Table 1.
Summary pharmacokinetics statistics after administration of gabapentin as a single IV bolus (5 mg/kg; n = 8), a single oral dose (10 mg/kg; n = 7), and repeated oral doses (10 mg/kg; n = 7)
| Parameter | IV | Single oral | Repeated oral |
|---|---|---|---|
| F (%) | * | 94.8 (82.5‐122.8) | * |
| K01 (1/hr) | * | 5.24 (1.77‐15.62) | 7.06 (1.32‐11.46) |
| K10 (1/hr) | 1.21 (0.87‐1.67) | 0.20 (0.14‐0.23) | 0.18 (0.15‐0.22) |
| K12 (1/hr) | 13.67 (8.35‐25.46) | * | * |
| K21 (1/hr) | 2.82 (1.88‐5.12) | * | * |
| V1 (mL/kg) | 129.09 (80.35‐171.50) | * | * |
| TLAG (hr) | * | 0.45a (0.24‐0.72) | 0.21a (0.01‐0.23) |
| A (μg/mL) | 32.77 (23.79‐55.89) | * | * |
| α (1/hr) | 16.97 (11.15‐31.74) | * | * |
| α T1/2 (hr) | 0.04 (0.02‐0.06) | * | * |
| B (μg/mL) | 5.61 (4.21‐6.80) | * | * |
| β (1/hr) | 0.18 (0.15‐0.22) | * | * |
| β T1/2 (hr) | 3.78 (3.12‐4.47) | * | * |
| AUC (hr*μg/mL) | 32.01 (24.61‐42.38) | 73.68 (55.71‐107.19) | 77.25 (66.26‐121.06) |
| CL (mL/kg/hr) | 160.67 (119.63‐199.11) | * | * |
| CMAX (μg/mL) | * | 12.42 (8.31‐18.35) | 14.78 (9.70‐18.41) |
| K01 T1/2 (hr) | * | 0.13 (0.04‐0.39) | 0.10 (0.06‐0.53) |
| K10 T1/2 (hr) | * | 3.53 (2.96‐4.78) | 3.90 (3.12‐4.51) |
| MRT (hr) | 5.17 (4.34‐6.05) | * | * |
| VSS (mL/kg) | 804.57 (643.71‐1049.90) | * | * |
| TMAX (hr) | * | 1.05 (0.74‐2.11) | 0.77 (0.58‐1.64) |
Results are presented as median (range). F, bioavailability, or fraction absorbed unchanged; K01, absorption rate constant to the central compartment; K10, elimination rate constant from the central compartment; K12, distribution rate constant from the central (1) to peripheral compartment (2); K21, distribution rate constant from the peripheral (2) to central compartment (1); V1, apparent volume of the central compartment; TLAG, lag time or delay for drug absorption following oral administration; A and B, and α and β = Coefficients and exponents, respectively, in the following equation used describe the drug disposition curve at time t: (A X e–αt) + (B X e–βt), where e is Euler's number (2.7183); T1/2, half‐life; α T1/2, plasma or distribution half‐life after IV administration; β T1/2, elimination half‐life after IV administration; AUC, area under the curve for the concentration versus time profile; CL, systemic clearance; CMAX, peak concentration; K01 T1/2, absorption half‐life after oral administration; K10 T1/2, elimination half‐life after oral administration; VSS, apparent volume of distribution at steady state, TMAX time to peak concentration.
Statistically significant difference (P = .0052).