Table 3.
Effect of food on the steady-state pharmacokinetics of nelfinavir/ritonavir given once daily.
| Geometric mean ratio (light/full breakfast) + 90% CI†‡ | |||
|---|---|---|---|
| Parameter* | Group 1: nelfinavir/ritonavir2000/200 mg (n = 8) | Group 2: nelfinavir/ritonavir 2000/400 mg (n = 8) | Group 3: nelfinavir/ritonavir 2500/200 mg (n = 4) |
| Nelfinavir | |||
| AUC24h,corr (h.mg l−1) | 0.75 (0.67–0.84) | 0.75 (0.66–0.85) | 0.53 (0.29–0.98) |
| Cmax (mg l−1) | 0.88 (0.80–0.97) | 0.84 (0.75–0.94) | 0.57 (0.32–1.00) |
| Cmin (mg l−1) | 0.78 (0.65–0.94) | 0.77 (0.61–0.99) | 0.69 (0.53–0.90) |
| tmax (h) | +0.1 (−2.4 to +1.0) | −0.5 (−3.0 to +5.0) | −0.75 (−2.0 to 0.0) |
| M8 | |||
| AUC24h,corr (h.mg l−1) | 0.83 (0.68–1.01) | 0.77 (0.65–0.91) | 0.55 (0.28–1.06) |
| Cmax (mg l−1) | 0.93 (0.90–0.96) | 0.84 (0.71–0.98) | 0.63 (0.40–0.99) |
| Cmin (mg l−1) | 0.83 (0.69–0.99) | 0.82 (0.63–1.07) | 0.62 (0.36–1.05) |
| tmax (h)§ | −1.0 (−1.0 to 0.0) | −1.0 (−2.0 to +5.0) | −0.75 (−2.0 to 0.0) |
| Nelfinavir + M8 | |||
| AUC24h,corr (h.mg l−1) | 0.78 (0.68–0.91) | 0.75 (0.65–0.87) | 0.53 (0.28–1.00) |
| Cmin (mg l−1) | 0.80 (0.67–0.96) | 0.80 (0.62–1.02) | 0.63 (0.43–0.91) |
| Ritonavir | |||
| AUC24h,corr (h.mg l−1) | 0.78 (0.66–0.92) | 0.92 (0.78–1.08) | 0.52 (0.29–0.95) |
| Cmax (mg l−1) | 0.95 (0.78–1.15) | 1.07 (0.89–1.27) | 0.49 (0.24–0.98) |
| Cmin (mg l−1) | 0.90 (0.74–1.09) | 1.03 (0.59–1.80) | 1.17 (0.91–1.50) |
| tmax (h) | +0.5 (−1.0 to +2.0) | +0.5 (−1.0 to +5.1) | −0.5 (−2.0 to 0.0) |
Abbreviations of pharmacokinetic parameters: seeTable 1
CI, Confidence interval. If the CI does not contain one, this implies a significant difference at the 10% significance level between administration of nelfinavir/ritonavir with a light or full breakfast.
A ratio refers to the fraction of a pharmacokinetic parameter after administration of nelfinavir/ritonavir with a light breakfast (day 16) to the same parameter after administration with a full breakfast (day 15). Full breakfast: 610 kcal, 33% fat, 16% proteins, 51% carbohydrates, 130 ml water. Light breakfast: 27 1 kcal, 37% fat, 24% proteins, 39% carbohydrates, 130 ml fluid.
Median difference in tmax after administration of nelfinavir/ritonavir with a light breakfast compared with a full breakfast (tmax day 16 − tmax day 15), and range. No significant differences in tmax values (light breakfast vs full breakfast) were found for nelfinavir, M8, or ritonavir, except for M8 in group 1 (P = 0.03, Wilcoxon signed ranks test).