Applied biopharmaceutics & pharmacokinetics:
Gespeichert in:
Vorheriger Titel: | Shargel, Leon, 1941- Applied biopharmaceutics & pharmacokinetics |
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Format: | Buch |
Sprache: | English |
Veröffentlicht: |
New York
McGraw Hill
[2016]
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Ausgabe: | Seventh edition |
Schriftenreihe: | McGraw Hill education
|
Schlagworte: | |
Online-Zugang: | Inhaltsverzeichnis Klappentext |
Beschreibung: | xvii, 910 Seiten Illustrationen, Diagramme |
ISBN: | 9780071830935 |
Internformat
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245 | 1 | 0 | |a Applied biopharmaceutics & pharmacokinetics |c editors: Leon Shargel, Andrew B. C. Yu |
246 | 1 | 3 | |a Applied biopharmaceutics and pharmacokinetics |
250 | |a Seventh edition | ||
264 | 1 | |a New York |b McGraw Hill |c [2016] | |
300 | |a xvii, 910 Seiten |b Illustrationen, Diagramme | ||
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Datensatz im Suchindex
_version_ | 1804177032665366528 |
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adam_text | Contributors xi
Preface xv
Preface to First Edition xvii
1. Introduction to Biopharmaceutics and
Pharmacokinetics 1
Drug Product Performance 1
Biopharmaceutics 1
Pharmacokinetics 4
Pharmacodynamics 4
Clinical Pharmacokinetics 5
Practical Focus 8
Pharmacodynamics 10
Drug Exposure and Drug Response 10
Toxicokinetics and Clinical Toxicology 10
Measurement of Drug Concentrations 11
Basic Pharmacokinetics and Pharmacokinetic
Models 15
Chapter Summary 21
Learning Questions 22
Answers 23
References 25
Bibliography 25
2. Mathematical Fundamentals in
Pharmacokinetics 27
Calculus 27
Graphs 29
Practice Problem 31
Mathematical Expressions and Units 33
Units for Expressing Blood Concentrations 34
Measurement and Use of Significant Figures 34
Practice Problem 35
Practice Problem 36
Rates and Orders of Processes 40
Chapter Summary 42
Learning Questions 43
Answers 46
References 50
3. Biostatistics 51
Variables 51
Types of Data (Nonparametric Versus Parametric) 51
Distributions 52
Measures of Central Tendency 53
Measures of Variability 54
Hypothesis Testing 56
Statistically Versus Clinically Significant
Differences 58
Statistical Inference Techniques in Hypothesis
Testing for Parametric Data 59
Goodness of Fit 63
Statistical Inference Techniques for Hypothesis
Testing With Nonparametric Data 63
Controlled Versus Noncontrolled Studies 66
Blinding 66
Confounding 66
Validity 67
Bioequivalence Studies 68
Evaluation of Risk for Clinical Studies 68
Chapter Summary 70
Learning Questions 70
Answers 72
References 73
4. One-Compartment Open Model:
Intravenous Bolus Administration 75
Elimination Rate Constant 76
Apparent Volume of Distribution 77
Clearance 80
Clinical Application 85
Calculation of k From Urinary Excretion Data 86
Practice Problem 87
Practice Problem 88
Clinical Application 89
Chapter Summary 90
Learning Questions 90
Answers 92
Reference 96
Bibliography 96
5. Multicompartment Models:
Intravenous Bolus Administration 97
Two-Compartment Open Model 100
Clinical Application 105
V»
CONTENTS
Practice Problem 107
Practical Focus 107
Practice Problem 110
Practical Focus 113
Three-Compartment Open Model 114
Clinical Application 115
Clinical Application 116
Determination of Compartment Models 116
Practical Focus 117
Clinical Application 118
Practical Problem 120
Clinical Application 121
Practical Application 121
Clinical Application 122
Chapter Summary 123
Learning Questions 124
Answers 126
References 128
Bibliography 129
6. Intravenous Infusion 131
One-Compartment Model Drugs 131
Infusion Method for Calculating Patient Elimination
Half-Life 135
Loading Dose Plus IV Infusion—One-Compartment
Model 136
Practice Problems 138
Estimation of Drug Clearance and Vu From infusion
Data 140
Intravenous Infusion of Two-Compartment Model
Drugs 141
Practical Focus 142
Chapter Summary 144
Learning Questions 144
Answers 146
Reference 148
Bibliography 148
7. Drug Elimination, Clearance, and
Renal Clearance 149
Drug Elimination 149
Drug Clearance 150
Clearance Models 152
The Kidney 157
Clinical Application 162
Practice Problems 163
Renal Clearance 163
Determination of Renal Clearance 168
Practice Problem 169
Practice Problem 169
Relationship of Clearance to Elimination Half-Life
and Volume of Distribution 170
Chapter Summary 171
Learning Questions 171
Answers 172
References 175
Bibliography 175
8. Pharmacokinetics of Oral
Absorption 177
Introduction 177
Basic Principles of Physiologically Based
Absorption Kinetics (Bottom-Up Approach) 178
Absoroption Kinetics
(The Top-Down Approach) 182
Pharmacokinetics of Drug Absorption 182
Significance of Absorption Rate Constants 184
Zero-Order Absorption Model 184
Clinical Application—Transdermal Drug
Delivery 185
First-Order Absorption Model 185
Practice Problem 191
Chapter Summary 199
Answers 200
Application Questions 202
References 203
Bibliography 204
9. Multiple-Dosage Regimens 205
Drug Accumulation 205
Clinical Example 209
Repetitive Intravenous Injections 210
Intermittent Intravenous Infusion 214
Clinical Example 216
Estimation of k and VD of Aminoglycosides in
Clinical Situations 217
Multiple-Oral-Dose Regimen 218
Loading Dose 219
Dosage Regimen Schedules 220
Clinical Example 222
Practice Problems 222
Chapter Summary 224
Learning Questions 225
Answers 226
References 228
Bibliography 228
10. Nonlinear Pharmacokinetics 229
Saturable Enzymatic Elimination Processes 231
Practice Problem 232
Practice Problem 233
Drug Elimination by Capacity-Limited
Pharmacokinetics: One-Compartment
Model, IV Bolus Injection 233
Practice Problems 235
Clinical Focus 242
Clinical Focus 243
Drugs Distributed as One-Compartment
Model and Eliminated by Nonlinear
Pharmacokinetics 243
CONTENTS
Vll
Clinical Focus 244
Chronopharmacokinetics and Time-Dependent
Pharmacokinetics 245
Clinical Focus 247
Bioavailability of Drugs That Follow Nonlinear
Pharmacokinetics 247
Nonlinear Pharmacokinetics Due to Drug-Protein
Binding 248
Potential Reasons for Unsuspected
Nonlinearity 251
Dose-Dependent Pharmacokinetics 252
Clinical Example 253
Chapter Summary 254
Learning Questions 254
Answers 255
References 257
Bibliography 258
Physiologic Drug Distribution and
Protein Binding 259
Physiologic Factors of Distribution 259
Clinical Focus 267
Apparent Volume Distribution 267
Practice Problem 270
Protein Binding of Drugs 273
Clinical Examples 275
Effect of Protein Binding on the Apparent Volume
of Distribution 276
Practice Problem 279
Clinical Example 280
Relationship of Plasma Drug-Protein Binding to
Distribution and Elimination 281
Clinical Examples 282
Clinical Example 284
Determinants of Protein Binding 285
Clinical Example 285
Kinetics of Protein Binding 286
Practical Focus 287
Determination of Binding Constants and Binding
Sites by Graphic Methods 287
Clinical Significance of Drug-Protein
Binding 290
Clinical Example 299
Clinical Example 300
Modeling Drug Distribution 301
Chapter Summary 302
Learning Questions 303
Answers 304
References 306
Bibliography 307
Drug Elimination and Hepatic
Clearance 309
Route of Drug Administration and Extrahepatic
Drug Metabolism 309
Practical Focus 311
Hepatic Clearance 311
Extrahepatic Metabolism 312
Enzyme Kinetics—Michaelis-Menten
Equation 313
Clinical Example 317
Practice Problem 319
Anatomy and Physiology of the Liver 321
Hepatic Enzymes Involved in the Biotransformation
of Drugs 323
Drug Biotransformation Reactions 325
Pathways of Drug Biotransformation 326
Drug Interaction Example 331
Clinical Example 338
First-Pass Effects 338
Hepatic Clearance of a Protein-Bound Drug:
Restrictive and Nonrestrictive Clearance From
Binding 344
Biliary Excretion of Drugs 346
Clinical Example 348
Role of Transporters on Hepatic Clearance
and Bioavailability 348
Chapter Summary 350
Learning Questions 350
Answers 352
References 354
Bibliography 355
Pharmacogenetics and Drug
Metabolism 357
Genetic Polymorphisms 358
Cytochrome P-450 Isozymes 361
Phase II Enzymes 366
Transporters 367
Chapter Summary 368
Glossary 369
Abbreviations 369
References 370
Physiologic Factors Related to Drug
Absorption 373
Drug Absorption and Design
of a Drug Product 373
Route of Drug Administration 374
Nature of Cell Membranes 377
Passage of Drugs Across Cell Membranes 378
Drug Interactions in the Gastrointestinal
Tract 389
Oral Drug Absorption 390
Oral Drug Absorption During Drug Product
Development 401
Methods for Studying Factors That Affect Drug
Absorption 402
Effect of Disease States on Drug Absorption 405
Miscellaneous Routes of Drug Administration 407
13*
VIII
CONTENTS
Chapter Summary 408
Learning Questions 409
Answers to Questions 410
References 411
Bibliography 414
15. Biopharmaceutic Considerations in
Drug Product Design and In Vitro Drug
Product Performance 415
Biopharmaceutic Factors and Rationale for Drug
Product Design 416
Rate-Limiting Steps in Drug Absorption 418
Physicochemical Properties of the Drug 420
Formulation Factors Affecting Drug Product
Performance 423
Drug Product Performance, In Vitro: Dissolution
and Drug Release Testing 425
Compendial Methods of Dissolution 429
Alternative Methods of Dissolution Testing 431
Dissolution Profile Comparisons 434
Meeting Dissolution Requirements 436
Problems of Variable Control in Dissolution
Testing 437
Performance of Drug Products: In Vitro-In Vivo
Correlation 437
Approaches to Establish Clinically Relevant Drug
Product Specifications 441
Drug Product Stability 445
Considerations in the Design of a Drug
Product 446
Drug Product Considerations 450
Clinical Example 456
Chapter Summary 461
Learning Questions 462
Answers 462
References 463
Bibliography 466
16. Drug Product Performance, In Vivo:
Bioavailability and Bioequivalence 469
Drug Product Performance 469
Purpose of Bioavailability and Bioequivalence
Studies 471
Relative and Absolute Availability 472
Practice Problem 474
Methods for Assessing Bioavailability and
Bioequivalence 475
In Vivo Measurement of Active Moiety or Moieties
in Biological Fluids 475
Bioequivalence Studies Based on Pharmacodynamic
Endpoints—In Vivo Pharmacodynamic (PD)
Comparison 478
Bioequivalence Studies Based on Clinical
Endpoints—Clinical Endpoint Study 479
In Vitro Studies 481
Other Approaches Deemed Acceptable
(by the FDA) 482
Bioequivalence Studies Based on Multiple
Endpoints 482
Bioequivalence Studies 482
Design and Evaluation of Bioequivalence
Studies 484
Study Designs 490
Crossover Study Designs 491
Clinical Example 496
Clinical Example 496
Pharmacokinetic Evaluation of the Data 497
The Partial AUC in Bioequivalence
Analysis 498
Examples of Partial AUC Analyses 499
Bioequivalence Examples 500
Study Submission and Drug Review Process 502
Waivers of In Vivo Bioequivalence Studies
(Biowaivers) 503
The Biopharmaceutics Classification System
(BCS) 507
Generic Biologies (Biosimilar Drug
Products) 510
Clinical Significance of Bioequivalence
Studies 511
Special Concerns in Bioavailability and
B ioequivalence Studies 512
Generic Substitution 514
Glossary 517
Chapter Summary 520
Learning Questions 520
Answers 525
References 526
17. Biopharmaceutical Aspects of the
Active Pharmaceutical Ingredient and
Pharmaceutical Equivalence 529
Introduction 529
Pharmaceutical Alternatives 533
Practice Problem 534
Bioequivalence of Drugs With Multiple
Indications 536
Formulation and Manufacturing Process
Changes 536
Size, Shape, and Other Physical Attributes of
Generic Tablets and Capsules 536
Changes to an Approved NDA or ANDA 537
The Future of Pharmaceutical Equivalence and
Therapeutic Equivalence 538
Biosimilar Drug Products 539
Historical Perspective 540
Chapter S ummary 541
Learning Questions 541
Answers 542
References 542
CONTENTS
ix
18. Impact of Biopharmaceutics on
Drug Product Quality and Clinical
Efficacy 545
Risks From Medicines 545
Risk Assessment 546
Drug Product Quality and Drug Product
Performance 547
Pharmaceutical Development 547
Example of Quality Risk 550
Excipient Effect on Drug Product
Performance 553
Practical Focus 554
Quality Control and Quality Assurance 554
Practical Focus 555
Risk Management 557
Scale-Up and Postapproval Changes (SUPAC) 558
Practical Focus 561
Product Quality Problems 561
Postmarketing Surveillance 562
Glossary 562
Chapter Summary 563
Learning Questions 564
Answers 564
References 565
Bibliography 565
19. Modified-Release Drug Products and
Drug Devices 567
Modified-Release (MR) Drug Products and
Conventional (Immediate-Release, IR)
Drug Products 567
Biopharmaceutic Factors 572
Dosage Form Selection 575
Advantages and Disadvantages of Extended-
Release Products 575
Kinetics of Extended-Release Dosage Forms 577
Pharmacokinetic Simulation of Extended-Release
Products 578
Clinical Examples 580
Types of Extended-Release Products 5 81
Considerations in the Evaluation of
Modified-Release Products 601
Evaluation of Modified-Release Products 604
Evaluation of In Vivo Bioavailability Data 606
Chapter Summary 608
Learning Questions 609
References 609
Bibliography 613
20. Targeted Drug Delivery Systems and
Biotechnological Products 615
Biotechnology 615
Drug Carriers and Targeting 624
Targeted Drug Delivery 627
Pharmacokinetics of Biopharmaceuticals 630
Bioequivalence of Biotechnology-Derived ,
Drug Products 631
Learning Questions 632
Answers 632
References 633
Bibliography 633
21. Relationship Between Pharmacokinetics
and Pharmacodynamics 635
Pharmacokinetics and Pharmacodynamics 635
Relationship of Dose to Pharmacologic Effect 640
Relationship Between Dose and Duration of
Activity (reff), Single IV Bolus Injection 643
Practice Problem 643
Effect of Both Dose and Elimination Half-Life on
the Duration of Activity 643
Effect of Elimination Half-Life on Duration of
Activity 644
Substance Abuse Potential 644
Drug Tolerance and Physical Dependency 645
Hypersensitivity and Adverse Response 646
Chapter Summary 673
Learning Questions 674
Answers 677
References 678
22. Application of Pharmacokinetics to
Clinical Situations 681
Medication Therapy Management 681
Individualization of Drug Dosage Regimens 682
Therapeutic Drug Monitoring 683
Clinical Example 690
Clinical Example 692
Design of Dosage Regimens 692
Conversion From Intravenous Infusion to
Oral Dosing 694
Determination of Dose 696
Practice Problems 696
Effect of Changing Dose ond Dosing Interval on
Cx C- and C 697
Determination of Frequency of Drug
Administration 698
Determination of Both Dose and Dosage
Interval 698
Practice Problem 699
Determination of Route of Administration 699
Dosing Infants and Children 700
Practice Problem 702
Dosing the Elderly 702
Practice Problems 703
Clinical Example 704
Dosing the Obese Patients 705
Pharmacokinetics of Drug Interactions 706
Inhibition of Drug Metabolism 710
X
CONTENTS
Inhibition of Monoamine Oxidase (MAO) 712
Induction of Drug Metabolism 712
Inhibition of Drug Absorption 712
Inhibition of Biliary Excretion 713
Altered Renal Reabsorption Due to Changing
Urinary pH 713
Practical Focus 713
Effect of Food on Drug Disposition 713
Adverse Viral Drug Interactions 714
Population Pharmacokinetics 714
Clinical Example 722
Regional Pharmacokinetics 724
Chapter Summary 725
Learning Questions 725
Answers 728
References 731
Bibliography 732
23. Application of Pharmacokinetics to
Specific Populations: Geriatric, Obese,
and Pediatric Patients 735
Specific and Special Populations 735
Module I: Application of Pharmacokinetics to the
Geriatric Patients 736
Summary 749
Learning Questions 749
Answers 750
References 751
Further Reading 754
Module II: Application of Pharmacokinetics to the
Obese Patients 754
Summary 760
Learning Questions 760
Answers 761
References 761
Module III: Application of Pharmacokinetics to the
Pediatric Patients 763
Summary 769
Learning Questions 770
Answers 771
References 773
24. Dose Adjustment in Renal and Hepatic
Disease 775
Renal Impairment 775
Pharmacokinetic Considerations 775
General Approaches for Dose Adjustment in Renal
Disease 777
Measurement of Glomerular Filtration Rate 779
Serum Creatinine Concentration and
Creatinine Clearance 780
Practice Problems 782
Dose Adjustment for Uremic Patients 785
Practice Problem 787
Practice Problem 792
Practice Problems 793
Practice Problem 795
Extracorporeal Removal of Drugs 796
Practice Problem 799
Clinical Examples 800
Effect of Hepatic Disease
on Pharmacokinetics 803
Practice Problem 805
Chapter Summary 809
Learning Questions 810
Answers 811
References 813
Bibliography 815
25. Empirical Models, Mechanistic
Models, Statistical Moments, and
Noncompartmental Analysis 817
Empirical Models 818
Mechanistic Models 822
Noncompartmental Analysis 835
Comparison of Different Approaches 842
Selection of Pharmacokinetic Models 844
Chapter Summary 845
Learning Questions 845
Answers 846
References 847
Bibliography 848
Appendix A Applications of
Software Packages in
Pharmacokinetics 851
Appendix B Glossary 875
Index 879
FROM THE FOREMOST AUTHOR TEAM IN
COMES THE NEW EDITION OF THE DISCIPLINE S AUTHORITATIVE TEXT
For over three decades Applied Biopharmaceutics and Pharmacokinetics has established itself
as the field s leading textbook. Since the first edition, Leon Shargel and Andrew Yu have built a
loyal following among pharmacy students who trust their unique insights drawn from personal
experience in clinical research, academia, pharmaceutical industy and regulatory affairs.
More than any other text, Applied Biopharmaceutics and Pharmacokinetics gives the reader
fundamental understanding of biopharmaceutics and pharmacokinetics principles that can
be applied to drug product development and drug therapy. Reinforcing this essential’coverage
are practice problems, clinical examples, FAQs, and learning questions—all designed to
enhance your knowledge that can be applied to pharmacokinetic/bioparmaceutical research
and drug therapy.
The seventh edition is now an edited textbook with contributions from nationally and
internationally known experts in their field. This new edition contains new and updated
chapters reflecting the rapid growth of knowledge and understanding of drug development
and therapeutic requirements associated with safe and efficacious drug therapy. Each page
provides an interactive guide that puts fundamentals of the discipline into practice.
• New chapter, Biostatistics, provides an introduction to topics such as risk concept,
non-inferiority, and other basic concepts in the evaluation of drug studies.
• New chapter, Application of Pharmacokinetics in Specific Populations, highlights
drug and patient related pharmacokinetics topics in various patient populations.
• New chapter, Biopharmaceutic Aspects of the Active Pharmaceutical Ingredient and
Pharmaceutical Equivalence” explains the synthesis, quality and physical/chemical
properties of the active paharmaceutical ingredients affect the bioavailability of
the drug from the drug product and clincial efficacy.
• Chapters are revised to reflect the latest perspectives on bioavailability,
bioequivalence, pharmacokinetics, pharmacodynamics and drug therapy.
• Focus on the critical evaluation of biopharmaceutics and its effect
on drug product performance.
• Guidance on working with real data to solve problems in
biopharmaceutics, pharmacokinetics and drug therapy.
• And more!
|
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author_GND | (DE-588)1145926010 (DE-588)172470196 |
building | Verbundindex |
bvnumber | BV044030188 |
classification_rvk | VX 8500 XI 1817 |
ctrlnum | (OCoLC)926639659 (DE-599)BVBBV044030188 |
dewey-full | 615/.7 |
dewey-hundreds | 600 - Technology (Applied sciences) |
dewey-ones | 615 - Pharmacology and therapeutics |
dewey-raw | 615/.7 |
dewey-search | 615/.7 |
dewey-sort | 3615 17 |
dewey-tens | 610 - Medicine and health |
discipline | Chemie / Pharmazie Medizin |
edition | Seventh edition |
format | Book |
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id | DE-604.BV044030188 |
illustrated | Illustrated |
indexdate | 2024-07-10T07:41:38Z |
institution | BVB |
isbn | 9780071830935 |
language | English |
oai_aleph_id | oai:aleph.bib-bvb.de:BVB01-029437475 |
oclc_num | 926639659 |
open_access_boolean | |
owner | DE-355 DE-BY-UBR |
owner_facet | DE-355 DE-BY-UBR |
physical | xvii, 910 Seiten Illustrationen, Diagramme |
publishDate | 2016 |
publishDateSearch | 2016 |
publishDateSort | 2016 |
publisher | McGraw Hill |
record_format | marc |
series2 | McGraw Hill education |
spelling | Applied biopharmaceutics & pharmacokinetics editors: Leon Shargel, Andrew B. C. Yu Applied biopharmaceutics and pharmacokinetics Seventh edition New York McGraw Hill [2016] xvii, 910 Seiten Illustrationen, Diagramme txt rdacontent n rdamedia nc rdacarrier McGraw Hill education Pharmakokinetik (DE-588)4115557-9 gnd rswk-swf Biopharmazie (DE-588)4006890-0 gnd rswk-swf Biopharmazie (DE-588)4006890-0 s DE-604 Pharmakokinetik (DE-588)4115557-9 s Shargel, Leon 1941- Sonstige (DE-588)1145926010 oth Yu, Andrew B. 1945- Sonstige (DE-588)172470196 oth Ersatz von Shargel, Leon, 1941- Applied biopharmaceutics & pharmacokinetics Digitalisierung UB Regensburg - ADAM Catalogue Enrichment application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=029437475&sequence=000003&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA Inhaltsverzeichnis Digitalisierung UB Regensburg - ADAM Catalogue Enrichment application/pdf http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=029437475&sequence=000004&line_number=0002&func_code=DB_RECORDS&service_type=MEDIA Klappentext |
spellingShingle | Applied biopharmaceutics & pharmacokinetics Pharmakokinetik (DE-588)4115557-9 gnd Biopharmazie (DE-588)4006890-0 gnd |
subject_GND | (DE-588)4115557-9 (DE-588)4006890-0 |
title | Applied biopharmaceutics & pharmacokinetics |
title_alt | Applied biopharmaceutics and pharmacokinetics |
title_auth | Applied biopharmaceutics & pharmacokinetics |
title_exact_search | Applied biopharmaceutics & pharmacokinetics |
title_full | Applied biopharmaceutics & pharmacokinetics editors: Leon Shargel, Andrew B. C. Yu |
title_fullStr | Applied biopharmaceutics & pharmacokinetics editors: Leon Shargel, Andrew B. C. Yu |
title_full_unstemmed | Applied biopharmaceutics & pharmacokinetics editors: Leon Shargel, Andrew B. C. Yu |
title_old | Shargel, Leon, 1941- Applied biopharmaceutics & pharmacokinetics |
title_short | Applied biopharmaceutics & pharmacokinetics |
title_sort | applied biopharmaceutics pharmacokinetics |
topic | Pharmakokinetik (DE-588)4115557-9 gnd Biopharmazie (DE-588)4006890-0 gnd |
topic_facet | Pharmakokinetik Biopharmazie |
url | http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=029437475&sequence=000003&line_number=0001&func_code=DB_RECORDS&service_type=MEDIA http://bvbr.bib-bvb.de:8991/F?func=service&doc_library=BVB01&local_base=BVB01&doc_number=029437475&sequence=000004&line_number=0002&func_code=DB_RECORDS&service_type=MEDIA |
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