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

• Published in: Molecular pharmaceutics Vol. 15; no. 2; pp. 548 - 559
• Main Authors: Grimm, Michael, Koziolek, Mirko, Saleh, Marwa, Schneider, Felix, Garbacz, Grzegorz, Kühn, Jens-Peter, Weitschies, Werner
• Format: Journal Article
• Language: English
• Published: United States American Chemical Society 05.02.2018
• Subjects: Adult; Biological Availability; Citrus paradisi; Cross-Over Studies; Female; Food-Drug Interactions; Fructose - administration & dosage; Fruit and Vegetable Juices; Gastric Emptying; Glucose - administration & dosage; Healthy Volunteers; Humans; Intestinal Secretions - chemistry; Intestine, Small; Magnetic Resonance Imaging; Male; Pilot Projects; Stomach - diagnostic imaging; Water; Young Adult; grapefruit juice; secretion/absorption; stomach and duodenum; malabsorption; clinical pharmacology; small intestine; gastric emptying; radiology/imaging
• ISSN: 1543-8384; 1543-8392; 1543-8392
• DOI: 10.1021/acs.molpharmaceut.7b00919

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.