Chromatography Of Technetium 99m Radiopharmaceuticals

Radioactive drug development is a multi-disciplinary task. Therefore, dedicated scientists and experts from different fields of specialisation have contributed to this book. The text reviews forty years of advances in radiopharmaceutical development based on Technetium. The first section reviews basic principles and analytic methods, and information on chemical makeup of radiopharmaceuticals. Part 2 reviews 99mTc-radiopharmaceuticals used in nuclear medicine, thoroughly outlining their chemistry, formulation, pharmacokinetics and clinical applications.

In 1906, Michael T. Sweet first developed the chromatographic method by using an adsorbant to separate pigments. Since that time, the technological advances in TLC and HPLC have brought about new definitions of purity in parallel with the advances. Radiopharmaceutical chemistry is especially dependent on the chromat ographic technique because of the relatively small amount of material in most radiopharmaceuticals-often so small that the usual physical methods of analytical chemistry cannot be used. As a result, this collection of papers represents the key to successful radiopharmaceutical development by setting the standard for the pres of radiochemical purity. ent-day definition William C. Eckelman, Ph.D. Diagnostics Associate Director The Squibb Institute for Medical Research New Brunswick, New Jersey Preface The chapters herein are updated and expanded versions of presentations that the authors made at a symposium held on June 4, 1984 in Los Angeles, California under the sponsorship of the Radiopharmaceutical Science Council of the Society of Nuclear Medicine. All manuscripts were refereed. The intent of the symposium organizers was to enlist participants who work on a day-to-day basis with the analytical and chromatographic techniques to be discussed at the symposium. We feel confident that this distillation of hands-on experience will be of value to graduate students as well as experienced researchers in radio pharmaceutical chemistry and related fields which use radiotracer methodology.

Advances have led to the production of new radiopharmaceuticals and availability of new production routes. Various new diagnostic agents in the field (such as Ga-68 radiopharmaceuticals and generators) as well as therapeutic agents (such as alpha emitters) have been added to the clinician's menu. It is essential that radiopharmaceuticals are prepared within a robust quality control system encompassing materials and personnel, with adequate documentation, and continuous review of ongoing results. This publication provides guidelines and best practices for the quality control of medical radioisotopes and radiopharmaceuticals. It was written by a group of experts with experience across a range of radiopharmaceuticals and is intended to support professionals in the preparation of good quality and safe products to be used in nuclear medicine procedures.

This book is a comprehensive guide to radiopharmaceutical chemistry. The stunning clinical successes of nuclear imaging and targeted radiotherapy have resulted in rapid growth in the field of radiopharmaceutical chemistry, an essential component of nuclear medicine and radiology. However, at this point, interest in the field outpaces the academic and educational infrastructure needed to train radiopharmaceutical chemists. For example, the vast majority of texts that address radiopharmaceutical chemistry do so only peripherally, focusing instead on nuclear chemistry (i.e. nuclear reactions in reactors), heavy element radiochemistry (i.e. the decomposition of radioactive waste), or solely on the clinical applications of radiopharmaceuticals (e.g. the use of PET tracers in oncology). This text fills that gap by focusing on the chemistry of radiopharmaceuticals, with key coverage of how that knowledge translates to the development of diagnostic and therapeutic radiopharmaceuticals for the clinic. The text is divided into three overarching sections: First Principles, Radiochemistry, and Special Topics. The first is a general overview covering fundamental and broad issues like “The Production of Radionuclides” and “Basics of Radiochemistry”. The second section is the main focus of the book. In this section, each chapter’s author will delve much deeper into the subject matter, covering both well established and state-of-the-art techniques in radiopharmaceutical chemistry. This section will be divided according to radionuclide and will include chapters on radiolabeling methods using all of the common nuclides employed in radiopharmaceuticals, including four chapters on the ubiquitously used fluorine-18 and a “Best of the Rest” chapter to cover emerging radionuclides. Finally, the third section of the book is dedicated to special topics with important information for radiochemists, including “Bioconjugation Methods,” “Click Chemistry in Radiochemistry”, and “Radiochemical Instrumentation.” This is an ideal educational guide for nuclear medicine physicians, radiologists, and radiopharmaceutical chemists, as well as residents and trainees in all of these areas.

Currently an estimated 17 million nuclear medicine procedures are performed each year in the US and constantly evolving, as new radiopharmaceuticals and imaging techniques are introduced for better diagnosis and treatment of human diseases. In keeping up with new developments, the Seventh Edition of Fundamentals of Nuclear Pharmacy chronicles the advancements in radiopharmaceuticals and their use in clinical applications. It discusses basic concepts such as the atom, radioactive decay, instrumentation and production of radionuclides, and explores the design, labeling, characteristics and quality control of radiopharmaceuticals. Radiation regulations and diagnostic and therapeutic applications of radiopharmaceuticals are detailed. Thoroughly updated, the Seventh Edition includes new topics such as alternative productions of 99Mo; production of 64Cu, 86Y, 89Zr, 177Lu, 223Ra; synthesis and clinical uses of new radiopharmaceuticals such as DaTscan, Xofigo, Amyvid, Neuraceq, Vizamyl, Axumin and 68Ga-DOTATATE; dosimetry of new radiopharmaceuticals; theranostic agents and translational medicine. It features numerous examples, diagrams, and images to further clarify the information and offers end- of-chapter questions to help readers assess their comprehension of the material. Recognized as a classic text on nuclear chemistry and pharmacy and acclaimed for its concise and easy-to-understand presentation, Fundamentals of Nuclear Pharmacy is an authoritative resource for nuclear medicine physicians, residents, students, and technologists.

This second edition now includes practical information on drug enhancement of nuclear medicine studies; radiopharmaceuticals as therapeutic agents; pharmacokinetics and a section on current radiopharmaceutical research. This book begins with the basic scientific principles of radiation physics, generator systems and preparation of radiopharmaceuticals. It deals with methods of localization of radiopharmaceuticals such as lung deposition, ion exchange, membrane transportation, phagocytosis and pinocytosis. The important role of radiolabelling blood components is reviewed. The latest information on factors affecting biodistribution, adverse and unusual reactions, the integrity of radiopharmaceuticals and dosimetry is also included. There is also a section on new radiopharmaceuticals. The final chapter on paediatric radiopharmacy deals with the preparation of doses for children, methods of calculating doses and documentation.

The most frequently requested investigation in any nuclear medicine department remains the technetium-99m (99mTc)-labelled diphosphonate bone scan. Despite rapid advances in all imaging modalities. there has been no serious challenge to the role of bone scanning in the evaluation of the skeleton. The main reason for this is the exquisite sensitivity of the bone scan for lesion detection. combined with clear visualisation of the whole skeleton. In recent years several new diphosphonate agents have become available with claims for superior imaging of the skeleton. Essentially. they all have higher affinity for bone. thus allowing the normal skeleton to be visualised all the more clearly. However. as will be dis cussed. this may occur at some cost to the principal role of bone scanning. lesion detection. The major strength of nuclear medicine is its ability to provide functional and physiological information. With bone scanning this leads to high sensitivity for focal disease if there has been any disturbance of skeletal metabolism. However. in many other clinical situations. and particularly in metabolic bone disease. more generalised alteration in skeletal turnover may occur. and quantitation of diphosphonate uptake by the skeleton can provide valuable clinical information.