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العنوان
Radiolabeling, Chemical and Biological Evaluation of Some Drugs for Nuclear Medicine Applications /
المؤلف
Hafez, Fatma Elzahraa Ahmed Mohamed.
هيئة الاعداد
باحث / فاطمة الزهراء احمد محمد حافظ
مشرف / صلاح عبد الغنى ابو العينين
مشرف / فؤاد ابراهيم الحسينى
مشرف / جهاد جنيدى محمد
مشرف / عبير محمد أمين
مشرف / حنان عبد العزيزعبد الرازق الصباغ
تاريخ النشر
2022.
عدد الصفحات
107 p. :
اللغة
الإنجليزية
الدرجة
الدكتوراه
التخصص
Physical and Theoretical Chemistry
تاريخ الإجازة
1/1/2022
مكان الإجازة
جامعة عين شمس - كلية العلوم - الكيمياء
الفهرس
Only 14 pages are availabe for public view

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Abstract

In recent years, the development of new heart radiopharmaceuticals for SPECT imaging has progressed rapidly. SPECT alone or in combination with PET and / or functional magnetic resonance imaging (fMRI) can be alludes to non-surgical intervention imaging of the heart, including myocardial perfusion imaging. These cardiovascular methods are generally alluded to as echocardiography, SPECT has the advantage of being widely used around the world. SPECT was originally developed for clinical use, and subsequent preclinical adaptations of the imaging modality have enabled longitudinal molecular imaging in small laboratory animals. Suitable radiopharmaceuticals used for heart imaging, it should have a short half-life time and suitable photon energy within the range of the used gamma camera.
The purpose of this work is to develop potentially selective radiopharmaceuticals for non-invasive heart imaging. Lido, Vera, and Epin (three drugs that can target to heart) have been successfully radiolabeled and their biodistribution in mice has been studied and confirmed by imaging. This study was divided into three main chapters:
Chapter (I): Introduction and Object of Investigation
These include radiopharmaceuticals and their types, radionuclides and their decay processes, radiopharmaceuticals and their types, ideal radiopharmaceutical properties, radiopharmaceutical quality control, iodine chemistry and radiochemistry, radiowaste and its treatment, Heart imaging in nuclear medicine, human heart medicine, nuclear medicine and the radiopharmaceuticals used in it, Lido, Vera, Epin and literature reviews.
Chapter (II): Materials and Methods of Investigation
This chapter includes:
 Detailed information on the materials, equipment, animals, and buffers used in this study.
 Electrophile radioiodination procedure of Lido, Vera, Epin and method of determining radiochemical yield.
 Procedures for obtaining optimal conditions for radioactive labeling of pharmaceutical products.
 A method for determining the radiochemical purity.
 In vivo distribution studies in mice.
Chapter (III): Results and Discussion
This chapter describes the radiolabeling process of Lido, Vera, Epin with iodine-125 by electrophilic substitution and the selection of the optimum conditions required to obtain the maximum radiochemical yields of 125I-Lido, 125I-Vera, 125I-Epin. Radiolabeled drugs have been biologically examined in normal mice to elucidate the ability of the tracer to accumulate in the heart as fast as the tracer injected. These results show that:
 125I-Lido was obtained using 150 µg CAT as the oxidizing agent and150 µg Lido and 125 iodine on a neutral medium pH = 7. The reaction mixture was heated up to 60°C temperature for 30minutes. The radiochemical yield obtained was 93.2 % ± 0.1.
 Radiolabeling of Vera was performed by adding 150 µg of Vera as an oxidizing agent to 150 µg of CAT, followed by the addition of pH 7 radioactive iodine. The reaction mixture was heated at 60 ° C for 30 minutes. The radiochemical yield reached 95.4 % ± 0.4.
 100 µg Epin succeeded in successfully labeled with iodine-125 with a maximum radioactivity yield of (96% ± 0.8) by direct labeling technology using 150 µg CAT in neutral medium (pH = 7) at room temperature (25 ± 3oC) for 30 minutes.
 The stability of 125I-Lido, 125I-Vera, and 125I-Epin was investigated and the results were up to 2, 4, and 8 hours, respectively, with no by-products detected in the reaction mixture.
 The biodistribution profile of normal Swiss albino mice by the intravenous drugs route was examined at various time intervals, and the maximum uptake of radioidonated Lido and Vera by the mouse heart was 19.8 % after 60 minutes of injection, 18.3% respectively. The maximum uptake of radioidonated Epin was 18.6% 180 minutes after injection.