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Technology |
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Radiotracers in Drug Development
Publication Date March 2006
Publisher CRC Press
Product Type Book
Pages 320
ISBN Number 0849333474
Product Code CRC067
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Summary
- Describes the theory and practice behind the detection and measurement of radioactivity using scintillation counting
- Covers the principles of radioactive decay and measuring of radioactivity
- Discusses how to measure low levels of tracers with accelerator mass spectrometry
- Explores how radiotracers are applied to the conduct of drug metabolism studies, both in vitro and in vivo
- Presents examples and illustrations to show how the collected data is used in drug research
- Highlights the radionuclide imaging techniques of gamma-scintigraphy and single-photon emission computed tomography
Although there are numerous books on drug metabolism, Radiotracers in Drug Development is unique in explaining how radiotracers are used to elucidate a drug's absorption, distribution, metabolism, and excretion (ADME). Covering traditional and recent technologies and applications, the book takes a strong industrial approach, discussing the basics of scintillation counting and untangling the various data processing methods often specific to individual manufacturers.
The chapters include descriptions of the latest micro-plate counters and the growing applications of accelerator mass spectrometry, positron emission tomography, gamma-scintigraphy, and radioluminography. In addition to describing how the analytical technologies work, the contributors explain how the data are interpreted and used in the drug registration process.
A unique reference and training aid essential for every drug metabolism department or drug metabolism research team, the book provides insight into the use and practice of ADME in a way that is both instructive and practical. Moving easily across the boundaries of biology, chemistry, and physics, this is the only comprehensive, interdisciplinary resource covering the how-tos of employing radiotracers in drug development. It provides detailed information on how the science is relevant to the registration process.
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Content
- Radiotracers And Drug Registration, Graham Lappin
- The Drug Registration Process
- Drug Metabolism
- Origins Of Radiotracer Studies
- New Chemical Entities And Biopharmaceuticals
- What Are Radiotracers Used For In Drug Registration?
- Detection Of Radioactivity
- The Regulatory Position Of Metabolism Studies
- Acknowledgments
- References.
- Radioactivity And Radiotracers, Graham Lappin
- Atoms And Isotopes
- Isotope Stability
- Types Of Radioactive Decay
- Safety
- Units Of Radioactivity
- Units Of Dose
- Half-Life
- Specific Activity
- Maximum Theoretical Specific Activity
- Universal Quantification
- Calculation Of Limits Of Detection (Lod)
- Synthesis Of Radiolabeled Compounds
- Radiopurity And Autoradiolysis
- Kinetic Isotope Effects
- Further Reading
- Acknowledgments
- References
- The Study Of Drug Metabolism Using Radiotracers, Graham Lappin
- Introduction
- Choice Of Radiolabel
- Test Systems
- In Vitro Studies
- In Vivo Studies: Experimental Aspects
- In Vivo Studies:Data Interpretation
- Structural Alerts
- Appendix 1: An Overview Of Xenobiotic Biotransformations
- Appendix 2:Examples Of Xenobiotic Metabolism Studies From The Literature
- Appendix 3:Pharmacokinetics
- Acknowledgments
- References
- Dna Binding, Isotope Dilution, And Other Uses Of Radiotracers, Graham Lappin
- Introduction
- Dna Binding
- Radioimmunoassay
- Gel Blotting
- Isotope Dilution
- Miscellaneous Uses
- References
- Quantitative Whole-Body Autoradiography (Qwba), Brian Whitby
- Introduction
- Principles And History Of Qwba
- The Modern Technique Of Whole-Body Autoradiography
- Some Specific Uses Of The Qwba Technique
- Microautoradiography5.6 Summary
- Appendix 1: Dosimetry Calculations For The Administration Of Radioisotopes To Humans
- Acknowledgment
- References
- Scintillation Counting, Simon Temple
- Introduction
- How Does Scintillation Counting Work?
- Photomultipliers And Accompanying Circuitry
- Spectrum Analysis And The Introduction Of The Multichannel Analyzer
- Scintillators
- Quench
- Interferences In Scintillation Counting
- Static
- Wall Effect
- Cherenkov Counting
- Dual-Label Counting
- Gamma Counting
- ß--Counting With Solid Scintillators
- Multiwell Plate Scintillation Counting
- Flow Scintillation Counting
- References
- Statistics In Liquid Scintillation Counting, Simon Temple
- Introduction
- Standard Deviation
- Use Of %2ó In Scintillation Counting
- Low Activity Counting
- Limits Of Detection
- References
- Instrumentation For Detection Of Radioactivity, Simon Temple
- Introduction
- History
- Background Reduction
- Quench Correction: General Considerations
- Quench Correction Without An External Standard
- Methods Of Quench Correction Using External Standards
- Solid Vs. Liquid Scintillation Counting
- Microplate Scintillation Counters
- Flow Scintillation Counting
- Stationary Eluate Analysis
- Multicell Eluate Analysis
- Wire Scanners
- Radioluminography
- Appendix 1: List Of Instrument Manufacturers And Suppliers
- References
- Sample Preparation For Liquid Scintillation Counting, Simon Temple
- Introduction
- Solubilization Vs. Oxidation
- General Considerations
- Urine
- Whole Blood And Bile
- Plasma And Serum
- Biological Tissues
- Feces
- Noncommercial Solubilizers
- Acknowledgment
- Biomedical Accelerator Mass Spectrometry, Graham Lappin
- The Beginnings Of Accelerator Mass Spectrometry
- Ams Instrumentation
- Isotopes
- Sample Preparation
- Data Handling
- Sensitivity And Precision Of Ams
- The First Biomedical Ams Studies
- Ams And Drug Development
- Acknowledgments
- References
- Positron Emission Tomography, Barbara S. Koetz And Patricia M. Price
- Introduction
- General Principles Of Pet
- Spatial Resolution And Detectors
- Data Gathering And Interpretation
- Isotope Generation Using A Cyclotron
- Choice Of Radioisotopes
- Labeled Ligand And Drug Synthesis
- Pet Application: Pharmacokinetic Studies
- Pharmacodynamic Studies
- References
- Gamma Scintigraphy And Spect, Stephen P. Newman And Gary R. Pitcairn
- The Development Of Scintigraphic Imaging
- Data Gathering And Interpretation
- Applications To Formulation Design
- References
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