Predicted clinical PK parameters in plasma for midazolam, saquinavir, efavirenz, repaglinide, and desipramine
Single dose given on day 126 in the presence and absence of clofazimine (100 mg once daily, days 1–126).
| Substrate (dose) Simulated n = 100 | Mean (S.D.) | Geometric Mean (CV%) | Geometric Mean Ratio (90% CI) | |||
|---|---|---|---|---|---|---|
| AUCinf | Cmax | AUCinf | Cmax | AUC | Cmax | |
| ng/ml⋅h | ng/ml | ng/ml⋅h | ng/ml | |||
| Midazolam (5 mg) | 72.1 (55.8) | 25.1 (16.9) | 56.0 (77) | 20.4 (68) | ||
| Midazolam (5 mg) + clofazimine | 214 (174) | 42.3 (27.0) | 151 (81) | 34.2 (64) | 2.69 (2.58, 2.80) | 1.68 (1.62, 1.74) |
| Saquinavir (1200 mg) | 2197 (1519) | 388 (309) | 1810 (69) | 304 (80) | ||
| Saquinavir (1200 mg) + clofazimine | 6164 (3730) | 886 (567) | 5224 (60) | 736 (64) | 2.89 (2.87, 2.90) | 2.42 (2.30, 2.53) |
| Efavirenz (600 mg) | 118,424 (78,432) | 2376 (1653) | 97,306 (66) | 1950 (70) | ||
| Efavirenz (600 mg) + clofazimine | 124,951 (86,932) | 2389 (1671) | 101,211 (64) | 1958 (70) | 1.04 (1.04, 1.04) | 1.00 (1.00, 1.00) |
| Repaglinide (0.25 mg) | 8.27 (4.16) | 3.83 (1.36) | 7.14 (50) | 3.56 (36) | ||
| Repaglinide (0.25 mg) + clofazimine | 13.6 (8.75) | 5.04 (1.78) | 11.4 (59) | 4.69 (35) | 1.60 (1.58, 1.76) | 1.32 (1.29, 1.34) |
| Desipramine (50 mg) | 2836 (7808) | 17.3 (11.4) | 688 (275) | 14.5 (66) | ||
| Desipramine (50 mg) + clofazimine | 3125 (7745) | 20.4 (11.6) | 1009 (248) | 17.7 (57) | 1.47 (1.44, 1.50) | 1.27 (1.24, 1.30) |
AUCinf, area under plasma-drug concentration curve from 0 to infinity; CI, confidence interval.