Absorption, gastrointestinal transit, and tablet erosion of felodipine extended-release (ER) tablets.
The gastrointestinal transit and tablet erosion of felodipine extended release (ER) tablets 10 mg were studied by gamma scintigraphy in eight healthy young males after administration under fasting and nonfasting conditions. Plasma concentrations of felodipine were also measured. Gastric emptying after administration together with food (mean, 3.2 hr) was slower in all subjects compared to emptying under fasting conditions (mean, 0.6 hr). The mean small intestinal transit times for the two study conditions did not differ significantly (5.1 and 4.7 hr, respectively). Tablets did not leave the colon in any subject within 14 hr after administration. Felodipine was shown to be absorbed in the colon, although the major part of the dose was absorbed in the small intestine. The absorption rate of felodipine was related to erosion of the hydrophilic matrix tablet. Tablet erosion and hence drug absorption were slower in the more distal parts of the gastrointestinal tract. Administration together with food did not significantly affect tablet erosion.
Abrahamsson
B
B
Pharmaceutical R&D, Astra Hässle AB, Mölndal, Sweden.
Alpsten
M
M
Hugosson
M
M
Jonsson
U E
UE
Sundgren
M
M
Svenheden
A
A
Tölli
J
J
D000328:Adult; D003692:Delayed-Action Preparations; D005215:Fasting; D015736:Felodipine / Q000097:blood / Q000493:pharmacokinetics*; D005746:Gastric Emptying; D005772:Gastrointestinal Transit; D006801:Humans; D007408:Intestinal Absorption; D008297:Male; D012995:Solubility; D013607:Tablets
D003692:Delayed-Action Preparations; D013607:Tablets; D015736:Felodipine