Comparison of labels for Carafate in a gastric ulcer model
The purpose of this study was to evaluate three radiolabels for the drug Carafate (basic aluminum sucrose octasulfate), which, when ingested orally, is believed to coat gastric ulcers and protect them from digestive enzymes to promote healing. In order to study the mode of action and residence time in the stomach using external imaging, a gamma-emitting label which is truly bound to the molecule is needed. Carafate has been radiolabeled with Se-75, In-111 (both chemically incorporated into the molecule) and with Tc-99m-HSA which physically adheres to Carafate. In the presence of stomach acid, Carafate polymerizes; when the labeled Carafates were mixed in vitro with 0.1N HCl, >90% of the radio-activity was associated with the polymer in the case of Se-75 and Tc-99m, but the In-111 label was less stable (25-35% bound to polymer). The three labeled preparations were administered orally to rats with gastric ulcers, and the transit of each was followed by gamma camera imaging. Gamma camera images confirmed radioactivity remaining at the ulcer site after unbound material had emptied from the stomach, and the focal activity persisted for >5 hours. The stomachs were then removed, washed and dissected at 5.5 hours and in vitro measurements of ulcer crater: normal stomach tissue radioactivity ratios averaged 15.4, 6.3, and 5.6 for the Se-75, In-111, and Tc-99m-HSA labels, respectively. Biodistribution studies of oral Se-75-Carafate in rats and pigs indicated that very little is absorbed from the GI tract and the distribution is similar to that of C-14-Carafate. It is concluded that Se-75 is the best marker for Carafate of these three gamma-emitting labels and Se-75-Carafate is suitable for studying the kinetics of the drug Carafate in human subjects.
- Research Organization:
- Temple Univ. School of Medicine and Hospital, Philadelphia, PA
- OSTI ID:
- 6842506
- Report Number(s):
- CONF-840619-; TRN: 87-008943
- Journal Information:
- J. Nucl. Med.; (United States), Vol. 25:5; Conference: 31. annual meeting of the Society of Nuclear Medicine, Los Angeles, CA, USA, 5 Jun 1984
- Country of Publication:
- United States
- Language:
- English
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Related Subjects
ALUMINIUM SULFATES
THERAPEUTIC USES
INDIUM 111
SACCHAROSE
SELENIUM 75
STOMACH
RADIOISOTOPE SCANNING
TECHNETIUM 99
ULCERS
RADIOTHERAPY
DRUGS
ENZYMES
HUMAN POPULATIONS
IMAGE PROCESSING
IN VITRO
MIXING
ORAL ADMINISTRATION
POLYMERIZATION
RATS
TIME DEPENDENCE
TRACER TECHNIQUES
ALUMINIUM COMPOUNDS
ANIMALS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BODY
CARBOHYDRATES
CHEMICAL REACTIONS
COUNTING TECHNIQUES
DAYS LIVING RADIOISOTOPES
DIGESTIVE SYSTEM
DISACCHARIDES
ELECTRON CAPTURE RADIOISOTOPES
EVEN-ODD NUCLEI
GASTROINTESTINAL TRACT
HOURS LIVING RADIOISOTOPES
INDIUM ISOTOPES
INTERMEDIATE MASS NUCLEI
ISOMERIC TRANSITION ISOTOPES
ISOTOPE APPLICATIONS
ISOTOPES
MAMMALS
MEDICINE
MINUTES LIVING RADIOISOTOPES
NUCLEAR MEDICINE
NUCLEI
ODD-EVEN NUCLEI
OLIGOSACCHARIDES
ORGANIC COMPOUNDS
ORGANS
OXYGEN COMPOUNDS
PATHOLOGICAL CHANGES
POPULATIONS
PROCESSING
RADIOISOTOPES
RADIOLOGY
RODENTS
SACCHARIDES
SELENIUM ISOTOPES
SULFATES
SULFUR COMPOUNDS
TECHNETIUM ISOTOPES
THERAPY
USES
VERTEBRATES
YEARS LIVING RADIOISOTOPES
550604* - Medicine- Unsealed Radionuclides in Therapy- (1980-)