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Mol Pharm. 2018 Feb 5;15(2):548-559. doi: 10.1021/acs.molpharmaceut.7b00919. Epub 2018 Jan 18.

Gastric Emptying and Small Bowel Water Content after Administration of Grapefruit Juice Compared to Water and Isocaloric Solutions of Glucose and Fructose: A Four-Way Crossover MRI Pilot Study in Healthy Subjects.

Author information

1
Institute of Pharmacy, Center of Drug Absorption and Transport, University of Greifswald , D-17487 Greifswald, Germany.
2
Physiolution GmbH , 17489 Greifswald, Germany.
3
Institute of Radiology and Neuroradiology, University Medicine Greifswald , 17475 Greifswald, Germany.
4
Department of Radiology, University Medicine Dresden , 17475 Greifswald, Germany.

Abstract

Grapefruit juice (GFJ) is known to affect the bioavailability of drugs in different ways. Despite the influence on gastrointestinal enzymes and transporters, the influence on gastrointestinal fluid kinetics is regarded to be relevant for the absorption of several drugs. Thus, it was the aim of this pilot study to investigate the gastric and intestinal volumes after intake of GFJ compared to isocaloric fructose and glucose solutions and water. The gastric and small intestinal volume kinetics after intake of 240 mL of GFJ, 10.6% fructose solution, 10.6% glucose solution, and water were investigated with magnetic resonance imaging in a four-way crossover study in six healthy human volunteers. The carbohydrate content of the administered beverages was quantified by high-performance liquid chromatography. Even with the small sample size of this pilot study, the gastric emptying of GFJ and the glucose solution was significantly slower than that of water. The fructose solution had only a slightly delayed gastric emptying. Small bowel water content was increased by administration of GFJ and fructose solution, whereas it was decreased by glucose compared to the administration of pure water. At 80 min the small bowel water content after GFJ was twice as high as the small bowel water content after administration of water. The observed influence of GFJ on gastrointestinal fluid kinetics may explain certain phenomena in drugs pharmacokinetics. The effect is double edged, as the slower gastric emptying and increased intestinal filling can lead to enhanced or altered absorption. Due to the comparability of fruit juices, a general effect of fruit juices on gastrointestinal volumes is likely.

KEYWORDS:

clinical pharmacology; gastric emptying; grapefruit juice; malabsorption; radiology/imaging; secretion/absorption; small intestine; stomach and duodenum

[Indexed for MEDLINE]

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