TABLE 2.
Rat brain distribution of metformin treated with metformin threonate (SHY-01) or metformin hydrochloride (50 mg/kg, i.p.).
| Parameters | Unit | SHY-01 | Metformin hydrochloride |
|---|---|---|---|
| AUC (0−t) | hr·μg/ml | 1.87 ± 0.23 | 1.60 ± 0.18 |
| AUC (0−∞) | hr·μg/ml | 2.05 ± 0.18 | 1.89 ± 0.08 |
| MRT (0−t) | h | 5.73 ± 0.63 | 7.71 ± 0.45 |
| MRT (0−∞) | h | 8.19 ± 0.66 | 12.20 ± 2.90 |
| t 1/2 | h | 8.26 ± 1.88 | 6.03 ± 0.28 |
| t max | h | 0.5 | 0.5 |
| CLz | ml/hr/kg | 24.48 ± 2.25 | 26.46 ± 1.10 |
| Vz | ml/kg | 213.80 ± 29.93 | 31.65 ± 78.86 |
| Cmax | μg/ml | 0.52 ± 0.11 | 0.32 ± 0.08 |
Forty-two SD male rats were intraperitoneally administrated with SHY-01 (50 mg/kg) or Metformin hydrochloride (50 mg/kg). Brain samples were collected after sacrifice at 0.5, 1, 2, 4, 8, 12, and 24 h (three rats each time point per drug). The concentration of metformin in brain were analyzed by LC-MS/MS. The pharmacokinetic parameters of SHY-01 and metformin hydrochloride were calculated accordingly. The results are presented as means ± SD (n = 3/group).