Measured | Vss | AUC | Cmax | t1/2 | CL | Tmax |
---|---|---|---|---|---|---|
ml/kg | μM · min | μM | min | ml/min/kg | min | |
Following i.v. injection of HI-113 | ||||||
Total HI-113 | 920.0 ± 127.4 | 1071.8 ± 81.8 | 211.6 ± 29.3 | 3.6 ± 0.3 | 174.5 ± 13.2 | N.D. |
HI-113-A | 1005.3 ± 134.0 | 396.2 ± 48.7 | 106.3 ± 14.3 | 2.6 ± 0.1 | 266.5 ± 30.2 | N.D. |
HI-113-B | 791.8 ± 113.1 | 657.7 ± 41.3 | 110.7 ± 15.1 | 4.3 ± 0.4 | 127.3 ± 8.2 | N.D. |
ala-d4T-MP | N.D. | 2795.9 ± 361.2 | 69.3 ± 4.1 | 138.8 ± 40.2 | N.D. | 5.1 ± 0.7 |
d4T | N.D. | 2858.1 ± 182.2 | 15.6 ± 1.2 | 116.2 ± 11.9 | N.D. | 17.4 ± 2.6 |
Following i.v. injection of ala-d4T-MP | ||||||
ala-d4T-MP | 412.6 ± 126.3 | 11761.5 ± 447.2 | 1658.1 ± 544.9 | 38.9 ± 15.9 | 15.7 ± 0.6 | N.D. |
d4T | N.D. | 1818.2 ± 42.9 | 35.9 ± 3.7 | 32.4 ± 2.2 | N.D. | 5.0 ± 1.2 |
Following i.v. injection of d4T | ||||||
d4T | 581.8 ± 62.8 | 12173.6 ± 559.5 | 318.9 ± 15.7 | 26.6 ± 1.2 | 15.2 ± 0.7 | N.D. |
Pharmacokinetic parameters in BALB/c mice (n = 4–5 mice per time point) are presented as the mean ± S.E. A correction factor of 1.24 was used when determining the concentrations of HI-113A and HI-113B because of their different extinction coefficients (10,802 for HI-113B versus 8,686 for HI-113A, ratio = 1.24:1).
N.D., not determined.