The effect of food on gastrointestinal (GI) transit of sustained-release ibuprofen tablets as evaluated by gamma scintigraphy

Journal Article · Thu Mar 01 00:00:00 EST 1990 · Pharmaceutical Research; (USA)

DOI:https://doi.org/10.1023/A:1015842600189· OSTI ID:6746788

Borin, M T; Khare, S; Beihn, R M; Jay, M ^[1]

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1. Upjohn Company, Kalamazoo, MI (USA)

The GI transit of radiolabeled sustained-release ibuprofen 800-mg tablets in eight healthy, fed volunteers was monitored using external gamma scintigraphy. Ibuprofen serum concentrations were determined from blood samples drawn over 36 hr following dosing. Sustained-release ibuprofen tablets containing 0.18% of 170Er2O3 (greater than 96% 170Er) in the bulk formulation were manufactured under pilot-scale conditions and were radiolabeled utilizing a neutron activation procedure which converted stable 170Er to radioactive 171Er (t1/2 = 7.5 hr). At the time of dosing, each tablet contained 50 mu Ci of 171Er. Dosage form position were reported at various time intervals. In five subjects the sustained-release tablet remained in the stomach and eroded slowly over 7-12 hr, resulting in gradual increases in small bowel radioactivity. In the remaining three subjects, the intact tablet was ejected from the stomach and a gastric residence time of approximately 4 hr was measured. This is in marked contrast to a previous study conducted in fasted volunteers in which gastric retention time ranged from 10 to 60 min. Differences in GI transit between fed and fasted volunteers had little effect on ibuprofen bioavailability. AUC and Tmax were unaltered and Cmax was increased by 24%, which is in agreement with results from a previous, crossover-design food effect study.

• OSTI ID: 6746788
• Journal Information: Pharmaceutical Research; (USA), Vol. 7:3; ISSN 0724-8741
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
DRUGS
METABOLISM
FOOD
BIOLOGICAL EFFECTS
ACTIVATION ANALYSIS
BIOLOGICAL AVAILABILITY
ERBIUM 170
ERBIUM 171
GAMMA RADIATION
GASTROINTESTINAL TRACT
MAN
NEUTRON REACTIONS
STOMACH
ANIMALS
BARYON REACTIONS
BETA DECAY RADIOISOTOPES
BETA-MINUS DECAY RADIOISOTOPES
BODY
CHEMICAL ANALYSIS
DIGESTIVE SYSTEM
ELECTROMAGNETIC RADIATION
ERBIUM ISOTOPES
EVEN-EVEN NUCLEI
EVEN-ODD NUCLEI
HADRON REACTIONS
HOURS LIVING RADIOISOTOPES
INTERMEDIATE MASS NUCLEI
IONIZING RADIATIONS
ISOTOPES
MAMMALS
NUCLEAR REACTIONS
NUCLEI
NUCLEON REACTIONS
ORGANS
PRIMATES
RADIATIONS
RADIOISOTOPES
RARE EARTH ISOTOPES
RARE EARTH NUCLEI
STABLE ISOTOPES
VERTEBRATES
550501* - Metabolism- Tracer Techniques