Correlation of ibuprofen bioavailability with gastrointestinal transit by scintigraphic monitoring of /sup 171/Er-labeled sustained-release tablets
External gamma scintigraphy was used to monitor the gastrointestinal (GI) transit of radiolabeled sustained-release tablets containing 800 mg ibuprofen in eight fasted healthy volunteers. Ibuprofen serum concentrations were determined from blood samples drawn sequentially over a 24-hr period. Serum concentrations and related parameters were correlated to the position of the dosage form in the GI tract from the scintiphotos. The sustained-release tablets were radiolabeled intact utilizing a neutron activation procedure, by incorporating 0.18% of /sup 170/Er2O3 (enriched to greater than 96% /sup 170/Er) into the bulk formulation. After manufacture of the final dosage forms, the tablets were irradiated in a neutron flux (4.4 x 10(13) n/cm2.sec) for 2 min, converting the stable /sup 170/Er to radioactive /sup 171/Er (t1/2 = 7.5 hr). Each tablet contained 50 microCi of /sup 171/Er at the time of administration. The scintigraphy studies suggested that the greatest proportion of ibuprofen was absorbed from this dosage form while the tablet was in the large bowel. The dosage forms eroded slowly in the small bowel and appeared to lose their integrity in the large bowel. In vitro studies showed only minimal effects of the neutron irradiation procedure on the dosage form performance.
- Research Organization:
- Univ. of Kentucky, Lexington (USA)
- OSTI ID:
- 5942396
- Journal Information:
- Pharm. Res.; (United States), Vol. 4:6
- Country of Publication:
- United States
- Language:
- English
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DRUGS
INTESTINAL ABSORPTION
GASTROINTESTINAL TRACT
SCINTISCANNING
ACTIVATION ANALYSIS
BIOLOGICAL AVAILABILITY
COMPARATIVE EVALUATIONS
ERBIUM 170
ERBIUM 171
ERBIUM 173
MAN
METABOLISM
NEUTRON REACTIONS
ABSORPTION
ANIMALS
BARYON REACTIONS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
CHEMICAL ANALYSIS
COUNTING TECHNIQUES
DIAGNOSTIC TECHNIQUES
DIGESTIVE SYSTEM
ERBIUM ISOTOPES
EVEN-EVEN NUCLEI
EVEN-ODD NUCLEI
HADRON REACTIONS
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
ISOTOPES
MAMMALS
NUCLEAR REACTIONS
NUCLEI
NUCLEON REACTIONS
PRIMATES
RADIOISOTOPE SCANNING
RADIOISOTOPES
RARE EARTH ISOTOPES
RARE EARTH NUCLEI
STABLE ISOTOPES
UPTAKE
VERTEBRATES
550601* - Medicine- Unsealed Radionuclides in Diagnostics