TABLE 3.
Pharmacokinetic parameters for cyclic HPMPC and cidofovir following oral administration of cyclic HPMPC to HIV-infected patientsa
| Cyclic HPMPC dose (mg/kg) | Species | Tmax (h) | Cmax (μg/ml) | t1/2β (h) | AUC0–tlast (μg · h/ml) | AUC0–∞ (μg · h/ml) | % Total oral AUC | % Dose excreted in 24 h | Bioavail-ability (%) |
|---|---|---|---|---|---|---|---|---|---|
| 1.5 | Cyclic HPMPC | 1.3 (1.0)b | 0.036 (0.021) | 2.02 (0.706)c | 0.068 (0.090) | 0.188 (0.099)c | 96.5 (7.86) | 1.1d | 1.76 (1.48) |
| Cidofovir | 12d | 0.008 (0.020) | NDe | 0.004 (0.010) | ND | 2.93 (7.18) | 0.14f | 0.04 (0.10) | |
| 3.0 | Cyclic HPMPC | 2.0 (1.27) | 0.082 (0.038) | 4.36 (2.88) | 0.292 (0.125) | 0.497 (0.166) | 95.2 (11.9) | 1.48 (0.69) | 3.10 (1.16) |
| Cidofovir | 6d | 0.006 (0.014) | ND | 0.043 (0.106) | ND | 9.80 (24.0) | 0.61 (0.38) | 0.75 (1.85) |
t1/2β, elimination half-life. The other abbreviations are defined in the text. Values are means (SDs).
Data for five patients. The concentrations in the remaining patient did not exceed the limit of quantitation (<0.025 μg/ml).
Data for four patients. There were insufficient datum points with quantifiable levels in the remaining patients to calculate a terminal phase.
Data for one patient. The concentrations in the remaining patients did not exceed the limit of quantitation (<0.025 μg/ml in serum or <5 μg/ml in urine).
ND, not determined due to insufficient datum points above the limit of quantitation (<0.025 μg/ml).
Data for two patients. Concentrations in the remaining patients did not exceed the limit of quantitation (<0.025 μg/ml in serum or <0.5 μg/ml in urine).