Radiopharmaceuticals labelled with 18F are the most studied compounds in nuclear medicine, especially for positron emission tomography (PET). Recent studies are engaged in developing new compounds for PET, which should be more specific in certain processes than the widespread 2-deoxy-2-[18F]fluoro-D-glucose ([18F] FDG). Novel radiopharmaceutical compounds trace cell metabolism, such as protein synthesis, amino acid transport, or nucleoside synthesis. Several promising fluorinated compounds are introduced.
18F-Labelled compounds as active substances of radiopharmaceuticals are used for imaging in positron emission tomography (PET) in nuclear medicine. The radiosynthesis of PET radiopharmaceuticals is based on nucleophilic substitution with F- in a precursor. The synthesis is demonstrated on 3?-deoxy-3?-[18F]fluorothymidine.
(166)Ho is a beta-emitter (E(_max) = 1.84 MeV, T1/2 = 26.7 hours) with a mean penetration in the soft tissue of 2.2 mm and gamma-photons 81keV and 1380keV. In this paper, we present our experiences with preparation of (166)Ho-macroaggregates ((166)Ho-MA) for radiosynoviorhesis. Ho-MA were prepared by reacting the aqueous solution of holmium nitrate pentahydrate with sodium borohydride solution in 0.2 M NaOH. After centrifugation, washing, and drying at 105 degrees C, final fineness of 1-15 microm was attained using a homogenizer working at 70,000 rpm. Neutron activation was carried out in screwed titanium ampules in a nuclear reactor at the neutron flux 10E12-10E14 neutrons.cm-24.s-1. The irradiated samples were allowed to cool 24 hours before further manipulation. (166)Ho-MA were clinically tested on 20 patients suffering from gonarthrosis (15), rheumatoid arthritis (5), psoriatic arthritis (1), and gout arthropathy (1). (166)Ho-MA are currently produced under GMP and production facility allows producing radioactivity for 6 patients within one production run.
The aim of this study was to evaluate adverse and therapeutic effects of applicated holmium-boro-macroaggregates (HBMAs) in the radiosynoviorthesis (RSO) of knees in patients suffering from chronic synovitis. We started RSO of the knees by means of a new radiopharmaceutical (RF) HBMA in patients with gonarthrosis, rheumatoid arthritis, chronic synovitis, psoriatic arthritis, and gout arthropathy. Seventeen (17) intra-articular injections were performed in 15 patients who were receiving a mean activity of 972 MBq (range, 904-1057) of 166Ho-HBMA. Patient inclusion to the study followed a series of inclusion and exclusion criterions. The patients were hospitalized for 3 days. Side-effects were evaluated during their hospital stay and again after 6-8 weeks. Static scintigraphy of knee joints and measurements of blood radioactivity were performed. Therapeutic effects were evaluated after 6-8 weeks and at 6 months. In 2 hours and 2 days following the application, we proved, by means of knee and inguinal scintigraphy, only insignificant radiopharmaceutical leakage from the joint cavity to the inguinal lymph nodes in 4 patients. In the treated patients, no serious adverse effects occurred. Nine (9) patients were without complaints, 4 patients had slight knee exudation, and 2 patients had great exudation. Therapeutic effects were as follows: 2 patients were without pain, 9 were with lower pain, 3 were with the same pain, and 1 patient was with increased pain. Joint motion was improved in 7 patients, remained the same in 7 patients, and was impaired in 1 patient. Analgesics consumption was lower in 5 patients, the same in 9 patients, and greater in 1 patient. Knee exudation was absent in 2 patients, lower in 4 patients, the same in 6 patients, and greater in 3 patients. In 3 patients it was necessary to do surgical RSO. This RF can extend the range of clinically used radiopharmaceuticals for RSO and to supplement space between 90Y with high energy and 186Re with 169Er with lower beta energy. The energy of 166Ho is suitable for great and medium joints (i.e., knees, hips, shoulders, elbows, wrists, and ankles).
- MeSH
- časové faktory MeSH
- dospělí MeSH
- holmium škodlivé účinky terapeutické užití MeSH
- koleno patologie účinky záření MeSH
- lidé středního věku MeSH
- lidé MeSH
- mladiství MeSH
- synovitida patologie radioterapie MeSH
- Check Tag
- dospělí MeSH
- lidé středního věku MeSH
- lidé MeSH
- mladiství MeSH
- mužské pohlaví MeSH
- ženské pohlaví MeSH
- Publikační typ
- klinické zkoušky MeSH
Závěrečná zpráva o řešení grantu Interní grantové agentury MZ ČR
50 l. : il., tab., grafy ; 30 cm
Study of the 3´- deoxy-3´-(18F) fluorothymidine (FJFLT) preparation and finding a suitable synthesis precursor including the synthesis parameters optimization. Completion of the study of an irradiation target for sufficient production of fluorine. Development of methods of (18F) FLT quality control, above all of the radiochemical and chemical purity of the synthesized product. Performing the introductory biodistribution study including the distribution visualizing on a PET camera.
Studium přípravy 3´- deoxy ´- (18F) fluorothymidin (18F) FLT a nalezení vhodného prekuzoru pro syntézu ( 18F) FLT). Vývoj metod kontroly kvality (18F)FLT, především kontroly radiochemické čistoty a chemické čistoty syntetizovaného produktu. Provedení úvodní biodistribuční studie včetně zobrazení distribuce na PET kameře.
