Table 2.
Pharmacokinetic parameters of CPT-11, SN-38, and SN-38G in control and SXD-treated rats after intravenous administration of CPT-11 at 20 mg/kg (n = 6, Mean ± SEM).
Analytes | Pharmacokinetic parameters | Groups | |
---|---|---|---|
SXD-treated | Control | ||
CPT-11 | AUC0 → 24h (h*ng/mL) | 10022.75 ± 1049.02* | 7016.64 ± 661.96 |
AUC0 → ∞ (h*ng/mL) | 10070.14 ± 1056.34* | 7100.89 ± 682.87 | |
C0 (ng/mL) | 4690.05 ± 306.47*** | 2587.52 ± 148.94 | |
MRT (h) | 1.90 ± 0.16 | 2.23 ± 0.16 | |
CLobs (mL/h/kg) | 2117.13 ± 258.05* | 2947.11 ± 273.08 | |
Vd (mL/kg) | 5747.81 ± 1051.19 | 10134.97 ± 1980.99 | |
t(1/2) (h) | 1.94 ± 0.37 | 2.42 ± 0.45 | |
SN-38 | AUC0 → 24h (h*ng/mL) | 963.02 ± 60.52** | 1605.39 ± 165.09 |
AUC0 → ∞ (h*ng/mL) | 979.67 ± 67.41** | 1642.37 ± 175.95 | |
Cmax (ng/mL) | 179.50 ± 34.31*** | 325.33 ± 26.45 | |
MRT (h) | 4.77 ± 0.32 | 4.93 ± 0.23 | |
t(1/2) (h) | 3.89 ± 0.34 | 4.33 ± 0.29 | |
AUC ratio SN-38/CPT-11 (%) | 10.18 ± 1.50*** | 22.84 ± 2.02 | |
SN-38G | AUC0 → 24h (h*ng/mL) | 518.80 ± 38.19 | 420.89 ± 57.47 |
AUC0 → ∞ (h*ng/mL) | 590.43 ± 39.43 | 495.02 ± 89.53 | |
Cmax (ng/mL) | 117.53 ± 9.88** | 63.03 ± 8.19 | |
MRT (h) | 6.98 ± 0.43 | 7.51 ± 0.45 | |
t(1/2) (h) | 8.17 ± 2.36 | 7.66 ± 1.43 | |
AUC ratio SN-38G/SN-38 (%) | 54.62 ± 4.29** | 27.69 ± 4.98 |
Statistical difference between control and SXD-treated rats,
p < 0.05,
p < 0.01,
p < 0.001.