Skip Navigation


JAC Advance Access originally published online on February 18, 2005
Journal of Antimicrobial Chemotherapy 2005 55(4):542-545; doi:10.1093/jac/dki043
This Article
Right arrow Full Text Freely available
Right arrow FREE Full Text (PDF) Freely available
Right arrow All Versions of this Article:
55/4/542    most recent
dki043v1
Right arrow Alert me when this article is cited
Right arrow Alert me if a correction is posted
Services
Right arrow Email this article to a friend
Right arrow Similar articles in this journal
Right arrow Similar articles in ISI Web of Science
Right arrow Similar articles in PubMed
Right arrow Alert me to new issues of the journal
Right arrow Add to My Personal Archive
Right arrow Download to citation manager
Right arrow Search for citing articles in:
ISI Web of Science (3)
Right arrowRequest Permissions
Right arrow Disclaimer
Google Scholar
Right arrow Articles by Boffito, M.
Right arrow Articles by Pozniak, A.
Right arrow Search for Related Content
PubMed
Right arrow PubMed Citation
Right arrow Articles by Boffito, M.
Right arrow Articles by Pozniak, A.
Social Bookmarking
Add to CiteULike   Add to Connotea   Add to Del.icio.us  
What's this?

© The Author 2005. Published by Oxford University Press on behalf of the British Society for Antimicrobial Chemotherapy. All rights reserved. For Permissions, please e-mail: journals.permissions{at}oupjournals.org

Boosted saquinavir hard gel formulation exposure in HIV-infected subjects: ritonavir 100 mg once daily versus twice daily

Marta Boffito1,*, Desmond Maitland1, Laura Dickinson2, David Back2, Andrew Hill2,3, Carl Fletcher1, Graeme Moyle1, Mark Nelson1, Brian Gazzard1 and Anton Pozniak1

1 PK Research Ltd, St Stephen's Centre, Chelsea and Westminster Hospital, 369 Fulham Road, London SW10 9NH, UK; 2 University of Liverpool, Liverpool, UK; 3 Roche, Welwyn, UK

* Corresponding author. Tel: +44-20-8846-6507; Fax: +44-20-8746-5628; Email: marta.boffito{at}chelwest.nhs.uk

Objectives: The amount of ritonavir needed to enhance saquinavir hard gel (hg) plasma concentrations is unclear. Reduced ritonavir dosing may help to reduce ritonavir-related side effects and costs. This study examined the pharmacokinetics of twice-daily saquinavir-hg (1000 mg) in the presence of ritonavir 100 mg, dosed twice-daily and once-daily on one single occasion.

Methods: Eighteen HIV-infected adults taking saquinavir/ritonavir 1000/100 mg twice-daily underwent pharmacokinetic (PK) assessment of saquinavir/ritonavir on day 1 following a morning saquinavir/ritonavir dose. On day 2, PK assessment was repeated when subjects took saquinavir without ritonavir. Drug intake (with a standard meal containing 20 g of fat) was timed on days –1, 1 and 2. Geometric mean ratios (GMR) and 95% confidence intervals (CI) were calculated to assess changes in saquinavir PK parameters.

Results: Geometric mean saquinavir AUC0–12, Ctrough, Cmax and elimination half-life on days 1 and 2 were 14 389 and 9590 ng·h/mL, 331 and 234 ng/mL, 2503 and 1893 ng/mL and 2.80 and 2.82 h, respectively. The GMR (95% CI) for these parameters were 0.67 (0.53–0.84), 0.71 (0.48–1.04), 0.76 (0.58–0.98) and 1.01 (0.86–1.18), respectively.

Conclusions: Withholding a ritonavir dose significantly reduces overall saquinavir exposure and Cmax, but had no impact on the elimination half-life. These data establish the need to administer saquinavir and ritonavir simultaneously.

Keywords: saquinavir , ritonavir , pharmacokinetics , boosted protease inhibitors


Add to CiteULike CiteULike   Add to Connotea Connotea   Add to Del.icio.us Del.icio.us    What's this?


This article has been cited by other articles:


Home page
 J Antimicrob ChemotherHome page
L. Dickinson, M. Boffito, S. H. Khoo, M. Schutz, L. J. Aarons, A. L. Pozniak, and D. J. Back
Pharmacokinetic analysis to assess forgiveness of boosted saquinavir regimens for missed or late dosing
J. Antimicrob. Chemother., July 1, 2008; 62(1): 161 - 167.
[Abstract] [Full Text] [PDF]

Home page
 J Antimicrob ChemotherHome page
D. W. Cameron, S. Becker, M. S. King, B. da Silva, C. Klein, D. Tokimoto, C. Foit, D. Calhoun, B. Bernstein, and G. J. Hanna
Exploratory study comparing the metabolic toxicities of a lopinavir/ritonavir plus saquinavir dual protease inhibitor regimen versus a lopinavir/ritonavir plus zidovudine/lamivudine nucleoside regimen
J. Antimicrob. Chemother., May 1, 2007; 59(5): 957 - 963.
[Abstract] [Full Text] [PDF]


Disclaimer:
Please note that abstracts for content published before 1996 were created through digital scanning and may therefore not exactly replicate the text of the original print issues. All efforts have been made to ensure accuracy, but the Publisher will not be held responsible for any remaining inaccuracies. If you require any further clarification, please contact our Customer Services Department.