Premium
Impact of Food and Different Meal Types on the Pharmacokinetics of Rilpivirine
Author(s) -
Crauwels Herta M.,
van Heeswijk Rolf P.G.,
Buelens Annemie,
Stevens Marita,
Boven Katia,
Hoetelmans Richard M.W.
Publication year - 2013
Publication title -
the journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.92
H-Index - 116
eISSN - 1552-4604
pISSN - 0091-2700
DOI - 10.1002/jcph.107
Subject(s) - rilpivirine , pharmacokinetics , medicine , pharmacology , human immunodeficiency virus (hiv) , virology , viral load , antiretroviral therapy
The objective of the study was to determine the impact of food and different meal types on the pharmacokinetics of rilpivirine, a nonnucleoside reverse transcriptase inhibitor. In this open‐label, randomized, crossover study, healthy volunteers received a single, oral 75 mg dose of rilpivirine either with a normal‐fat breakfast (reference), under fasting conditions, with a high‐fat breakfast, or with a protein‐rich nutritional drink. Pharmacokinetic parameters were determined by non‐compartmental methods and analyzed using a linear mixed‐effects model. Safety was assessed throughout. The least‐squares mean ratio for area under the plasma concentration–time curve to last timepoint was 0.57 (90% confidence interval [CI]: 0.46–0.72) under fasting conditions compared to dosing with a normal‐fat breakfast. With a high‐fat breakfast or only a protein‐rich nutritional drink, the corresponding values were 0.92 (90% CI: 0.80–1.07) and 0.50 (90% CI: 0.41–0.61), respectively, compared to dosing with a normal‐fat breakfast. Under all conditions, rilpivirine was generally safe and well tolerated. Administration of rilpivirine under fasting conditions or with only a protein‐rich nutritional drink substantially lowered the oral bioavailability when compared to administration with a normal‐fat breakfast. Rilpivirine bioavailability was similar when administered with a high‐fat or normal‐fat breakfast. Rilpivirine should always be taken with a meal to ensure adequate bioavailability.