Journal Article

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

Marta Boffito, Desmond Maitland, Laura Dickinson, David Back, Andrew Hill, Carl Fletcher, Graeme Moyle, Mark Nelson, Brian Gazzard and Anton Pozniak

in Journal of Antimicrobial Chemotherapy

Published on behalf of British Society for Antimicrobial Chemotherapy

Volume 55, issue 4, pages 542-545
Published in print April 2005 | ISSN: 0305-7453
Published online April 2005 | e-ISSN: 1460-2091 | DOI: http://dx.doi.org/10.1093/jac/dki043
Boosted saquinavir hard gel formulation exposure in HIV-infected subjects: ritonavir 100 mg once daily versus twice daily

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  • Medical Oncology
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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

Journal Article.  2820 words.  Illustrated.

Subjects: Medical Oncology ; Critical Care

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