Selenium-75-labeled sucralfate: comparison with other radiolabels and initial clinical studies
Sucralfate was synthesized to include a /sup 75/Se label, then compared with /sup 111/In-sucralfate and /sup 99m/Tc-Human serum albumin (HSA)-sucralfate in vitro and in an animal ulcer model. The /sup 75/Se label was the only one of the three that was stable in both human gastric juice and simulated intestinal fluid in vitro. In rats with gastric ulcers, ulcer:nonulcer ratios of bound radioactivity averaged 15.4, 6.3, and 5.6 for /sup 75/Se, /sup 111/In, and /sup 99m/Tc-HSA labels, respectively. Biodistribution studies of /sup 75/Se-sucralfate indicated that little is absorbed from the gastrointestinal tract, and the distribution is similar to that of /sup 14/C-sucralfate. Selective binding of /sup 75/Se sucralfate was successfully imaged in patients with esophagitis (esophageal mean T1/2 binding = 65 +/- 32 min), gastritis (gastric mean T 1/2 binding = 118 +/- 34 min), and gastric ulcers (ulcer mean T 1/2 binding = 135 +/- 59 min). Duodenal ulcers were not successfully imaged. Normal subjects showed no abnormal localization of sucralfate, and esophageal and gastric clearances were rapid.
- Research Organization:
- Temple Univ. Hospital, Philadelphia, PA (USA)
- OSTI ID:
- 6827561
- Journal Information:
- Am. J. Physiol. Imag.; (United States), Journal Name: Am. J. Physiol. Imag.; (United States) Vol. 3:1; ISSN AJPIE
- Country of Publication:
- United States
- Language:
- English
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62 RADIOLOGY AND NUCLEAR MEDICINE
ABSORPTION
ALUMINIUM COMPLEXES
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BIOLOGICAL MODELS
COMPARATIVE EVALUATIONS
COMPLEXES
DAYS LIVING RADIOISOTOPES
DIAGNOSIS
DIGESTIVE SYSTEM DISEASES
DISEASES
DISTRIBUTION
DRUGS
ELECTRON CAPTURE RADIOISOTOPES
EVEN-ODD NUCLEI
HOURS LIVING RADIOISOTOPES
INDIUM 111
INDIUM ISOTOPES
INTERMEDIATE MASS NUCLEI
INTESTINAL ABSORPTION
ISOMERIC NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
LABELLED COMPOUNDS
MAMMALS
MINUTES LIVING RADIOISOTOPES
NUCLEI
ODD-EVEN NUCLEI
PATHOLOGICAL CHANGES
RADIOISOTOPES
RADIOPHARMACEUTICALS
RATS
RODENTS
SELENIUM 75
SELENIUM ISOTOPES
TECHNETIUM 99
TECHNETIUM ISOTOPES
TISSUE DISTRIBUTION
TRACER TECHNIQUES
ULCERS
UPTAKE
VERTEBRATES
YEARS LIVING RADIOISOTOPES