Table 1.
Pharmacokinetic parameters following intranasal administration of insulin plus TCTP-PTD analogs in normal rats.
| Formulation | Dose (IU/kg) | Tmax (min) | Cmax (μU/mL) | AUC (μU/mL·min) | BA (%) |
|---|---|---|---|---|---|
| Insulin alone | 5 | 16.0 ± 2.4 | 4.9 ± 0.9 | 180.5 ± 37.6 | 0.4 ± 0.1 |
| +0.1 mM l-TCTP-PTD 13 | 1 | 12.0 ± 2.0 | 26.4 ± 7.8 | 847.1 ± 132.9 | 9.0 ± 1.4 |
| +0.1 mM l-TCTP-PTD 13M1 | 1 | 10.0 ± 0.0 | 47.1 ± 3.1 | 1966.3 ± 130.5 | 20.9 ± 1.4 |
| +0.1 mM l-TCTP-PTD 13M2 | 1 | 10.0 ± 0.0 | 64.5 ± 4.0 | 2121.9 ± 306.2 | 22.5 ± 3.2 |
| +0.25 mM l-TCTP-PTD 13 | 1 | 10.0 ± 0.0 | 53.4 ± 6.7 | 2081.7 ± 238.6 | 22.1 ± 2.5 |
| +0.25 mM l-TCTP-PTD 13M1 | 1 | 13.3 ± 2.1 | 15.0 ± 3.3 | 951.7 ± 225.9 | 10.1 ± 2.4 |
| +0.25 mM l-TCTP-PTD 13M2 | 1 | 10.0 ± 0.0 | 108.5 ± 8.7 | 3494.4 ± 284.7 | 37.1 ± 3.0 |
| +0.25 mM d-TCTP-PTD 13 | 1 | 14.0 ± 2.4 | 13.8 ± 4.2 | 645.5 ± 191.2 | 6.8 ± 2.0 |
| +0.25 mM d-TCTP-PTD 13M2 | 1 | 13.0 ± 3.0 | 23.0 ± 5.0 | 949.7 ± 243.6 | 10.1 ± 2.6 |
| Insulin (s.c.) | 0.25 | 14 .0 ± 4.8 | 40.9 ± 0.9 | 2356.4 ± 106.2 | 100 |
Values are expressed as means ± SEM (n = 5–7).
AUC: area under the curve; BA: relative bioavailability compared to s.c.; Cmax: maximum concentration; s.c.: subcutaneous; Tmax: time to reach maximum concentration (Cmax).