Table 3. Pharmacokinetic parameters of rifabutin and 25-O desacetyl rifabutin.
Rifabutin | 25-O desacetyl rifabutin | |||||
Alone | with lopinavir/ritonavir | Alone | with lopinavir/ritonavir | |||
300 mg OD | 150 mg OD | 150 mg TPW | 300 mg OD | 150 mg OD | 150 mg TPW | |
Cmax ng/mL | 792 (344 – 1105) | 671 (246 – 1146) | 544 (55 – 964) | 80 (25 - 595) | 216 (94 – 535) | 142 (31 – 308) |
Tmax h | 3 (2 – 4) | 3 (2 – 5) | 3 (0 – 5) | 3 (0 – 5) | 4 (2 – 8) | 4 (2 – 6) |
C0 ng/mL | 74 (13 – 161) | 180 (121 – 310) | 70 (25 – 413) | 10 (0 – 595) | 137 (48 – 334) | 54 (14 – 118) |
Cmin ng/mL n = 25 | 79 (13 – 170) | 169 (71 – 320) | NA | 6 (6 – 329) | 115 (59 – 253) | NA |
Cmin ng/mL n = 15 | 61 (13 – 118) | 161 (71 – 289) | 54 (13 – 414) | 6 (0 – 33) | 114 (73 – 253) | 67 (11 – 214) |
AUCτ ng.h/mL | 5640 (2715–8876) | 7292 (3524–12514) | 7344 (1426–10896) | 697 (245–10250) | 4127 (1769–8616) | 3807 (872–7628) |
Cave ng/mL | 235 (113–370) | 304 (147–521) | 153 (30–227) | 29 (10–427) | 79 (18–159) | 172 (74–359) |
Data are presented as medians with the range in parenthesis
OD – once daily; TPW - three times per week; Cmax -peak concentration; Tmax - time to reach peak concentration; C0 - concentration at time 0; Cmin -concentration at the end of a dosing interval (24 h or 48 h);NA non available, Cmin 48 h post dosing non available in 10 patients; AUCτ – area under the curve during a dosing interval τ, τ is 24 h for OD dosing and 48 h for TPW. Cave – average concentration (AUCτ/τ).