Abstract
Aims. To investigate the pharmacokinetic profile of the protease inhibitor saquinavir (SQV) after multiple doses in HIV-positive patients and to evaluate the possibility of predicting total body exposure of SQV from concentrations determined at single time points. Methods. Twenty HIV-positive patients on steady-state treatment with SQV (Hard-Gel-Capsule, Invirase®) enrolled in this study. Serial blood samples were obtained during a dosing interval. SQV plasma concentrations were determined by high performance liquid chromatography (h.p.l.c.) and pharmacokinetic parameters were determined by noncompartmental techniques. Results. There was a marked interindividual variability in SQV pharmacokinetic parameters with a 11-fold variability in total systemic exposure to SQV, as expressed by AUC(0,8h) values (range: 268-3009 ng ml-1 h, CV: 69%). The oral clearance shows an interindividual CV of 75%. A strong correlation (r = 0.94) was found between SQV plasma concentration at 3 h (C(3 h)) and AUC(0,8h). Conlusions. This study shows that C(3 h) is a good predictor for total body exposure of SQV and might be useful to predict SQV disposition in HIV-positive patients on steady-state treatment.
| Original language | English |
|---|---|
| Pages (from-to) | 379-382 |
| Number of pages | 4 |
| Journal | British Journal of Clinical Pharmacology |
| Volume | 47 |
| Issue number | 4 |
| DOIs | |
| Publication status | Published - 1999 |
Fingerprint
Keywords
- HIV infection
- Pharmacokinetics
- Saquinavir
ASJC Scopus subject areas
- Pharmacology (medical)
- Pharmacology, Toxicology and Pharmaceutics(all)
Cite this
Pharmacokinetic variability and strategy for therapeutic drug monitoring of saquinavir (SQV) in HIV-1 infected individuals. / Regazzi, Mario B.; Villani, Paola; Maserati, Renato; Cocchi, Laura; Giacchino, Roberto; Burroni, Daniela; Rettani, Mauro.
In: British Journal of Clinical Pharmacology, Vol. 47, No. 4, 1999, p. 379-382.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Pharmacokinetic variability and strategy for therapeutic drug monitoring of saquinavir (SQV) in HIV-1 infected individuals
AU - Regazzi, Mario B.
AU - Villani, Paola
AU - Maserati, Renato
AU - Cocchi, Laura
AU - Giacchino, Roberto
AU - Burroni, Daniela
AU - Rettani, Mauro
PY - 1999
Y1 - 1999
N2 - Aims. To investigate the pharmacokinetic profile of the protease inhibitor saquinavir (SQV) after multiple doses in HIV-positive patients and to evaluate the possibility of predicting total body exposure of SQV from concentrations determined at single time points. Methods. Twenty HIV-positive patients on steady-state treatment with SQV (Hard-Gel-Capsule, Invirase®) enrolled in this study. Serial blood samples were obtained during a dosing interval. SQV plasma concentrations were determined by high performance liquid chromatography (h.p.l.c.) and pharmacokinetic parameters were determined by noncompartmental techniques. Results. There was a marked interindividual variability in SQV pharmacokinetic parameters with a 11-fold variability in total systemic exposure to SQV, as expressed by AUC(0,8h) values (range: 268-3009 ng ml-1 h, CV: 69%). The oral clearance shows an interindividual CV of 75%. A strong correlation (r = 0.94) was found between SQV plasma concentration at 3 h (C(3 h)) and AUC(0,8h). Conlusions. This study shows that C(3 h) is a good predictor for total body exposure of SQV and might be useful to predict SQV disposition in HIV-positive patients on steady-state treatment.
AB - Aims. To investigate the pharmacokinetic profile of the protease inhibitor saquinavir (SQV) after multiple doses in HIV-positive patients and to evaluate the possibility of predicting total body exposure of SQV from concentrations determined at single time points. Methods. Twenty HIV-positive patients on steady-state treatment with SQV (Hard-Gel-Capsule, Invirase®) enrolled in this study. Serial blood samples were obtained during a dosing interval. SQV plasma concentrations were determined by high performance liquid chromatography (h.p.l.c.) and pharmacokinetic parameters were determined by noncompartmental techniques. Results. There was a marked interindividual variability in SQV pharmacokinetic parameters with a 11-fold variability in total systemic exposure to SQV, as expressed by AUC(0,8h) values (range: 268-3009 ng ml-1 h, CV: 69%). The oral clearance shows an interindividual CV of 75%. A strong correlation (r = 0.94) was found between SQV plasma concentration at 3 h (C(3 h)) and AUC(0,8h). Conlusions. This study shows that C(3 h) is a good predictor for total body exposure of SQV and might be useful to predict SQV disposition in HIV-positive patients on steady-state treatment.
KW - HIV infection
KW - Pharmacokinetics
KW - Saquinavir
UR - http://www.scopus.com/inward/record.url?scp=0032928435&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0032928435&partnerID=8YFLogxK
U2 - 10.1046/j.1365-2125.1999.00919.x
DO - 10.1046/j.1365-2125.1999.00919.x
M3 - Article
VL - 47
SP - 379
EP - 382
JO - British Journal of Clinical Pharmacology
JF - British Journal of Clinical Pharmacology
SN - 0306-5251
IS - 4
ER -