Impact of Splitting or Crushing on the Relative Bioavailability of the Darunavir/Cobicistat/Emtricitabine/Tenofovir Alafenamide Single-Tablet Regimen.
Adenine
/ administration & dosage
Adult
Alanine
Biological Availability
Cobicistat
/ administration & dosage
Cross-Over Studies
Darunavir
/ administration & dosage
Drug Combinations
Emtricitabine
/ administration & dosage
Female
Healthy Volunteers
Humans
Linear Models
Male
Middle Aged
Tablets
Tenofovir
/ analogs & derivatives
Young Adult
bioavailability
crushed tablet
darunavir
human immunodeficiency virus-1
pharmacokinetics
single-tablet regimen
split tablet
tenofovir alafenamide
Journal
Clinical pharmacology in drug development
ISSN: 2160-7648
Titre abrégé: Clin Pharmacol Drug Dev
Pays: United States
ID NLM: 101572899
Informations de publication
Date de publication:
05 2019
05 2019
Historique:
received:
26
04
2018
accepted:
18
10
2018
pubmed:
7
12
2018
medline:
29
7
2020
entrez:
4
12
2018
Statut:
ppublish
Résumé
Darunavir/cobicistat/emtricitabine/tenofovir alafenamide (D/C/F/TAF) is an oral once-daily single-tablet regimen for the treatment of human immunodeficiency virus-1 infection. Different administration modalities for the D/C/F/TAF fixed-dose combination tablet were explored in this phase 1 randomized, open-label, 3-period, 3-treatment crossover study enrolling 30 healthy adults. The primary objective was to assess the relative bioavailability of each component after a single dose of D/C/F/TAF (800/150/200/10 mg) administered as a split or crushed tablet (tests) versus swallowed whole (reference). Pharmacokinetic parameters (noncompartmental analysis; logarithm-transformed) for each component were compared using linear mixed-effects modeling. For the split versus whole tablet, the bioavailabilities (maximum plasma concentration [C
Substances chimiques
Drug Combinations
0
Tablets
0
Tenofovir
99YXE507IL
tenofovir alafenamide
EL9943AG5J
Emtricitabine
G70B4ETF4S
Adenine
JAC85A2161
Cobicistat
LW2E03M5PG
Alanine
OF5P57N2ZX
Darunavir
YO603Y8113
Types de publication
Clinical Trial, Phase I
Journal Article
Randomized Controlled Trial
Research Support, Non-U.S. Gov't
Langues
eng
Sous-ensembles de citation
IM
Pagination
541-548Informations de copyright
© 2018, The American College of Clinical Pharmacology.