Gastrointestinal transit of a controlled release naproxen tablet formulation

doi:10.1016/0378-5173(86)90102-X

International Journal of Pharmaceutics

Volume 32, Issue 1, September 1986, Pages 85-90

https://doi.org/10.1016/0378-5173(86)90102-X Get rights and content

Abstract

The gastrointestinal transit of a controlled release naproxen tablet formulation has been measured in healthy young and old subjects using the technique of gamma scintigraphy. Gastric emptying of the tablet was affected by food (mean emptying times for fasted subjects were 0.64 h (young) and 0.86 h (old) increased to 3.0 h (young) and 3.3 h (old) following a light breakfast). The small intestinal transit times for both fed and fasted states was about 3.2 h. There were no significant differences that could be attributed to subject age for gastric emptying and small intestinal transit.

References (18)

S.S. Davis et al.
A comparative study of the gastrointestinal transit of a pellet and tablet formulation
Int. J. Pharm.
(1984)
S.S. Davis et al.
The effect of food on the gastrointestinal transit of pellets and an osmotic device (Osmet)
Int. J. Pharm.
(1984)
M. Feldman et al.
Gastric emptying of solid radiopaque markers: studies in healthy subjects and diabetic patients
Gastroenterology
(1984)
J.-R. Malagelada et al.
Intestinal transit of solid and liquid components of a meal in health
Gastroenterology
(1984)
H. Minami et al.
The physiology and pathophysiology of gastric emptying in humans
Gastroenterology
(1984)
F.N. Christensen et al.
The use of gamma scintigraphy to follow the gastrointestinal transit of pharmaceutical formulations
J. Pharm. Pharmacol.
(1985)
C.F. Code et al.
The interdigestive myo-electric complex of the stomach and small bowel of dogs
J. Physiol. (London)
(1975)
S.S. Davis et al.
Transit of pharmaceutical dosage forms through the small intestine
(1986)
M.A. Evans et al.
Gastric emptying rate in the elderly: implications for drug therapy
J. Am. Geriatr. Soc.
(1981)

There are more references available in the full text version of this article.

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Research paperGastrointestinal transit of a controlled release naproxen tablet formulation

Abstract

Int. J. Pharm.

Int. J. Pharm.

Gastroenterology

Gastroenterology

Gastroenterology

The use of gamma scintigraphy to follow the gastrointestinal transit of pharmaceutical formulations

J. Pharm. Pharmacol.

The interdigestive myo-electric complex of the stomach and small bowel of dogs

J. Physiol. (London)

Transit of pharmaceutical dosage forms through the small intestine

Gastric emptying rate in the elderly: implications for drug therapy

J. Am. Geriatr. Soc.

Research paper
Gastrointestinal transit of a controlled release naproxen tablet formulation