TABLE 11

Saquinavir bioavailability alone and with ritonavir

Saquinavir Alone Saquinavir + Ritonavir Δ Reference
HIV-infected patientsa Merry et al., 1997
     Cmax (ng/ml) 146 (57-702) 4795 (1420-15810) 33× ↑
     AUC0-8h (ng · h/ml) 470 (293-3446) 27458 (7357-108001) 58× ↑
Healthy volunteersb Hsu et al., 1998
     Cmax (ng/ml) 0.07 ± 0.03 2.2 ± 0.5 31× ↑
     AUC0-40h (μg · h/ml) 0.24 ± 0.18 26.8 ± 4.9 112× ↑
Wild-type micec Huisman et al., 2001
     [14C]saquinavir oral availability (%) 9.1 ± 1.1 232 ± 70 25× ↑
mdr1a/1b knockout micec Huisman et al., 2001
     [14C]saquinavir oral availability (%) 14.1 ± 2.2 865 ± 105 61× ↑

  • ↵ a 600 mg of saquinavir t.i.d. daily alone and with 300 mg ritonavir b.i.d. Data are median (range).

  • ↵ b Single 400 mg of saquinavir alone and with single 600 mg of ritonavir.

  • ↵ c 50 mg/kg ritonavir was administered 30 min before oral administration of [14C]saquinavir.