Pharmacokinetics of saquinavir hard gel/ritonavir (1000/100 mg twice daily) when administered with tenofovir diproxil fumarate in HIV‐1‐infected subjects

Article date: January 2005

By: Marta Boffito, David Back, Meredith Stainsby‐Tron, Andrew Hill, Giovanni Di Perri, Graeme Moyle, Mark Nelson, Jaqui Tomkins, Brian Gazzard, Anton Pozniak, in Volume 59, Issue 1, pages 38-42

Aims

To investigate whether the administration of tenofovir diproxil fumarate 300 mg once daily alters the plasma pharmacokinetics of the saquinavir hard gel/ritonavir combination in HIV‐1 infected individuals.

Methods

On day 1, 12 h pharmacokinetic profiles for saquinavir/ritonavir (1000/100 mg given twice daily) were obtained for 18 subjects. All subjects were receiving ongoing treatment with a saquinavir/ritonavir‐containing regimen. Tenofovir diproxil fumarate 300 mg given once daily was then added to the regimen and blood sampling was repeated at days 3 and 14. Saquinavir and ritonavir concentrations were measured by HPLC–MS/MS, and tenofovir concentrations by HPLC with UV detection.

Results

Following the addition of tenofovir diproxil fumarate to the regimen, saquinavir and ritonavir plasma concentrations were not significantly different compared with day 1. Thus the geometric mean ratios (95% confidence intervals) for the area under the concentration‐time curve were 1.16 (0.97, 1.59) and 0.99 (0.87, 1.30) for saquinavir and 1.05 (0.92, 1.28) and 1.08 (0.97, 1.30) for ritonavir, on days 3 and 14, respectively.

Conclusions

Tenofovir diproxil fumarate did not alter the pharmacokinetics of saquinavir hard gel/ritonavir.

DOI: 10.1111/j.1365-2125.2004.02240.x

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