Brussels, Brussels, Belgium
Manuel Mir ó , University of the Balearic Islands, Palma de Mallorca, Illes
Balears, Spain
Runa Naik, University of Florida, Gainesville, Florida
Kenichiro Nakashima, Nagasaki University, Nagasaki, Japan
Pradyot Nandi, University of Kansas, Lawrence, Kansas
Greg Nowak, Karolinska Institute, Karolinska University Hospital Huddinge,
Stockholm, Sweden
Sandrine Parrot, Universit é de Lyon and Lyon Neuroscience Research Center,
NeuroChem, Lyon, France; Universit é Lyon 1, Villeurbanne, France
Massimo Pierucci, University of Malta, Msida, Malta
Bernard Renaud, Universit é de Lyon and Lyon Neuroscience Research
Center, NeuroChem, Lyon, France; Universit é Lyon 1, Villeurbanne, France
Martina Sahre, University of Florida, Gainesville, Florida
Wim H. M. Saris, Maastricht University Medical Centre, Maastricht, The
Netherlands
Ilse Smolders, Vrije Universiteit Brussels, Brussels, Belgium
Tung - Hu Tsai, National Yang - Ming University and Taipei City Hospital,
Taipei, Taiwan
Mitsuhiro Wada, Nagasaki University, Nagasaki, Japan
Jan M. Wojcicki, Polish Academy of Sciences, Warsaw, Poland
Yu - Tse Wu, National Yang - Ming University, Taipei, Taiwan
Markus Zeitlinger, Medical University of Vienna, Vienna, Austria
Qingyu Zhou, Mount Sinai School of Medicine, New York, New York
Luc Zimmer, Universit é de Lyon and Lyon Neuroscience Research Center,
BioRaN Team, Lyon, France; Universit é Lyon 1, Villeurbanne, France
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[...]... estimation of accurate PK–PD models of new chemical entities is possible by means of microdialysis PET Microdialysis is also well suited for the determination of drug protein binding during early drug development The microdialysis technique allows the determination of in vivo protein binding using microdialysis sampling in blood and simultaneous blood sampling [33,34] The in vivo determination of protein binding... binding using the microdialysis method permits a more accurate determination of protein binding with regard to in vitro protocols, because it was found that in vitro determination systematically underestimated the unbound fraction [35] In addition, microdialysis permits the determination of the temporal course of protein binding in the same animal to determine saturation of the plasma protein binding... agonist of the c02.indd 23 7/11/2011 12:15:03 PM 24 MICRODIALYSIS IN DRUG DISCOVERY nicotinic acetylcholine receptor α4β2 subtype, in vivo microdialysis in freely moving rats showed that oral administration of varenicline caused moderate increases in dopamine release in the nucleus accumbens, inducing maximal response after 2 h of varenicline dosing [58] In addition, it was found that maximal dopamine... process In addition, as regards the role of PK–PD modeling during all stages of drug development and the ability of microdialysis for continuous monitoring of tissue extracellular levels of drugs and their effect on biochemical markers, this technique allows an early proof of concept of the activity of new chemical entities in the first stages of drug development, especially in preclinical models of efficacy... application of microdialysis in drug development (Table 5) As most cen- c02.indd 20 7/11/2011 12:15:03 PM 21 MICRODIALYSIS SAMPLING TABLE 5 Role of Microdialysis in Drug Development of Centrally Acting Drugs Therapeutic Group Utility of Microdialysis Sampling Antiepileptic drugs Estimation of hippocampal bioavailability Assessment of compromise of efflux transporters in brain distribution Assessment of neurochemical... essential in the preclinical phase of drug development, because these in vitro systems can speed up the processes of screening lead compounds, assessing metabolic stability, and evaluating permeation across membranes such as the gastrointestinal tract and the blood–brain barrier Microdialysis sampling of cell culture systems, enzyme kinetics, and proteinbinding assays are discussed in Chapter 15 Drug interaction... topic for clinical pharmacy, especially since the incidence of drug interactions is expected to increase with the increasing number of new drugs brought to the market Exploring the relevance and mechanisms of drug interactions will assist clinicians in avoiding these often serious events Herbal products, dietary supplements, and foods can also induce drug interactions The reduced concentration of a free-form... PK–PD relationships of lead compounds in animal models of efficacy, this technique allows an early determination of the proof of concept of new chemical entities during preclinical drug development and selection of the most adequate dosing interval for phase I clinical trials Although microdialysis could also contribute in early phases of clinical drug development, its applicability in human studies could... aspect of microdialysis technique is highly interesting for evaluation of the brain/plasma ratio in animal models of efficacy Moreover, regional distribution in brain parenchyma of central-acting drugs could be assessed by means of implantation of several probes in different central nuclei It is important to mention that imaging techniques also permit assessment of the time profile of tissue pharmacokinetics... 1 Aspects of Various Phases of Drug Development and the Utility of Microdialysis Sampling 467 335 Costs ($ millions) N.A N.A ++ +++++ N.A Applicability of Microdialysisa 10 MICRODIALYSIS IN DRUG DISCOVERY Another important objective of preclinical drug development is the establishment of the dosing interval of lead compounds to be used in early clinical trials At this point, development of mechanism-based . APPLICATIONS
OF MICRODIALYSIS
IN PHARMACEUTICAL
SCIENCE
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APPLICATIONS
OF MICRODIALYSIS.
1. Introduction, 445
2. Microdialysis Used in Culture Systems, 446
3. Microdialysis Used in Enzyme Kinetics, 453
4. Microdialysis Used in Protein Binding,
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