Intragastric Behavior and Absorption Kinetics of a Normal and “Floating” Modified-Release Capsule of Isradipine under Fasted and Fed Conditions

From measurements of drug levels in both gastric juice and plasma, we investigated whether or not a prolonged gastric residence time (GRT) is responsible for the slow absorption kinetics of a “floating” modified‐release (MR) capsule of isradipine [isopropyl methyl (±)4-(4-benzofurazanyl)-1,4-dihydro...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1988-08, Vol.77 (8), p.647-657
Main Authors: Mazer, Norman, Abisch, Eva, Gfeller, Jean-Claude, Laplanche, Robert, Bauerfeind, Peter, Cucala, Mercedes, Lukachich, Marianne, Blum, André
Format: Article
Language:English
Subjects:
Adult
Antihypertensive agents
Biological and medical sciences
Calcium Channel Blockers - administration & dosage
Calcium Channel Blockers - pharmacokinetics
Capsules
Cardiovascular system
Delayed-Action Preparations
Fasting
Female
Food
Gastric Juice - metabolism
Gastric Mucosa - metabolism
Humans
Intestinal Absorption
Isradipine
Male
Medical sciences
Models, Biological
Pharmacology. Drug treatments
Pyridines - administration & dosage
Pyridines - pharmacokinetics
Solubility
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Summary:From measurements of drug levels in both gastric juice and plasma, we investigated whether or not a prolonged gastric residence time (GRT) is responsible for the slow absorption kinetics of a “floating” modified‐release (MR) capsule of isradipine [isopropyl methyl (±)4-(4-benzofurazanyl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinedicarboxylate], a lipophilic dihydropyridine calcium channel blocker. The effects of a “high‐fat” breakfast on the intragastric behavior and absorption kinetics were also assessed. In an open crossover design, five healthy subjects ingested either a normal or MR capsule of isradipine under fasted conditions. Serial samples of gastric juice (obtained via an indwelling nasogastric tube) and plasma were collected up to 24h after drug intake, and were analyzed for isradipine by GC and RIA methods, respectively. The pH and titratable acid, protein, and pepsin concentrations of the gastric juice samples were also determined. Four additional subjects were similarly studied after ingesting the capsules following a high‐fat breakfast. Under fasted conditions, gastric juice drug levels of the normal and MR capsules indicated a median GRT of
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600770802