Table 1.
Pharmacokinetic parameters for rifabutin and 25-O- desacetylrifabutin for each study treatment
| Treatment period | Rifabutin 300 mg | Rifabutin 150 mg tiw plus LPV/r | Rifabutin 150 mg daily plus LPV/r |
|---|---|---|---|
| Rifabutin (n = 14) | |||
| AUC0–24 (ng.h/mL) | 3052.9 (2650.2-3431.5) | 2307.5 (1767.5-3884.0) | 4766.0 (3950.5-6099.5) |
| AUC0–48 (ng.h/mL) | 6105.8 (5300.4-6863.0)* | 3402.1 (2809.2-6092.0) | 9532.0 (2238.2-22425.4)* |
| Cmax (ng/mL) | 291.5 (250.0-377.0) | 167.5 (87.8-294.0) | 311.0 (258.0-376.0) |
| Tmax (h) | 3.0 (3.0-4.0) | 3.5 (3.0-5.0) | 3.0 (3.0-4.0) |
| C0 (ng/mL) | 59.0 (36.4-78.6) | 49.1 (27.7-58.9) | 176.5 (149.0-195.0) |
| Cmin 24 h (ng/mL) | 60.7 (40.6-68.8) | 70.7 (45.7-96.6) | 133.0 (105.0-191.0) |
| Cmin 48 h (ng/mL) | - | 37.0 (26.6-70.0) | - |
| CL/F (L/h) | 98.3 (87.4-113.2) | 65.2 (38.6-85.0) | 31.5 (25.0-38.0) |
| AUC0–24 (ng.h/mL) (Rifabutin + Metabolite) | 3402.3 (2900.3-3717.2) | 3937.2 (2424.6-6772.7) | 8753.0 (7771.7-11 505.0) |
| d-RBT (n = 14) | |||
| AUC0–24 (ng.h/mL) | 273.3 (235.7-344.1) | 1565.5 (1105.5-2567.3) | 4118.0 (2678.2-5405.5) |
| AUC0–48 (ng.h/mL) | 546.6 (471.4-688.2)* | 2318.2 (1722.9-4685.9) | 8236.0 (5356.4-10811.0)* |
| Cmax (ng/mL) | 32.5 (25.2-37.7) | 77.2 (58.6-128) | 236.5 (159.0-274.0) |
| Tmax (h) | 3.0 (3.0-4.0) | 5.0 (4.0-6.0) | 4.0 (3.0-3.0) |
| C0 (ng/mL) | 5.1 (2.7-6.6) | 44.6 (31.7-68.9) | 186.0 (115.0-232.0) |
| Cmin 24 h (ng/mL) | 5.0 (3.4 -5.8 | 63.9 (42.7-101.0) | 155.0 (53.6-206.0) |
| Cmin 48 h (ng/mL) | - | 35.4 (27.7-81.0) | - |
Parameters are median values (interquartile range).
*calculated by 2X AUC0–24.
RBT = rifabutin.
d-RBT =25-O-desacetylrifabutin.
LPV/r = lopinavir/ritonavir based ART.
tiw = three times per week.
AUC = area under the curve.
Cmax = maximum concentration in plasma.
Tmax = time at which maximum plasma attained.
CL/F = clearance.
C0 = pre-dose concentration.
Cmin = trough concentration.