Next Article in Journal
Study on Ajuga reptans Extract: A Natural Antioxidant in Microencapsulated Powder Form as an Active Ingredient for Nutraceutical or Pharmaceutical Purposes
Next Article in Special Issue
Food Effects on Oral Drug Absorption: Application of Physiologically-Based Pharmacokinetic Modeling as a Predictive Tool
Previous Article in Journal
Nanosystems for the Encapsulation of Natural Products: The Case of Chitosan Biopolymer as a Matrix
Previous Article in Special Issue
Application of the Gastrointestinal Simulator (GIS) Coupled with In Silico Modeling to Measure the Impact of Coca-Cola® on the Luminal and Systemic Behavior of Loratadine (BCS Class 2b)
Article

Exploring the Effect of Esomeprazole on Gastric and Duodenal Fluid Volumes and Absorption of Ritonavir

1
Drug Delivery and Disposition, KU Leuven, Gasthuisberg O&N II, Herestraat 49—Box 921, 3000 Leuven, Belgium
2
Center of Drug Absorption and Transport, Institute of Pharmacy, University of Greifswald, 17489 Greifswald, Germany
3
Radiology Department, University Hospitals Leuven, 3000 Leuven, Belgium
4
Translational Research Center for Gastrointestinal Disorders, TARGID, KU Leuven, 3000 Leuven, Belgium
*
Author to whom correspondence should be addressed.
Pharmaceutics 2020, 12(7), 670; https://doi.org/10.3390/pharmaceutics12070670
Received: 7 June 2020 / Revised: 7 July 2020 / Accepted: 13 July 2020 / Published: 17 July 2020
(This article belongs to the Special Issue Mechanistic In Vitro and In Silico Modeling of Oral Drug Absorption)
Proton-pump inhibitors (PPIs), frequently prescribed to lower gastric acid secretion, often exert an effect on the absorption of co-medicated drug products. A previous study showed decreased plasma levels of the lipophilic drug ritonavir after co-administration with the PPI Nexium (40 mg esomeprazole), even though duodenal concentrations were not affected. The present study explored if a PPI-induced decrease in gastrointestinal (GI) fluid volume might contribute to the reduced absorption of ritonavir. In an exploratory cross-over study, five volunteers were given a Norvir tablet (100 mg ritonavir) orally, once without PPI pre-treatment and once after a three-day pre-treatment with the PPI esomeprazole. Blood samples were collected for eight hours to assess ritonavir absorption and magnetic resonance imaging (MRI) was used to determine the gastric and duodenal fluid volumes during the first three hours after administration of the tablet. The results confirmed that PPI intake reduced ritonavir plasma concentrations by 40%. The gastric residual volume and gastric fluid volume decreased by 41% and 44% respectively, while the duodenal fluid volume was reduced by 33%. These data suggest that the PPI esomeprazole lowers the available fluid volume for dissolution, which may limit the amount of ritonavir that can be absorbed. Although additional factors may play a role, the effect of PPI intake on the GI fluid volume should be considered when simulating the absorption of poorly soluble drugs like ritonavir in real-life conditions. View Full-Text
Keywords: MRI; PPI effect; ritonavir; gastric fluid volume; intestinal fluid volume; drug absorption MRI; PPI effect; ritonavir; gastric fluid volume; intestinal fluid volume; drug absorption
Show Figures

Graphical abstract

MDPI and ACS Style

de Waal, T.; Rubbens, J.; Grimm, M.; Vandecaveye, V.; Tack, J.; Weitschies, W.; Brouwers, J.; Augustijns, P. Exploring the Effect of Esomeprazole on Gastric and Duodenal Fluid Volumes and Absorption of Ritonavir. Pharmaceutics 2020, 12, 670. https://doi.org/10.3390/pharmaceutics12070670

AMA Style

de Waal T, Rubbens J, Grimm M, Vandecaveye V, Tack J, Weitschies W, Brouwers J, Augustijns P. Exploring the Effect of Esomeprazole on Gastric and Duodenal Fluid Volumes and Absorption of Ritonavir. Pharmaceutics. 2020; 12(7):670. https://doi.org/10.3390/pharmaceutics12070670

Chicago/Turabian Style

de Waal, Tom, Jari Rubbens, Michael Grimm, Vincent Vandecaveye, Jan Tack, Werner Weitschies, Joachim Brouwers, and Patrick Augustijns. 2020. "Exploring the Effect of Esomeprazole on Gastric and Duodenal Fluid Volumes and Absorption of Ritonavir" Pharmaceutics 12, no. 7: 670. https://doi.org/10.3390/pharmaceutics12070670

Find Other Styles
Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Article Access Map by Country/Region

1
Back to TopTop