Table 5.
Pharmacokinetic parameters of various dalbavancin components in plasma following IV administration of 40 mg/kg dalbavancin hydrochloride in rats (mean ± SD, n = 10).
| Stage | Parameters | Components | ||||
|---|---|---|---|---|---|---|
| A0 | A1 | B0 | B1 | B2 | ||
| D1 | AUC(0–t) (μg/mL·h) | 10.5 ± 2.6 | 155.4 ± 79.9 | 5776.5 ± 2593.2 | 688.2 ± 272.2 | 163.7 ± 79.5 |
| AUC(0–∞) (μg/mL·h) | 11.8 ± 2.6 | 173.1 ± 65.6 | 6566.7 ± 1820.3 | 756.2 ± 191.4 | 187.2 ± 61.2 | |
| T1/2 (h) | 6.5 ± 0.6 | 27.5 ± 11.4 | 74.6 ± 45.9 | 29.1 ± 1.1 | 87.3 ± 68.9 | |
| Cmax (μg/mL) | 1.8 ± 0.2 | 14.8 ± 6.1 | 437.3 ± 160.3 | 42.9 ± 18.9 | 23.4 ± 10.4 | |
| MRT(0–t) (h) | 5.6 ± 0.3 | 17.0 ± 3.8 | 23.0 ± 0.9 | 32.3 ± 1.5 | 16.2 ± 2.4 | |
| Vz (L/kg) | 32.9 ± 5.7 | 9.4 ± 3.3 | 0.7 ± 0.5 | 2.3 ± 0.4 | 28.0 ± 23.0 | |
| D28 | AUC(0–t) (μg/mL·h) | 34.0 ± 4.5 *** | 524.7 ± 32.8 *** | 15,781.3 ± 1980.4 *** | 3593.7 ± 6,02.1 *** | 482.4 ± 35.2 *** |
| AUC(0–∞) (μg/mL·h) | 49.5 ± 8.6 *** | 631.0 ± 41.8 *** | 18,543.8 ± 2839.6 *** | 4333.9 ± 848.9 *** | 646.0 ± 53.3 *** | |
| T1/2 (h) | 1,67.1 ± 32.0 *** | 109.5 ± 10.6 *** | 88.8 ± 34.5 | 87.0 ± 27.5 *** | 152.8 ± 43.0 * | |
| C0 (μg/mL) | 0.1 ± 0.0 | 6.3 ± 0.7 | 132.6 ± 15.7 | 37.1 ± 4.1 | 3.9 ± 0.5 | |
| Cmax (μg/mL) | 1.2 ± 0.2 *** | 21.1 ± 1.6 *** | 571.5 ± 67.4 * | 84.3 ± 7.4 *** | 28.0 ± 2.6 | |
| MRT(0–t) (h) | 60.7 ± 2.7 *** | 53.0 ± 5.2 *** | 62.0 ± 3.7 *** | 68.6 ± 8.2 *** | 55.7 ± 4.7 *** | |
| Vz (L/kg) | 196.0 ± 27.3 *** | 10.1 ± 1.3 | 0.3 ± 0.1 * | 1.2 ± 0.4 *** | 13.5 ± 3.4 | |
* p < 0.05, *** p < 0.001, when compared to day 1. Abbreviations: AUC(0–t), the area under the plasma drug concentration-time curve during the time period from 0 to 216 h, the final time point sampled; AUC(0–∞), the area under the plasma drug concentration-time curve during the time period from 0 to infinity; T1/2, the time taken for half the initial drug concentration to be eliminated; Cmax, the maximum drug concentration; MRT(0–t), mean residence time; Vz, apparent volume of distribution; CLz, Plasma clearance; C0, the average value of the plasma concentrations before administration. D1, D28, Days 1, 28 following administration.