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
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
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DOI：
10.1021/acs.molpharmaceut.7b00919
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发表时间：
2018-02-01
影响因子：
4.9
通讯作者：
Weitschies, Werner
中科院分区：
文献类型：
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作者：
Grimm, Michael;Koziolek, Mirko;Weitschies, Werner
众所周知，葡萄柚汁（GFJ）会以不同的方式影响药物的生物利用度。尽管对胃肠道酶和转运蛋白有影响，但对胃肠道流体动力学的影响被认为与几种药物的吸收有关。因此，本初步研究的目的是研究摄入GFJ后，与摄入等热量果糖和葡萄糖溶液以及水相比，胃和肠道体积的变化。采用磁共振成像技术对6名健康志愿者在摄入240 mL GFJ、10.6%果糖溶液、10.6%葡萄糖溶液和水后的胃和小肠体积动力学进行了四向交叉研究。采用高效液相色谱法定量测定饮料中碳水化合物的含量。即使在本初步研究的小样本量下，GFJ和葡萄糖溶液的胃排空也明显慢于水。果糖溶液只略微延迟胃排空。与给药纯水相比，给药GFJ和果糖溶液增加了小肠水分含量，而葡萄糖则降低了小肠水分含量。在80分钟，GFJ后的小肠含水量是给水后的小肠含水量的两倍。观察到的GFJ对胃肠道流体动力学的影响可以解释药物药代动力学中的某些现象。这种效果是双刃剑，因为胃排空变慢和肠道充盈增加会导致吸收增强或改变。由于果汁的可比性，果汁对胃肠道容量的一般影响是可能的。
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.